CAS 585543-15-3|Losmapimod

Introduction:Basic information about CAS 585543-15-3|Losmapimod, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameLosmapimod
CAS Number585543-15-3Molecular Weight383.459
Density1.2±0.1 g/cm3Boiling Point529.4±50.0 °C at 760 mmHg
Molecular FormulaC22H26FN3O2Melting Point/
MSDS/Flash Point274.0±30.1 °C

Names

Name6-[5-(cyclopropylcarbamoyl)-3-fluoro-2-methylphenyl]-N-(2,2-dimethylpropyl)pyridine-3-carboxamide
SynonymMore Synonyms

Losmapimod BiologicalActivity

DescriptionLosmapimod is a selective, potent, and orally active p38 MAPK inhibitor with pKis of 8.1 and 7.6 for p38α and p38β, respectively.
Related CatalogSignaling Pathways >>Autophagy >>AutophagySignaling Pathways >>MAPK/ERK Pathway >>p38 MAPKResearch Areas >>Inflammation/Immunology
Target

pKi: 8.1 (p38α), 7.6 (p38β)

In VivoIn 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].
Animal AdminMale 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 + rofecoxib (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 with isoflurane 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.
References

[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.

[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.

Chemical & Physical Properties

Density1.2±0.1 g/cm3
Boiling Point529.4±50.0 °C at 760 mmHg
Molecular FormulaC22H26FN3O2
Molecular Weight383.459
Flash Point274.0±30.1 °C
Exact Mass383.200897
PSA78.07000
LogP3.30
Vapour Pressure0.0±1.4 mmHg at 25°C
Index of Refraction1.582
InChIKeyKKYABQBFGDZVNQ-UHFFFAOYSA-N
SMILESCc1c(F)cc(C(=O)NC2CC2)cc1-c1ccc(C(=O)NCC(C)(C)C)cn1
Storage condition-20℃

Synonyms

UNII-F2DQF16BXE
6-[5-(Cyclopropylcarbamoyl)-3-fluoro-2-methylphenyl]-N-(2,2-dimethylpropyl)nicotinamide
Losmapimod
3-Pyridinecarboxamide, 6-[5-[(cyclopropylamino)carbonyl]-3-fluoro-2-methylphenyl]-N-(2,2-dimethylpropyl)-
CAS 444606-18-2|SB-681323
CAS 1196450-97-1|3,6-Diamino-4-phenyl-1H-indazole-5-carbonitrile
Recommended......
TOP