WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H510245
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.
Hodoodo Cat#: H510245
Name: RPR-200765A Mesylayte
CAS#: 218162-38-0 (RPR-200765 mesylate salt); 218158-45-3 (RPR-200765, free base).
Chemical Formula: C24H25FN4O4
Exact Mass: 452.19
Molecular Weight: 452.480
Elemental Analysis: C, 63.71; H, 5.57; F, 4.20; N, 12.38; O, 14.14
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 Key: HYXPWOSDWIYCSH-QRIJWHNFSA-N
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
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
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.
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: |
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.