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.

Chemical Structure

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R-130823
CAS# 321344-32-5
Instruction

Theoretical Analysis

MedKoo Cat#: 510246
Name: R-130823
CAS#: 321344-32-5
Chemical Formula: C28H26FN3
Exact Mass: 423.21
Molecular Weight: 423.520
Elemental Analysis: C, 79.40; H, 6.19; F, 4.49; N, 9.92

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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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

More Info:          

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.