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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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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

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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

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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
- Olesen UH, .et al. Topical delivery of vismodegib using ablative fractional laser and micro-emulsion formulation in vitro, Lasers Surg Med, 2018, Aug 28 PMID: 30152536
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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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SB225002

Catalog No. A14209
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CXCR2 拮抗剂

SB225002是一种有效的选择性CXCR2拮抗剂，IC50为22 nM，可抑制白介素IL-8与CXCR2的结合，选择性是其他测试的7-TMR的150倍以上。了解更多

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Maraviroc (UK-427857)

Catalog No. A10556
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CCR 拮抗剂

Maraviroc (UK-427857)是CCR5受体拮抗剂类别的抗逆转录病毒药物，用于治疗HIV感染。了解更多

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- Roman V Uzhachenko, .et al. Metabolic modulation by CDK4/6 inhibitor promotes chemokine-mediated recruitment of T cells into mammary tumors, Cell Rep, 2021, Apr 6;35(1):108944 PMID: 33826903
- Karampoor S, .et al. Maraviroc attenuates the pathogenesis of experimental autoimmune encephalitis, Int Immunopharmacol, 2020, Mar;80:106138 PMID: 32007705
- Taisuke Ito, .et al. CCR5 is a novel target for the treatment of experimental alopecia areata, JCIA, 2020, 22 January
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MRS 2578

Catalog No. A11486
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P2Y6 Receptor 拮抗剂

MRS 2578是P2Y6核苷酸受体的选择性拮抗剂。了解更多

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AMD3100 (Plerixafor)

Catalog No. A13074
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CXCR4 拮抗剂

AMD3100 (Plerixafor)是用于增殖造血干细胞的免疫刺激剂，并且是用于动员造血干细胞进行移植的趋化因子受体-4拮抗剂。了解更多

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- Hitoshi Maeda, .et al. Cell-penetrating albumin enhances the sublingual delivery of antigens through macropinocytosis, Int J Biol Macromol, 2022, Sep 17;221:1439-1452 PMID: 36126807
- Jingying Chen, .et al. Brain vascular damage-induced lymphatic ingrowth is directed by Cxcl12b/Cxcr4a, Development, 2022, Jul 1;149(13) PMID: 35694896
- Narubhorn Ongprakobkul, .et al. Effects of local vs systemic administration of CXCR4 inhibitor AMD3100 on orthodontic tooth movement in rats, Am J Orthod Dentofacial Orthop, 2022, Mar 2;S0889-5406(22)00107-X PMID: 35248418
- Chunliang Liu, .et al. Positive effects of selenium supplementation on selenoprotein S expression and cytokine status in a murine model of acute liver injury, J Trace Elem Med Biol, 2022, Jan 10;71:126927 PMID: 35030482
- Eri Watanabe, .et al. Stromal cell-derived factor 1 (SDF1) attenuates platelet-derived growth factor-B (PDGF-B)-induced vascular remodeling for adipose tissue expansion in obesity, Angiogenesis, 2020, Jul 22 PMID: 32699964
- Alessandra Esposito, .et al. Role of Prx1-expressing skeletal cells and Prx1-expression in fracture repair, Bone, 2020, Jul 3;139:115521 PMID: 32629173
- Kentaro Suzuki, .et al. C-terminal?Cmodifed LY2510924: a versatile scafold for targeting C-X-C chemokine receptor type 4, Sci Rep, 2019, 9: 15284
- Ichimizu S, .et al. Cell-penetrating mechanism of intracellular targeting albumin: Contribution of macropinocytosis induction and endosomal escape, J Control Release, 2019, May 10;304:156-163 PMID: 31082432
- Nan Li, .et al. LPS-induced CXCR7 expression promotes gastric Cancer proliferation and migration via the TLR4/MD-2 pathway, Diagn Pathol, 2019, Jan 12;14(1):3 PMID: 30636642
- Thida W, .et al. The role of conventional antibodies targeting the CD4 binding site and CD4-induced epitopes in the control of HIV-1 CRF01_AE viruses, Biochem Biophys Res Commun, 2018, Nov 20. pii: S0006-291X(18)32477-X PMID: 30470571
- Henry R. Hampton, .et al. Microbe-dependent lymphatic migration of neutrophils modulates lymphocyte proliferation in lymph nodes, Nat Commun, 2015, 6: 7139 PMID: 25972253
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Exherin (ADH-1)

Catalog No. A13689
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N-cadherin 拮抗剂

