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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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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

Product Citations (5)

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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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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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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

Product Citations (5)

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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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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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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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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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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

Product Citations (4)

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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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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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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

Product Citations (9)

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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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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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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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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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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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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

Product Citations (1)

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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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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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ICI 118,551 hydrochloride

Catalog No. A13225
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β2 adrenergic 拮抗剂

ICI 118,551 hydrochloride是选择性的β2 adrenergic receptor 拮抗剂,结合 β2，β1 和 β3 肾上腺素能受体的Ki 值分别为 0.7，49.5 和 611 nM。了解更多

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(-)-MK 801 maleate

Catalog No. A13435
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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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SB-705498

Catalog No. A11143
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TRPV1 拮抗剂

SB-705498是有效，选择性和口服生物利用的TRPV1拮抗剂，抑制TRPV1的Capsaicin，酸和热激活，IC50分别为3 nM， 0.1 nM和6 nM，该作用具有一定的电压依赖性，作用于TRPV1比作用于TRPM8选择性高100倍以上。了解更多

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Buflomedil HCl

Catalog No. A11737
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VEGFR 拮抗剂

Buflomedil HCl是一种用于治疗外周血管疾病的血管活性剂。了解更多

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AR7

Catalog No. A12905
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RARα 拮抗剂.

AR7是视黄酸受体α(RARα)拮抗剂。了解更多

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WAY-100635 maleate salt

Catalog No. A15282
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5HT1A 拮抗剂

WAY-100635 maleate salt是一种有效的、选择性的5-羟色胺1A拮抗剂，对5-HT的IC50为0.95-0.12 nM。了解更多

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5-hydroxymethyl tolterodine (PNU 200577)

Catalog No. A11166
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muscarinic receptor 拮抗剂

5-hydroxymethyl tolterodine (PNU 200577)是托特罗定的代谢产物，tolterodine是一种用于治疗尿失禁的毒蕈碱受体拮抗剂。了解更多

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Dyphylline

Catalog No. A10339
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Adenosine receptor 拮抗剂

Dyphylline是黄嘌呤衍生物，具有支气管扩张药和血管扩张药的作用。它充当腺苷受体拮抗剂和磷酸二酯酶抑制剂。了解更多

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SIB 1757

Catalog No. A13758
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mGluR 拮抗剂

SIB 1757是mGlu5代谢型谷氨酸受体亚型的高度选择性拮抗剂。了解更多

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(+)-MK 801 Maleate

Catalog No. A12761
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NMDA receptor 拮抗剂

(+)-MK 801 Maleate是NMDA的有效拮抗剂，Ki值为30.5nM。了解更多

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Ginkgolide B

Catalog No. A10429
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PAFR 拮抗剂

Ginkgolide B (BN 52021)是一种PAFR拮抗剂，IC50为3.6 μM。了解更多

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Granisetron Hydrochloride

Catalog No. A10437
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5-HT3 receptor 拮抗剂

Granisetron Hydrochloride是血清素5-ht3受体拮抗剂。了解更多

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JNJ7777120

Catalog No. A12713
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Histamine 拮抗剂

JNJ7777120是有效的，选择性的非咪唑histamine H4 receptor拮抗剂。了解更多

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- K Yamamoto, .et al. Activation of orexinergic and histaminergic pathway involved in therapeutic effect of histamine H4 receptor antagonist against cisplatin-induced anorexia in mice, Naunyn-Schmiedeberg's Arch Pharmacol, 2019, pp 1-12
- Yamamoto K, .et al. Effects of a histamine H4 receptor antagonist on cisplatin-induced anorexia in mice, Neurosci Lett, 2018, May 29;676:103-107 PMID: 29655943
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Flutamide

Catalog No. A10402
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Androgen receptor 拮抗剂

Flutamide是一种抗雄激素药物，其活性代谢洛丽塔与Ki值为55nM的雄激素受体结合，可作用于前列腺癌。了解更多

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Solifenacin succinate

Catalog No. A11215
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muscarinic M3 receptor antagoinst

Solifenacin succinate是毒蕈碱M3受体拮抗剂，用于治疗尿失禁。了解更多

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SB-408124

Catalog No. A11567
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OX Receptor 拮抗剂

SB-408124是一种选择性的非肽orexin OX1受体拮抗剂(人OX1和OX2受体的Kb值分别为21.7和1405 nM)。体内口服后阻断orexin-A诱导的修饰。了解更多

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RU 58841

Catalog No. A11541
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AR 拮抗剂

RU 58841，也称为PSK-3841或HMR-3841，是一种非甾体类抗雄激素药物。了解更多

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GDC-0449 (Vismodegib)

Catalog No. A10258
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Hedgehog 拮抗剂

GDC-0449 (Vismodegib)是一种新型有效的，特异性hedgehog抑制剂，IC50为3 nM。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
- Yi Yang, .et al. Tumidulin, a Lichen Secondary Metabolite, Decreases the Stemness Potential of Colorectal Cancer Cells, Molecules, 2018, Nov; 23(11): 2968 PMID: 30441806
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SYN-115 (Tozadenant)

Catalog No. A11560
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A2a receptor 拮抗剂

SYN115是口服，有效和选择性的腺苷2a（A2a）受体抑制剂，作用于人类和恒河猴的 adenosine A2A 受体，Ki 值分别为 11.5 nM 和 6 nM。了解更多

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Firategrast (SB 683699)

Catalog No. A12787
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α4β1/α4β7 integrin 拮抗剂

Firategrast (SB 683699)是一种口服可生物利用的alpha4 beta1/alpha4 beta7整联蛋白拮抗剂，旨在减少淋巴细胞向中枢神经系统（CNS）的运输。了解更多

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- Higuchi S, .et al. Inhibition of the integrin signal constitutes a mouse iPS cell niche, Dev Growth Differ, 2016, Sep;58(7):586-99 PMID: 27633818

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