CP-863187
- CAS No.
- 668981-02-0
- Chemical Name:
- CP-863187
- Synonyms
- CP-281384;CP-863187;CP 281384,CP281384;CP-863187 >=98% (HPLC);1,2,4-Triazolo[4,3-a]pyridine, 6-[4-(2,5-difluorophenyl)-5-oxazolyl]-3-(1-methylethyl)-
- CBNumber:
- CB97245735
- Molecular Formula:
- C18H14F2N4O
- Molecular Weight:
- 340.33
- MDL Number:
- MFCD30480740
- MOL File:
- 668981-02-0.mol
| Density | 1.39±0.1 g/cm3(Predicted) |
|---|---|
| storage temp. | room temp |
| solubility | DMSO: 10mg/mL, clear |
| pka | 2.42±0.50(Predicted) |
| form | powder |
| color | white to beige |
| FDA UNII | FG7DYB4F07 |
| UNSPSC Code | 12352200 |
| NACRES | NA.77 |
CP-863187 Chemical Properties,Uses,Production
Uses
p38α inhibitor 7 (compound 1) is an effective p38α inhibitor with oral efficacy and generally favorable pharmacokinetic properties[1].
Biological Activity
CP-863187 is a potent p38α (p38α) inhibitor (IC50 = 5.8 nM) with 44-fold selectivity over p38β (p38β) and no inhibitory potency against p38γ (p38γ) and p38δ (p38δ) isoforms. CP-863187 effectively inhibits LPS-stimulated cellular TNF-α production in vitro (IC50 = 259 and 25 nM, using human whole blood and isolated mononuclear cells, respectively) and in rats in vivo (ED50 = 0.3 mg/kg p.o.) with good pharmacokinetic profile and oral availability (F = 87%/dog, 40%/monkey, 30%/r at with 5 mg/kg oral dosage; F = 66%/r at with 50 mg/kg oral dosage).
IC 50
p38α
References
[1] Amit S. Kalgutkar, et al. Preclinical Pharmacokinetics and Metabolism of 6-(4-(2,5- Difluorophenyl)oxazol-5-yl)-3-isopropyl-[1,2,4]-triazolo[4,3-a] pyridine, a Novel and Selective p38a Inhibitor: Identification of an Active Metabolite in Preclinical Species and Human Liver Microsomes. Biopharm. Drug Dispos. 27: 371–386 (2006).
CP-863187 Preparation Products And Raw materials
Raw materials
Preparation Products
CP-863187 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +17819995354 | marketing@targetmol.com | United States | 32285 | 58 |
| TargetMol Chemicals Inc. | +17819995354 | marketing@targetmol.com | United States | 19904 | 58 |
| Energy Chemical | 021-58432009 400-005-6266 | marketing@energy-chemical.com | China | 44918 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 21356 | 58 |
| Merck KGaA | 21-20338288 | ordercn@merckgroup.com | China | 6394 | 58 |
| Biosynth Biological Technology (Suzhou) Co Ltd | 51288865780 | sales@biosynth.com | China | 6051 | 58 |
| Supplier | Advantage |
|---|---|
| TargetMol Chemicals Inc. | 58 |
| TargetMol Chemicals Inc. | 58 |
| Energy Chemical | 58 |
| TargetMol Chemicals Inc. | 58 |
| Merck KGaA | 58 |
| Biosynth Biological Technology (Suzhou) Co Ltd | 58 |
