For research use only. Not for therapeutic Use.
Dilmapimod（Cat No.:I005975）, also known as SB-681323 and GW-681323, is a potent inhibitor of p38 MAPK (mitogen-activated protein kinase). It has demonstrated superior inhibition of the p38 MAPK pathway compared to prednisolone and has shown efficacy in suppressing inflammation, particularly in chronic obstructive pulmonary disease (COPD). Additionally, Dilmapimod has been found to inhibit the production of TNF-alpha, a pro-inflammatory cytokine. It has also been investigated for its potential to reduce high-sensitivity C-reactive protein (hsCRP) levels in patients undergoing elective percutaneous coronary intervention (PCI).
| Catalog Number | I005975 |
| CAS Number | 444606-18-2 |
| Molecular Formula | C23H19F3N4O3 |
| Purity | ≥95% |
| Solubility | Soluble in DMSO, not in water |
| Storage | Store at -20°C |
| IUPAC Name | 8-(2,6-difluorophenyl)-2-(1,3-dihydroxypropan-2-ylamino)-4-(4-fluoro-2-methylphenyl)pyrido[2,3-d]pyrimidin-7-one |
| InChI | InChI=1S/C23H19F3N4O3/c1-12-9-13(24)5-6-15(12)20-16-7-8-19(33)30(21-17(25)3-2-4-18(21)26)22(16)29-23(28-20)27-14(10-31)11-32/h2-9,14,31-32H,10-11H2,1H3,(H,27,28,29) |
| InChIKey | ORVNHOYNEHYKJG-UHFFFAOYSA-N |
| SMILES | CC1=C(C=CC(=C1)F)C2=C3C=CC(=O)N(C3=NC(=N2)NC(CO)CO)C4=C(C=CC=C4F)F |
| Reference | </br>1:Population Pharmacokinetics and Pharmacodynamics Modelling of Dilmapimod in Severe Trauma Subjects at Risk for Acute Respiratory Distress Syndrome. Yang S, Dumitrescu TP.Drugs R D. 2017 Mar;17(1):145-158. doi: 10.1007/s40268-016-0161-9. PMID: 28004376 Free PMC Article</br>2:A Randomized Dose-Escalation Study of the Safety and Anti-Inflammatory Activity of the p38 Mitogen-Activated Protein Kinase Inhibitor Dilmapimod in Severe Trauma Subjects at Risk for Acute Respiratory Distress Syndrome. Christie JD, Vaslef S, Chang PK, May AK, Gunn SR, Yang S, Hardes K, Kahl L, Powley WM, Lipson DA, Bayliffe AI, Lazaar AL.Crit Care Med. 2015 Sep;43(9):1859-69. doi: 10.1097/CCM.0000000000001132. PMID: 26102252 </br>3:Gene expression changes caused by the p38 MAPK inhibitor dilmapimod in COPD patients: analysis of blood and sputum samples from a randomized, placebo-controlled clinical trial. Betts JC, Mayer RJ, Tal-Singer R, Warnock L, Clayton C, Bates S, Hoffman BE, Larminie C, Singh D.Pharmacol Res Perspect. 2015 Feb;3(1):e00094. doi: 10.1002/prp2.94. Epub 2014 Dec 9. PMID: 25692013 Free PMC Article</br>4:Clinical trial of the p38 MAP kinase inhibitor dilmapimod in neuropathic pain following nerve injury. Anand P, Shenoy R, Palmer JE, Baines AJ, Lai RY, Robertson J, Bird N, Ostenfeld T, Chizh BA.Eur J Pain. 2011 Nov;15(10):1040-8. doi: 10.1016/j.ejpain.2011.04.005. Epub 2011 May 14. PMID: 21576029 |
