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BI-685509

Names

[ CAS No. ]:
1579514-06-9

[ Name ]:
BI-685509

Biological Activity

[Description]:

BI-685509 is a potent and orally active sGC activator. BI-685509 restores cyclic guanosine monophosphate (cGMP) and improves functionality of nitric oxide (NO) pathways. BI-685509 can be used in research of chronic kidney disease (CKD) and diabetic kidney disease (DKD)[1].

[Related Catalog]:

Research Areas >> Cardiovascular Disease
Signaling Pathways >> Others >> Others
Research Areas >> Metabolic Disease

[In Vitro]

BI 685509 在用血红素氧化剂 ODQ (HY-101255) 处理的人和大鼠富含血小板的血浆中增加 cGMP,EC50 值分别为 467 nM 和 304 nM[1]。

[In Vivo]

BI 685509 (1, 3, 10, 30 mg/kg; p.o.) 与 Enalapril (HY-B0331) 共同给药以剂量依赖性方式降低蛋白尿和肾小球硬化的发生率[1]。 BI 685509 (30 mg/kg; p.o.) 减少大鼠单侧输尿管梗阻 (UUO) 模型中的肾小管间质纤维化[1]。 Animal Model: ZSF1 rat model[1] Dosage: 1, 3, 10, 30 mg/kg; 3 mg/kg (enalapril) Administration: Oral administration; daily Result: Reduced proteinuria and incidence of glomerular sclerosis in a dose-dependent manner. Animal Model: rat UUO model[1] Dosage: 30 mg/kg Administration: v Result: Reduced tubulointerstitial fibrosis in rat UUO model.

[References]

[1]. Reinhart GA, et, al. The Novel, Clinical-Stage Soluble Guanylate Cyclase Activator BI 685509 Protects from Disease Progression in Models of Renal Injury and Disease. J Pharmacol Exp Ther. 2023 Mar;384(3):382-392.  

Chemical & Physical Properties

[ Molecular Formula ]:
C34H38N4O5

[ Molecular Weight ]:
582.69


Related Compounds