R-130823

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 510246

CAS#: 321344-32-5

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.


Price and Availability

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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 sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 510246
Name: R-130823
CAS#: 321344-32-5
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


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

SMILES Code: FC1=CC=C(C2=C(C3=CC=NC=C3)C(C4=CCN(CCC5=CC=CC=C5)CC4)=CN2)C=C1


Technical Data

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).

Harmonized System Code:
293490


Additional Information

  
  
 
 


References

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.