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Umeclidinium bromide

Catalog No. A15268
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Muscarinic receptor 拮抗剂

Umeclidinium bromide (GSK573719A)是毒蕈碱受体拮抗剂，可用于治疗慢性阻塞性肺疾病（COPD）。了解更多

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LDE225 (NVP-LDE225, Sonidegib)

Catalog No. A10520
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Smo 拮抗剂

LDE225 (NVP-LDE225)是一种强效、选择性和口服生物可利用的平滑(SMO)拮抗剂，通过平滑受体(SMO)的拮抗作用抑制hedgehog (Hh)信号通路。了解更多

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- Daniel Doheny, .et al. Combined inhibition of JAK2-STAT3 and SMO-GLI1/tGLI1 pathways suppresses breast cancer stem cells, tumor growth, and metastasis, Oncogene, 2020, Oct;39(42):6589-6605 PMID: 32929154
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Proparacaine HCl

Catalog No. A11715
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Voltage-gated sodium channels 拮抗剂

Proparacaine HCl是一种电压门控钠通道拮抗剂，ED50为3.4 mM。了解更多

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Telmisartan

Catalog No. A10905
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AT1 拮抗剂

Telmisartan是一种抑制血管紧张素II AT1受体的血管紧张素II受体拮抗剂。了解更多

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N-Desmethylclozapine

Catalog No. A13762
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5-HT2C serotonin receptor 拮抗剂

N-Desmethylclozapine是一种有效的选择性5-HT2C血清素受体拮抗剂。了解更多

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Macitentan

Catalog No. A11492
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Endothelin receptor 拮抗剂

Macitentan是一种口服活性非肽双重ETA/ETB(内皮素) receptor双重拮抗剂，IC50为0.5 nM/391 nM。用于治疗特发性肺纤维化(IPF)和肺动脉高压(PAH)。了解更多

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RS-127445

Catalog No. A11165
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5-HT2B receptor 拮抗剂

RS-127445是5-羟色胺5-HT2B受体的有效和选择性拮抗剂，相对于密切相关的5-HT2A和5-HT2C受体具有约1000倍的选择性。了解更多

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- Takeshi Takayanagi, .et al. Serotonin 5-HT2B receptor antagonism is fundamental for protecting PC12 cells exposed to hydrogen peroxide, Fujita Medical Journal, 2015, 1(1), 1-5, 2015
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Asenapine maleate

Catalog No. A10091
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H1 拮抗剂

Asenapine maleate平对多种受体具有高亲和力（pKi），包括5-羟色胺5-HT1A（8.6），5-HT1B（8.4），5-HT2A（10.2），5-HT2B（9.8），5-HT2C（10.5），5 -HT5A（8.8），5-HT6（9.5）和5-HT7（9.9）受体，肾上腺素α1（8.9），α2A（8.9），α2B（9.5）和α2C（8.9）受体，多巴胺D1（ 8.9），D2（8.9），D3（9.4）和D4（9.0）受体以及组胺H1（9.0）和H2（8.2）受体。了解更多

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- Keisuke Obara, .et al. Inhibitory Effects of Antipsychotics on the Contractile Response to Acetylcholine in Rat Urinary Bladder Smooth Muscles, Biol Pharm Bull, 2021, 44, 1140-1150
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AM251

Catalog No. A12914
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CB1 receptor 拮抗剂

AM251是有效的CB1受体拮抗剂（IC50 = 8 nM，Ki = 7.49 nM），其选择性是CB2受体的306倍。了解更多

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- Potential for pharmacological manipulation of human embryonic stem cells. Br J Pharmacol. 2013 May; 169(2): 269–289.
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MK-571

Catalog No. A12529
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CysLT1 receptor 拮抗剂

MK-571是有效的CysLT1（LTD4）白三烯受体反向激动剂，EC50值为1.3 nM。了解更多

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- Jung-Hung Chen, .et al. Transplacental transfer of acetaminophen in pregnant rats, Biomed Pharmacother, 2022, Oct;154:113613 PMID: 36058146
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Eprosartan

Catalog No. A11121
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AT1 receptor 拮抗剂

Eprosartan是一种用于治疗高血压的血管紧张素II受体拮抗剂。了解更多

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Gallamine triethiodide

Catalog No. A10417
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mAChR M2 拮抗剂

Gallamine Triethiodide是一种具有显著心脏选择性的mAChR M2拮抗剂。了解更多

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Tasosartan

Catalog No. A10891
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Angiotensin II receptor 拮抗剂

