585543-15-3
585543-15-3 structure
- Name: Losmapimod
- Chemical Name: 6-[5-(cyclopropylcarbamoyl)-3-fluoro-2-methylphenyl]-N-(2,2-dimethylpropyl)pyridine-3-carboxamide
- CAS Number: 585543-15-3
- Molecular Formula: C22H26FN3O2
- Molecular Weight: 383.459
- Catalog: Biochemical Inhibitor Mitogen-activated protein kinase (MAPK) P38 MAPK inhibitor
- Create Date: 2018-12-18 14:08:27
- Modify Date: 2024-01-20 14:08:07
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Losmapimod is a selective, potent, and orally active p38 MAPK inhibitor with pKis of 8.1 and 7.6 for p38α and p38β, respectively.
| Name | 6-[5-(cyclopropylcarbamoyl)-3-fluoro-2-methylphenyl]-N-(2,2-dimethylpropyl)pyridine-3-carboxamide |
|---|---|
| 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)- |
| Description | Losmapimod is a selective, potent, and orally active p38 MAPK inhibitor with pKis of 8.1 and 7.6 for p38α and p38β, respectively. |
|---|---|
| Related Catalog | |
| Target |
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]. |
| Animal Admin | 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 + 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 |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Boiling Point | 529.4±50.0 °C at 760 mmHg |
| Molecular Formula | C22H26FN3O2 |
| Molecular Weight | 383.459 |
| Flash Point | 274.0±30.1 °C |
| Exact Mass | 383.200897 |
| PSA | 78.07000 |
| LogP | 3.30 |
| Vapour Pressure | 0.0±1.4 mmHg at 25°C |
| Index of Refraction | 1.582 |
| Storage condition | -20℃ |