WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 510246
Description: R-130823 is a ighly selective inhibition against mitogen-activated protein kinase p38alpha (IC50=22 nM). The release of tumor necrosis factor-alpha, interleukin-1beta, -6 and -8 was inhibited in lipopolysaccharide-stimulated human blood pretreated by R-130823 , with IC50 values of 0.089, 0.066, 0.95 and 0.16 microM, respectively. R-130823 reduced the established hind paw swelling in rat adjuvant-induced arthritis, while methotrexate showed no suppression. In the same model, R-130823 ameliorated adjuvant-induced hyperalgesia with rapid onset and long duration comparable to a cyclooxygenase-2 inhibitor, celecoxib.
MedKoo Cat#: 510246
Chemical Formula: C28H26FN3
Exact Mass: 423.21108
Molecular Weight: 423.52
Elemental Analysis: C, 79.40; H, 6.19; F, 4.49; N, 9.92
R130823 is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to email@example.com to inquire quote.
Synonym: R130823; R-130823; R 130823.
IUPAC/Chemical Name: 4-(2-(4-fluorophenyl)-4-(1-phenethyl-1,2,3,6-tetrahydropyridin-4-yl)-1H-pyrrol-3-yl)pyridine
InChi Key: XLEONXLSQBBRAN-UHFFFAOYSA-N
InChi Code: InChI=1S/C28H26FN3/c29-25-8-6-24(7-9-25)28-27(23-10-15-30-16-11-23)26(20-31-28)22-13-18-32(19-14-22)17-12-21-4-2-1-3-5-21/h1-11,13,15-16,20,31H,12,14,17-19H2
SMILES Code: FC1=CC=C(C2=C(C3=CC=NC=C3)C(C4=CCN(CCC5=CC=CC=C5)CC4)=CN2)C=C1
The following data is based on the product molecular weight 423.52 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Wada Y, Shimada K, Sugimoto K, Kimura T, Ushiyama S. 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 Feb;6(2):144-55. Epub 2005 Aug 24. PubMed PMID: 16399619.
2: Wada Y, Shimada K, Kimura T, Ushiyama S. Novel p38 MAP kinase inhibitor R-130823 suppresses IL-6, IL-8 and MMP-13 production in spheroid culture of human synovial sarcoma cell line SW 982. Immunol Lett. 2005 Oct 15;101(1):50-9. PubMed PMID: 15888346.
3: Wada Y, Nakajima-Yamada T, Yamada K, Tsuchida J, Yasumoto T, Shimozato T, Aoki K, Kimura T, Ushiyama S. R-130823, a novel inhibitor of p38 MAPK, ameliorates hyperalgesia and swelling in arthritis models. Eur J Pharmacol. 2005 Jan 4;506(3):285-95. Epub 2004 Dec 16. PubMed PMID: 15627439.