Tasosartan是一种血管紧张素II受体拮抗剂。了解更多

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Flavoxate

Catalog No. A12900
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muscarinic AChR antagonist

Flavoxate结合并抑制毒蕈碱受体，从而通过改变脑干的排尿中心来抑制排尿反射并增加膀胱容量。了解更多

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Tolterodine tartrate (Detrol LA)

Catalog No. A10937
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muscarinic receptor 拮抗剂

Tolterodine tartrate (Detrol LA)是毒蕈碱受体拮抗剂。了解更多

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Tolvaptan

Catalog No. A11594
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vasopressin receptor 2 拮抗剂

Tolvaptan是一种选择性的竞争性精氨酸加压素受体2拮抗剂，IC50为1.28μM。了解更多

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GDC-0152

Catalog No. A14135
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IAP 拮抗剂

GDC-0152是caspases（Smac）的第二个线粒体激活物，具有潜在的抗肿瘤活性。了解更多

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Flupirtine maleate

Catalog No. A10251
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NMDA 拮抗剂

Flupirtine maleate是Flupirine的盐形式，是一种非阿片类中枢性镇痛药，是一种选择性的神经元钾离子通道开放剂，也具有NMDA受体拮抗剂特性。了解更多

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Plerixafor 8HCl (DB06809)

Catalog No. A10913
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CXCR4 拮抗剂

Plerixafor 8HCl (DB06809)是CXCR4趋化因子受体拮抗剂，作用于CXCR4和CXCL12介导调节的趋化性， IC50分别为44 nM和5.7 nM。了解更多

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- Mei Zheng, .et al. CXCL12 inhibits hair growth through CXCR4, Biomed Pharmacother, 2022, Jun;150:112996 PMID: 35462338
- Asiedu KO, .et al. Bone marrow cell homing to sites of acute tibial fracture: 89Zr-oxine cell labeling with positron emission tomographic imaging in a mouse model, EJNMMI Res, 2018, Dec 13;8(1):109 PMID: 30547233
- Kingsley O. Asiedu, .et al. Bone marrow cell trafficking analyzed by 89Zr-oxine positron emission tomography in a murine transplantation model, Clin Cancer Res, 2017, Jun 1; 23(11): 2759-2768 PMID: 27965305
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SB 334867

Catalog No. A12786
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OX1 receptor 拮抗剂

SB 334867是一种选择性的非肽orexin OX1受体拮抗剂。对于分别表达人OX1和OX2受体的CHO细胞中的细胞内Ca2 +释放抑制，pKb值为7.2和<5。体内全身给药后，阻断orexin-A诱导的美容和进食。了解更多

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- Tony Ngo, .et al. Orphan receptor ligand discovery by pickpocketing pharmacological neighbors, Nat Chem Biol, 2017, Feb; 13(2): 235-242 PMID: 27992882
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JNJ-31020028

Catalog No. A14332
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neuropeptide Y Y2 receptor 拮抗剂

JNJ-31020028是一种新型的选择性脑渗透神经肽Y Y2受体拮抗剂。了解更多

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Bicalutamide (Casodex)

Catalog No. A10142
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Androgen Receptor 拮抗剂

Bicalutamide (Casodex)是一种口服非甾体抗雄激素，用于治疗前列腺癌和多毛症。了解更多

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- Mi Chen, .et al. TRIM33 drives prostate tumor growth by stabilizing androgen receptor from Skp2-mediated degradation, EMBO Rep, 2022, Aug 3;23(8):e53468 PMID: 35785414
- Takashi Azuma, .et al. Removal of pharmaceuticals in water by introduction of ozonated microbubbles, SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Anowara Khatun, .et al. Transcriptional Repression and Protein Degradation of the Ca2+-Activated K+ Channel KCa1.1 by Androgen Receptor Inhibition in Human Breast Cancer Cells, Front Physiol, 2018, 9: 312 PMID: 29713287
- Azuma T, .et al. Distribution of six anticancer drugs and a variety of other pharmaceuticals, and their sorption onto sediments, in an urban Japanese river, Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. Detection of pharmaceuticals and phytochemicals together with their metabolites in hospital effluents in Japan, and their contribution to sewage treatment plant influents, Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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Tamoxifen Citrate

Catalog No. A10885
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Estrogen receptor 拮抗剂

