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
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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
Appearance: white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
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.