PF-03882845

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PF-03882845 是一种高效、选择性、非类固醇、口服生物可利用的盐皮质激素受体拮抗剂，IC50 为 4.5 nM。

PF-03882845 is highly potent, selective, nonsteroidal, orally bioavailable Mineralocorticoid receptor antagonist with IC50 of 4.5 nM; displays >500-fold selectivity versus PR and other related nuclear hormone receptors; significantly increases urinary Na(+)/K(+) ratio in vivo; prevents renal injury with reduced risk of hyperkalemia in an animal model of nephropathy.Diabetes Phase 1 Discontinued.

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PF-3882845 reduces blood pressure, decreases urinary albumin, and protects kidney in Dahl SS rat. PF-3882845 exhibits moderate oral bioavailability (F 86%) following oral administration (2 mg/kg) in male Sprague-Dawley rats.PF-3882845 exhibits terminal elimination half-lives (T1/2 1.7 h) due to high plasma clearance (CL 9.8 mL/min/kg) combined with large volumes of distribution (Vdss 1.4 mL/kg respectively) following intravenous administration (2 mg/kg) in male Sprague-Dawley rats. Animal Model:Male Dahl salt sensitive (SS) rats Dosage:10, 40, and 100 mg/kg Administration:Orally via gavage; twice a day; for 21 days Result:Significant blood pressure reduction was observed with 10 mg/kg. Most noticeably, rats dosed at 40 and 100 mg/kg had negligible increase in blood pressure over 21 days in the presence of high salt.

PF03882845

Nuclear Receptor/Transcription Factor

MLR

MLR

Metabolic Disease

Diabetes

1023650-66-9

419.91

C24H22ClN3O2

>98% (HPLC)

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C1CCC(C1)C2C3CCC4=C(C3=NN2C5=CC(=C(C=C5)C#N)Cl)C=CC(=C4)C(=O)O

(3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid

(-20℃)

With Ice Pack

≥ 2 years