Tamoxifen Citrate是哺乳动物甾醇异构酶的选择性和有效抑制剂。了解更多

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- Renu Sudhakar, .et al. Bazedoxifene, a Postmenopausal Drug, Acts as an Antimalarial and Inhibits Hemozoin Formation, Microbiol Spectr, 2022, Jun 29;10(3) PMID: 35616371
- Takashi Azuma, .et al. Removal of pharmaceuticals in water by introduction of ozonated microbubbles, SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. Distribution of six anticancer drugs and a variety of other pharmaceuticals, and their sorption onto sediments, in an urban Japanese river, Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. Detection of pharmaceuticals and phytochemicals together with their metabolites in hospital effluents in Japan, and their contribution to sewage treatment plant influents, Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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Paliperidone

Catalog No. A10691
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Dopamine Receptor 拮抗剂

Paliperidone (Invega)是一种非典型的抗精神病药。了解更多

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- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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Otenabant

Catalog No. A15200
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CB1 receptor 拮抗剂

Otenabant是最近发现的选择性，高亲和力，竞争性CB1受体拮抗剂，Ki为0.7 nM。了解更多

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Ki16425

Catalog No. A10501
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LPA Receptor 拮抗剂

ki16425是对LPA1和LPA3具有选择性的LPA受体拮抗剂，对人LPA1、LPA2和LPA3受体分别显示Ki值为0.34、6.5和0.93 μM。了解更多

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- Maria F Fernandes, .et al. Glucagon-like Peptide-1 Secretion Is Inhibited by Lysophosphatidic Acid, Int J Mol Sci, 2022, Apr 9;23(8):4163 PMID: 35456981
- Rieko Suenaga, .et al. Lateral access mechanism of LPA receptor probed by molecular dynamics simulation, PLoS One, 2022, Feb 3;17(2):e0263296 PMID: 35113924
- Inoue A, .et al. Illuminating G-Protein-Coupling Selectivity of GPCRs, Cell, 2019, Jun 13;177(7):1933-1947 PMID: 31160049
- Taniguchi R, .et al. Structural insights into ligand recognition by the lysophosphatidic acid receptor LPA6, Nature, 2017, Aug 17;548(7667):356-360 PMID: 28792932
- T. HASHIMOTO, .et al. Generalized pruritus in primary sclerosing cholangitis: implications of histamine release by lysophosphatidic acid., Br J Dermatol., 2015, Nov;173(5):1334-6 PMID: 26122943
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Memantine hydrochloride

Catalog No. A11708
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NMDA receptor 拮抗剂

Memantine hydrochloride是nmda受体的拮抗剂，与离子通道位点结合。它还是CYP2B6和CYP2D6抑制剂，作用于重组CYP2B6和CYP2D6，Ki分别为0.51 nM和94.9 μM。它被用于治疗帕金森综合征。了解更多

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Reversine

Catalog No. A13250
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human A3 adenosine receptor 拮抗剂 /Aurora 抑制剂

Reversine是一种有效的人A3腺苷受体拮抗剂，Ki为0.66μM，是一种泛光A/B/C激酶抑制剂，IC50分别为12 nM/13 nM/20 nM。也用于干细胞去分化。了解更多

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- Hazheen K, .et al. BuGZ facilitates loading of spindle assembly checkpoint proteins to kinetochores in early mitosis, J Biol Chem, 2020, August 20
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Endoxifen

Catalog No. A12639
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Estrogen receptor 拮抗剂

Endoxifen是他莫昔芬的次生代谢产物。它是负责他莫昔芬在ER阳性乳腺癌中有效性的主要代谢物。Endoxifen Z-isomer抑制hERG, 这种作用具有浓度依赖性, IC50值为1.6μM。了解更多

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- Marina Arino Martin, .et al. Photolytic fate of (E)- and (Z)-endoxifen in water and treated wastewater exposed to sunlight, Environ Res, 2021, Apr 3;197:111121 PMID: 33823193
- Martin MA, .et al. Photodegradation of (E)- and (Z)-Endoxifen in water by ultraviolet light: Efficiency, kinetics, by-products, and toxicity assessment, Water Res, 2019, Dec 29;171:115451 PMID: 31901682
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Cyproterone acetate

Catalog No. A11409
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Androgen Receptor 拮抗剂

Cyproterone acetate是17-羟孕酮的合成衍生物，可作为雄激素受体拮抗剂以及具有弱孕激素和糖皮质激素活性的弱孕激素受体激动剂。了解更多

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AMD 3465 Hexahydrobromide

Catalog No. A11953
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CXCR4 拮抗剂

