BAY 41-2272

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

BAY 41-2272 是一种有效的、不依赖 NO 的、口服的可溶性鸟苷酸环化酶 (sGC) 刺激剂，IC50 为 0.3 uM。

BAY 41-2272 is a potent, NO-independent, orally available soluble guanylate cyclase (sGC) stimulator with IC50 of 0.3 uM (relaxation of preconstricted aortic rings); targets the cysteine 238 and cysteine 243 region in the alpha1-subunit of sGC, sensitizes sGC to its physiological stimulator nitric oxide; potently unloads the heart, increases cardiac output, and preserves glomerular filtration rate without activation of the renin-angiotensin-aldosterone system in experimental congestive heart failure models.Heart Failure Discontinued.

——

Animal Model:Hypertensive beagle dogs Dosage:0.3 mg/kg, 1 mg/kg, 3 mg/kg Administration:Oral gavage; single dose; monitored for 12 hr Result:Decreased the mean BP (MBP) in a dose-dependent manner with a decrease of ?0.29?±?5.40?mmHg (p?=?0.7960) at the lowest dose of 0.3?mg/kg, ?5.51?±?11.45?mmHg (p?=?0.1625) after 1.0?mg/kg and ?14.05?±?1.81?mmHg (p?=?0.0042) after 3.0?mg/kg.

BAY 412272 | BAY41-2272

Metabolic Enzyme/Protease

Guanylate Cyclase

Guanylatecyclase

Inflammation/Immunology

——

256376-24-6

360.3876

C20H17FN6

>98% (HPLC)

DMSO: 17.5 mg/mL

NC1=NC(C2=NN(CC3=CC=CC=C3F)C4=NC=CC=C42)=NC=C1C5CC5

4-Pyrimidinamine, 5-cyclopropyl-2-[1-[(2-fluorophenyl)methyl]-1H-pyrazolo[3,4-b]pyridin-3-yl]-

(-20℃)

With Ice Pack

≥ 2 years