RPR-200765A Mesylayte

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MedKoo CAT#: 510245

CAS#: 218162-38-0 (RPR-200765 mesylate salt); 218158-45-3 (RPR-200765, free base).

Description: RPR-200765A is a potent and selective inhibitor of p38 MAP kinase (IC50 = 50 nM). It inhibits LPS-stimulated TNFalpha release both in vitro, from human monocytes (EC50 = 110 nM), and in vivo in Balb/c mice (ED50 = 6 mg/kg). At oral doses between 10 and 30 mg/kg/day it reduces the incidence and progression in the rat streptococcal cell wall (SCW) arthritis model when administered in either prophylactic or therapeutic dosing regimens. The compound, which is a mesylate salt and exists as a stable monohydrate, shows good oral bioavailabiltiy (F = 50% in the rat) and excellent chemical stability. The data from the SCW disease model suggests that RPR200765A could exhibit a profile of disease modifying activity in rheumatoid arthritis (RA) patients which is not observed with current drug therapies.

Chemical Structure

RPR-200765A Mesylayte
CAS# 218162-38-0 (RPR-200765 mesylate salt); 218158-45-3 (RPR-200765, free base).

Theoretical Analysis

MedKoo Cat#: 510245
Name: RPR-200765A Mesylayte
CAS#: 218162-38-0 (RPR-200765 mesylate salt); 218158-45-3 (RPR-200765, free base).
Chemical Formula: C24H25FN4O4
Exact Mass: 452.18598
Molecular Weight: 452.48
Elemental Analysis: C, 63.71; H, 5.57; F, 4.20; N, 12.38; O, 14.14

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Synonym: RPR200765; RPR-200765; RPR 200765; RPR200765A.

IUPAC/Chemical Name: ((2r,5r)-2-(4-(4-fluorophenyl)-5-(pyridin-4-yl)-1H-imidazol-2-yl)-5-methyl-1,3-dioxan-5-yl)(morpholino)methanone methanesulfonate


InChi Code: InChI=1S/C24H25FN4O4.CH4O3S/c1-24(23(30)29-10-12-31-13-11-29)14-32-22(33-15-24)21-27-19(16-2-4-18(25)5-3-16)20(28-21)17-6-8-26-9-7-17;1-5(2,3)4/h2-9,22H,10-15H2,1H3,(H,27,28);1H3,(H,2,3,4)/t22-,24-;

SMILES Code: O=C([C@]1(C)CO[C@@H](C2=NC(C3=CC=C(F)C=C3)=C(C4=CC=NC=C4)N2)OC1)N5CCOCC5.OS(=O)(C)=O

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

Preparing Stock Solutions

The following data is based on the product molecular weight 452.48 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

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1: Foster ML, Halley F, Souness JE. Potential of p38 inhibitors in the treatment of rheumatoid arthritis. Drug News Perspect. 2000 Oct;13(8):488-97. PubMed PMID: 12937622.

2: Mclay LM, Halley F, Souness JE, McKenna J, Benning V, Birrell M, Burton B, Belvisi M, Collis A, Constan A, Foster M, Hele D, Jayyosi Z, Kelley M, Maslen C, Miller G, Ouldelhkim MC, Page K, Phipps S, Pollock K, Porter B, Ratcliffe AJ, Redford EJ, Webber S, Slater B, Thybaud V, Wilsher N. The discovery of RPR 200765A, a p38 MAP kinase inhibitor displaying a good oral anti-arthritic efficacy. Bioorg Med Chem. 2001 Feb;9(2):537-54. PubMed PMID: 11249145.

Additional Information