AMD 3465 Hexahydrobromide是一种有效的选择性CXCR4拮抗剂。了解更多

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- Kentaro Suzuki, .et al. C-terminal-modifed LY2510924: a versatile scafold for targeting C-X-C chemokine receptor type 4, Sci Rep, 2019, 9: 15284
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MDL 29951

Catalog No. A13729
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NMDA receptor 拮抗剂

MDL-29951是在体外和体内均能激活NMDA受体的新型甘氨酸拮抗剂（Ki = 0.14 mM，[3H]甘氨酸结合）。了解更多

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S1RA (E-52862)

Catalog No. A12504
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sigma-1 receptor 拮抗剂

S1RA是一种选择性sigma-1受体拮抗剂，据报道其结合亲和力为Ki = 17.0±7.0 nM，对sigma-2受体具有选择性，并且对其他170种受体，酶，转运蛋白和离子通道具有选择性。了解更多

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AZD1283

Catalog No. A15443
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P2Y12 receptor 拮抗剂

AZD1283是P2Y12受体的有效拮抗剂，EC50为3.0 ug/kg/min，TI> 10；结合IC50为11 nM。了解更多

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Nutlin-3

Catalog No. A10657
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Mdm2 拮抗剂

Nutlin-3是一种有效的，选择性Mdm2(它自身和p53的环指依赖性泛素蛋白连接酶)拮抗剂，是有效的凋亡诱导剂。了解更多

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- Maxime Parisotto, .et al. PTEN deletion in luminal cells of mature prostate induces replication stress and senescence in vivo, J Exp Med, 2018, Jun 4; 215(6): 1749-1763 PMID: 29743291
- Ohmuro-Matsuyama Y, .et al. Evaluation of protein-ligand interactions using the luminescent interaction assay FlimPIA with streptavidin-biotin linkage, Anal Biochem, 2018, Dec 15;563:61-66 PMID: 30316750
- Alisa A. Garaeva, .et al. Mitochondrial dysfunction induces SESN2 gene expression through Activating Transcription Factor 4, Cell Cycle, 2016, 15(1): 64-71 PMID: 26771712
- A G Evstafieva, .et al. A sustained deficiency of mitochondrial respiratory complex III induces an apoptotic cell death through the p53-mediated inhibition of pro-survival activities of the activating transcription factor 4, Cell Death Dis., 2014, 5(11): e1511. PMID: 25375376
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MK-0517 (Fosaprepitant)

Catalog No. A11756
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neurokinin-1 receptor 拮抗剂

MK-0517 (Fosaprepitant,L-758,298)是Aprepitant的水溶性磷酰基前药，它是NK1拮抗剂。了解更多

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XCT 790

Catalog No. A13299
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ERRα 拮抗剂/inverse 激动剂

XCT 790是ERRα的强效特异性反向激动剂。了解更多

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A-804598

Catalog No. A16066
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P2X7 receptor 拮抗剂

A-804598是一种P2X7选择性竞争性拮抗剂，对人，大鼠和小鼠通道的IC50值分别为11、10和9 nM。了解更多

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Biperiden HCl

Catalog No. A10147
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Muscarinic receptor antagonist

Biperiden HCl是毒蕈碱受体拮抗剂，对M1亚型表现出一定的选择性。了解更多

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MK-4305 (Suvorexant)

Catalog No. A11500
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OX receptor 拮抗剂

