321344-32-5
Chemical Structure
R-130823
- CAS No.: 321344-32-5
- Formula:C28H26FN3
- Molecular Weight:423.52
IUPAC Name: 4-(2-(4-fluorophenyl)-4-(1-phenethyl-1,2,3,6-tetrahydropyridin-4-yl)-1H-pyrrol-3-yl)pyridine
InChIKey: XLEONXLSQBBRAN-UHFFFAOYSA-N
SMILES: FC1=CC=C(C=C1)C2=C(C(C3=CCN(CC3)CCC4=CC=CC=C4)=CN2)C5=CC=NC=C5
Biological Activity: R-130823 is an orally active, highly selective p38α inhibitor with an IC50 of 22 nM against p38α, an IC50 of 820 nM against p38β, and no activity against p38γ or p38δ. R-130823 downregulates downstream cartilage degradation and inflammatory mediators, and inhibits the release of MMP-13, MMP-1 and PGE2. R-130823 reduces hind paw swelling, improves hyperalgesia, and blocks arthritis progression. R-130823 is applicable to research related to osteoarthritis and rheumatoid arthritis[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
R-130823 | R-130823 is an orally active, highly selective p38α inhibitor with an IC50 of 22 nM against p38α, an IC50 of 820 nM against p38β, and no activity against p38γ or p38δ. R-130823 downregulates downstream cartilage degradation and inflammatory mediators, and inhibits the release of MMP-13, MMP-1 and PGE2. R-130823 reduces hind paw swelling, improves hyperalgesia, and blocks arthritis progression. R-130823 is applicable to research related to osteoarthritis and rheumatoid arthritis. | |||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
- [1]. Wada Y, et al. Novel p38 mitogen-activated protein kinase inhibitor R-130823 protects cartilage by down-regulating matrix metalloproteinase-1,-13 and prostaglandin E2 production in human chondrocytes. Int Immunopharmacol. 2006;6(2):144-155. [Content Brief]
- [2]. Wada Y, et al. R-130823, a novel inhibitor of p38 MAPK, ameliorates hyperalgesia and swelling in arthritis models. Eur J Pharmacol. 2005;506(3):285-295. [Content Brief]
Keywords