Exherin (ADH-1)是一种小的环状五肽血管靶向药物，具有潜在的抗肿瘤和抗血管生成活性。了解更多

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- CM Madl, .et al. Matrix Remodeling Enhances the Differentiation Capacity of Neural Progenitor Cells in 3D Hydrogels, Adv Sci, 2019, 1801716
- Christopher M. Madl, .et al. Maintenance of Neural Progenitor Cell Stemness in 3D Hydrogels Requires Matrix Remodeling, Nat Mater, 2017, Dec; 16(12): 1233-1242 PMID: 29115291
- Andrew J. Lindsay, .et al. Rab coupling protein mediated endosomal recycling of N-cadherin influences cell motility, Oncotarget, 2017, Dec 1; 8(62): 104717-104732 PMID: 29285208
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JTC-801

Catalog No. A11076
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Opioid Receptor 拮抗剂

JTC-801是nociceptin receptor（也称为ORL-1受体）的选择性拮抗剂。了解更多

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- Lihao Gu, .et al. 10-Hydroxy-2-Decenoic Acid in Royal Jelly Extract Induced Both Filaggrin and Amino Acid in a Cultured Human Three-Dimensional Epidermis Model, Cosmetics, 2017, 4(4), 48
- Toshio Yawata, .et al. Brain opioid and nociceptin receptors are involved in regulation of bombesin-induced activation of central sympatho-adrenomedullary outflow in the rat, Mol Cell Biochem, 2016, Jan;411(1-2):201-11 PMID: 26427671
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Orphenadrine citrate

Catalog No. A11712
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NMDA receptor 拮抗剂

Orphenadrine柠檬酸盐是NMDA受体拮抗剂，Ki为6.0μM，还是HERG钾离子通道阻断剂。了解更多

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GANT61

Catalog No. A13252
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GLI 拮抗剂

GANT61是GLI1和GLI2诱导的转录的抑制剂，以5μM的IC50抑制hedgehog，对其他途径（例如TNF和糖皮质激素受体基因反式激活）表现出选择性。了解更多

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- Cheng Zhou, .et al. GLI1 reduces drug sensitivity by regulating cell cycle through PI3K/AKT/GSK3/CDK pathway in acute myeloid leukemia, Cell Death Dis, 2021, Mar 3;12(3):231 PMID: 33658491
- Hui Liang, .et al. Targeting the PI3K/AKT pathway via GLI1 inhibition enhanced the drug sensitivity of acute myeloid leukemia cells, Sci Rep, 2017, 7: 40361 PMID: 28098170
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SB-222200

Catalog No. A15230
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NK3 receptor 拮抗剂

SB 222200是人类NK-3受体（Ki = 4.4 nM）的选择性，可逆和竞争性拮抗剂，可有效穿越血脑屏障。了解更多

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Aprepitant (MK-0869)

Catalog No. A10083
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neurokinin-1 receptor 拮抗剂

Aprepitant (MK-0869)被归类为NK1拮抗剂。已经显示，阿瑞匹坦通过阻止P物质降落在大脑神经元受体上，从而抑制细胞毒性化疗药物引起的急性呕吐和延迟呕吐。还显示出它能增加5-HT3受体拮抗剂恩丹西酮和皮质类固醇地塞米松的活性，它们也可用于预防化学疗法引起的恶心和呕吐。了解更多

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- Kodji X, .et al. Sensory nerves mediate spontaneous behaviors in addition to inflammation in a murine model of psoriasis, FASEB J, 2018, Sep 11:fj201800395RR PMID: 30204499
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Aminophylline

Catalog No. A10066
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Adenosine receptor 拮抗剂

Aminophylline是一种非选择性的腺苷受体拮抗剂和磷酸二酯酶抑制剂，能够逆转局部缺血引起的bradyasystole。了解更多

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TCS 1102

Catalog No. A13439
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Dual orexin receptor 拮抗剂

TCS 1102是一种有效的双重食欲素受体拮抗剂（OX2和OX1受体的Ki值分别为0.2和3 nM）。了解更多

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AM630

Catalog No. A14993
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CB2 拮抗剂

AM630是一种选择性CB2拮抗剂，Ki为31.2 nM，选择性是CB1受体的150倍以上。了解更多

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- Md Shah Sufian, .et al. Early suppression of the endocannabinoid degrading enzymes FAAH and MAGL alters locomotor development in zebrafish, J Exp Biol, 2021, 21 JUNE

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