Suvorexant (MK-4305)是OX1R和OX2R的有效，选择性和口服可生物利用的拮抗剂，目前正在临床研究中作为失眠的新疗法。了解更多

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- Richard L Spinieli, .et al. Orexin contributes to eupnea within a critical period of postnatal development, Am J Physiol Regul Integr Comp Physiol, 2021, Oct 1;321(4):R558-R571 PMID: 34405704
- Jacob W Clark, .et al. Manipulation of REM sleep via orexin and GABAA receptor modulators differentially affects fear extinction in mice: effect of stable versus disrupted circadian rhythm, Sleep, 2021, Mar 15;zsab068 PMID: 33720375
- Zhang B, .et al. Hypothalamic orexin and mechanistic target of rapamycin activation mediate sleep dysfunction in a mouse model of tuberous sclerosis complex, Neurobiol Dis, 2019, Oct 9;134:104615 PMID: 31605778
- Obara K, .et al. Assessment of Inhibitory Effects of Hypnotics on Acetylcholine-Induced Contractions in Isolated Rat Urinary Bladder Smooth Muscle, Biol Pharm Bull, 2019, 42(2):280-288 PMID: 30713259
- James B Jaggard, .et al. Hypocretin underlies the evolution of sleep loss in the Mexican cavefish, eLife, 2018, 7: e32637 PMID: 29405117
- Skillman B, .et al. Quantification of suvorexant in blood using liquid chromatography-quadrupole/time of flight (LC-Q/TOF) mass spectrometry, J Chromatogr B Analyt Technol Biomed Life Sci, 2018, Aug 1;1091:87-95 PMID: 29859493
- Clark L, .et al. On the use of Pichia pastoris for isotopic labeling of human GPCRs for NMR studies, J Biomol NMR, 2018, Aug;71(4):203-211 PMID: 30121871
- Sullinger S, .et al. Identification of Suvorexant in Urine Using Liquid Chromatography-Quadrupole/Time-of-Flight Mass Spectrometry (LC-Q/TOF-MS), J Anal Toxicol, 2017, Apr 1;41(3):224-229 PMID: 28035034
- Carson M, .et al. Quantification of suvorexant in urine using gas chromatography/mass spectrometry, J Chromatogr B Analyt Technol Biomed Life Sci, 2017, Jan 1;1040:289-294 PMID: 27825624
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SB-742457

Catalog No. A14092
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5-HT6 receptor 拮抗剂

SB-742457是一种选择性的5-HT6受体拮抗剂，具有认知，记忆和增强学习的作用。了解更多

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Alvimopan (ADL 8-2698)

Catalog No. A11292
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Opioid 拮抗剂

Alvimopan (ADL 8-2698)表现为外周作用的opioid拮抗剂，Alvimopan竞争性结合胃肠道中的mu-opioid receptor。了解更多

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Birinapant (TL32711)

Catalog No. A12738
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XIAP/cIAP1 拮抗剂

Birinapant (TL32711)是第二个线粒体衍生的胱天蛋白酶（SMAC）激活剂和IAP（凋亡蛋白抑制剂）家族蛋白抑制剂的合成小分子和肽类似物，对cIAP1最有效，无细胞试验中Kd为<1 nM，具有潜在的抗肿瘤活性。了解更多

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AM966

Catalog No. A13982
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LPA1 receptor 拮抗剂

AM966是LPA1受体（溶血磷脂酸受体）的高亲和力，选择性口服拮抗剂，IC50值为17 nM。了解更多

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- Maria F Fernandes, .et al. Glucagon-like Peptide-1 Secretion Is Inhibited by Lysophosphatidic Acid, Int J Mol Sci, 2022, Apr 9;23(8):4163 PMID: 35456981
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MDV3100

Catalog No. A10562
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Androgen receptor 拮抗剂

MDV3100(Enzalutamide)是一种androgen-receptor (AR)拮抗剂。在AR研究中强烈推荐的抑制剂。了解更多

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- Shiv Verma, .et al. Increased cytokine gene expression and cognition risk associated with androgen deprivation therapy, Prostate, 2022, Oct;82(14):1389-1399 PMID: 35821621
- Mi Chen, .et al. TRIM33 drives prostate tumor growth by stabilizing androgen receptor from Skp2-mediated degradation, EMBO Rep, 2022, Aug 3;23(8):e53468 PMID: 35785414
- Prem P Kushwaha, .et al. Role of solute carrier transporters SLC25A17 and SLC27A6 in acquired resistance to enzalutamide in castration-resistant prostate cancer, Mol Carcinog, 2021, Dec 22 PMID: 34939235
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Alosetron

Catalog No. A11310
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5-HT3 拮抗剂

Alosetron是一种5-HT3拮抗剂，对胃肠道肠道神经系统的5-HT3受体具有拮抗作用。了解更多

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GSK 0660

Catalog No. A12392
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PPARδ 拮抗剂

GSK 0660是一种选择性PPARβ拮抗剂（在PPARβ，PPARα和PPARγ处，IC50值分别为0.155，> 10和≥10 ?M）。了解更多

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(-)-MK 801 maleate

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NMDA receptor 拮抗剂.

(-)-MK 801 maleate是一种有效的、选择性的、非竞争性的NMDA受体拮抗剂。它通过与NMDA相关离子通道内的一个位点结合而起作用。了解更多

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LY2940680 (Taladegib)

Catalog No. A11048
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SMO 拮抗剂

LY2940680 (Taladegib)已显示可影响由Hedgehog（Hh）蛋白引发的癌细胞信号通路。了解更多

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SB269970 HCl

Catalog No. A11925
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5-HT7 receptor 拮抗剂

SB269970 HCl是有效的选择性5-HT7受体拮抗剂。了解更多

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