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  6. GSK-AHAB; GW856553X; SB856553

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Supplier Contact

Supplier NameMedChemExpress (MCE)
Contactsales
Tel609-228-6898
Mobile609-228-6898
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Emailsales@medchemexpress.com; tech@medchemexpress.com
Websitehttps://www.medchemexpress.com/
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Product NameLosmapimod
SynonymsGSK-AHAB
GW-856553
LosMapiMod
GW 856553X
Losmapimod
LosMapiMod,GW-856553
Losmapimod (GW856553X)

Synonyms

GSK-AHAB
GW-856553
LosMapiMod
GW 856553X
Losmapimod
LosMapiMod,GW-856553
Losmapimod (GW856553X)
6-[5-(Cyclopropylcarbamoyl)-3-fluoro-2-methylphenyl]-N-(2,2-dimethylpropyl)pyridine-3-carboxamide
3-Pyridinecarboxamide, 6-[5-[(cyclopropylamino)carbonyl]-3-fluoro-2-methylphenyl]-N-(2,2-dimethylpropyl)-
CAS585543-15-3
EINECS
Chemical FormulaC22H26FN3O2
Molecular Weight383.46
inchi
Package10 mM * 1 mL;5 mg;10 mg;25 mg;50 mg;100 mg
PriceEmail to quote
DescriptionsLosmapimod

Losmapimod

MedChemExpress (MCE)

HY-10402

585543-15-3

GSK-AHAB

Descriptions

Losmapimod

Losmapimod

MedChemExpress (MCE)

HY-10402

585543-15-3

GSK-AHAB
GW856553X
SB856553

99.94%

Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Room temperature in continental US
may vary elsewhere.

Losmapimod (GSK-AHAB) is a selective, potent, and orally active p38 MAPK inhibitor with pKis of 8.1 and 7.6 for p38α and p38β, respectively.

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)[1].

Male SHR-SPs (n=70) are randomly assigned according to body weight into five groups (n=14 per group): normal diet controls (ND), high salt-fat diet controls (SFD), SFD + GSK-AHAB (1.2 mg/kg/day), and SFD + GSK-AHAB (12 mg/kg/day) and SFD + MK 966 (18 mg/kg/day). All drugs are administered in the diet by mixing with the SFD. A subgroup of animals from each group (n=6 per group) are anesthetized and surgically instrumented with radiotelemetry units for the conscious measurement of mean arterial blood pressure and heart rate. These animals are allowed to recover for at least 7 days before the start of the study.

pKi: 8.1 (p38α), 7.6 (p38β) In Vivo 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)[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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[1]. Willette RN, et al. Differential effects of p38 mitogen-activated protein kinase and cyclooxygenase 2 inhibitors in a model of cardiovascular disease. J Pharmacol Exp Ther. 2009 Sep
330(3):964-70.
[Content Brief]

[2]. Zhang XM, et al. Suppression of mitochondrial fission in experimental cerebral ischemia: The potential neuroprotective target of p38 MAPK inhibition. Neurochem Int. 2015 Nov
90:1-8.
[Content Brief]

Supplier Websitehttps://www.medchemexpress.com/Losmapimod.html
Last Update2025-05-21 16:50:25
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