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CAS No. : 195733-43-8
MCE 国际站:Atrasentan hydrochloride
产品活性:Atrasentan hydrochloride (ABT-627 hydrochloride) 是一种有效的选择性 内皮素 A 受体 (endothelin A receptor) 拮抗剂,抑制 ETA 的活性,IC50 值为 0.0551 nM。
研究领域:GPCR/G Protein
作用靶点:Endothelin Receptor
In Vitro: Atrasentan hydrochloride (ABT-627 hydrochloride) (0-50 μM) significantly inhibits LNCaP and C4-2b prostate cancer cell growth. Atrasentan profoundly induces several CYPs and drug transporters (e.g. 12-fold induction of CYP3A4 at 50 μM). It is a moderate P-gp inhibitor (IC50 in P388/dx cells=15.1±1.6 μM) and a weak BCRP inhibitor (IC50 in MDCKII-BCRP cells=59.8±11 μM).
In Vivo: Atrasentan hydrochloride (ABT-627 hydrochloride) (3 mg/kg, p.o.) inhibits the pressor response induced by big endothelin-1 (1 nmol/kg) in pithed rats. Aatrasentan (ABT-627, 10 mg/kg, i.p.) inhibits the C4-2b tumor growth within the bone environment to some extent in the SCID-hu model.
相关产品:Drug Repurposing Compound Library Plus | FDA-Approved Drug Library Plus | FDA-Approved Drug Library Mini | Bioactive Compound Library Plus | GPCR/G Protein Compound Library | FDA-Approved Drug Library | Anti-Cancer Compound Library | Drug Repurposing Compound Library | Anti-Cardiovascular Disease Compound Library | Endocrinology Compound Library | Anti-COVID-19 Compound Library | Orally Active Compound Library | Neurotransmitter Receptor Compound Library | FDA Approved & Pharmacopeial Drug Library | Angiogenesis-Related Compound Library | Rare Diseases Drug Library | EMA-Approved Drug Library | FDA-Approved Anticancer Drug Library | Anti-Prostate Cancer Compound Library | Coagulation and Anti-coagulation Compound Library | Heterocyclic Compound Library | Pain-Related Compound Library | Off-patent Drug Library | Antihypertensive Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | BQ-788 | [Asn18] Endothelin-1, human | TBC3711 | BQ-3020 TFA | Sparsentan | [Lys4] Sarafotoxin S6c | Nebentan potassium | Bosentan | Endothelin 1 (swine, human) (TFA) | Ambrisentan | Ro 46-2005 | [Ala2] Endothelin-3, human | ZD-1611 | PD-159020 | Aminaftone | A-192621 | Macitentan | Sulfisoxazole | Endothelin-3, human, mouse, rabbit, rat TFA | IRL 2500 | Carperitide acetate | Atrial Natriuretic Peptide (ANP) (1-28), rat TFA | ACT-373898 | Kendomycin | Zibotentan | BQ-123 TFA
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