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Phenoxybenzamine hydrochloride

Catalog No. A10719
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α-adrenergic (AR) 拮抗剂/CaM 抑制剂

Phenoxybenzamine hydrochloride是一种细胞可渗透的，非特异性的，不可逆的α-肾上腺素（AR）拮抗剂，也可作为CaM抑制剂。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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Sitaxsentan sodium (TBC-11251)

Catalog No. A11564
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ETA receptor 拮抗剂

Sitaxsentan sodium (TBC-11251)是一种选择性内皮素受体A拮抗剂，IC50和Ki分别为1.4 nM和0.43 nM。了解更多

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Felbamate

Catalog No. A11862
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Felbamate是NMDA相关甘氨酸结合位点的拮抗剂。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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(+)-Bicuculline

Catalog No. A12590
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GABAA 拮抗剂

(+)-Bicuculline是一种经典的GABAA拮抗剂。了解更多

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- Maryam Adenike Salaudeen, .et al. Anticonvulsant Activity of Tapinanthus dodoneifolius (DC.) Danser in Chicks and Mice: A Potential Source of Novel Anticonvulsant Agent, J Pharmacy and Drug Innovations, 2022, 3(4)
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WZ811

Catalog No. A12588
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CXCR4 拮抗剂

WZ811是4型C-X-C趋化因子受体（CXCR4）拮抗剂（EC50 = 0.3 nM）。在体外抑制CXCR4/基质细胞衍生因子1（SDF-1）介导的cAMP调节（EC50 = 1.2 nM）。了解更多

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MPEP

Catalog No. A12589
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mGlu5 receptor 拮抗剂

MPEP是mGlu5受体亚型（IC50 = 36 nM）的有效且高度选择性的非竞争性拮抗剂，并且是mGlu4受体的正构构调节剂。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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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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GSK-3787

Catalog No. A12391
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PPAR 拮抗剂

GSK-3787是一种有效的选择性过氧化物酶体增殖物激活受体δ（PPARδ）拮抗剂（pIC50 = 6.6）。了解更多

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