Losmapimod

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

Losmapimod (GSK-AHAB、GW856553X、SB856553) 是一种选择性、有效、口服活性的 p38 MAPK 抑制剂，p38α 和 p38β 的 pKi 分别为 8.1 和 7.6。

Losmapimod (GSK-AHAB, GW856553X, SB856553)?is a selective, potent, orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively; displays no significant activity for p38γ, p38δ (<25% inhibition at 10 uM), and COX-2; significantly and dose-dependently improves survival, endothelial-dependent and -independent vascular relaxation in rat model of cardiovascular disease.Ischemia Phase 3 Clinical(In Vitro):In the spontaneously hypertensive stroke-prone rat (SHR-SP), chronic treatment with GSK-AHAB significantly and dose-dependently improves survival, endothelial-dependent and -independent vascular relaxation, and indices of renal function, and it attenuates dyslipidemia, hypertension, cardiac remodeling, plasma renin activity (PRA), aldosterone, and interleukin-1β (IL-1β).

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In the spontaneously hypertensive stroke-prone rat (SHR-SP), chronic treatment with GSK-AHAB significantly and dose-dependently improves survival, endothelial-dependent and -independent vascular relaxation, and indices of renal function, and it attenuates dyslipidemia, hypertension, cardiac remodeling, plasma renin activity (PRA), aldosterone, and interleukin-1β (IL-1β).

GSK-AHAB | GW856553X | SB856553 | GW 856553X | SB 856553

MAPK/ERK Signaling

p38 MAPK

p38α|p38β

Cardiovascular Disease

Ischemia

585543-15-3

383.4591

C22H26FN3O2

>98% (HPLC)

DMSO: ≥ 58 mg/mL

O=C(C1=CC=C(C2=CC(C(NC3CC3)=O)=CC(F)=C2C)N=C1)NCC(C)(C)C

3-Pyridinecarboxamide, 6-[5-[(cyclopropylamino)carbonyl]-3-fluoro-2-methylphenyl]-N-(2,2-dimethylpropyl)-

(-20℃)

With Ice Pack

≥ 2 years