For research use only. Not for therapeutic Use.
Doramapimod (also known as BIRB 796)（Cat No.:I002974）is a potent, selective inhibitor of p38 MAPK (mitogen-activated protein kinase), targeting all four isoforms (α, β, γ, and δ) with high affinity. By inhibiting p38 MAPK, Doramapimod effectively reduces the production of pro-inflammatory cytokines, such as TNF-α and IL-1β, which play a significant role in inflammatory and autoimmune conditions. It has been investigated for potential therapeutic applications in diseases like rheumatoid arthritis, psoriasis, and Crohn’s disease. Doramapimod is a valuable research tool for exploring the p38 MAPK pathway and its role in regulating inflammation and immune response.
| Catalog Number | I002974 |
| CAS Number | 285983-48-4 |
| Synonyms | 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]urea |
| Molecular Formula | C₃₁H₃₇N₅O₃ |
| Purity | ≥95% |
| Target | p38 |
| Solubility | DMSO ≥102 mg/mL Water <1.2 mg/mL Ethanol ≥ 102mg/mL |
| Storage | -20°C |
| IC50 | 0.1 nM (Kd) |
| IUPAC Name | 1-[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]-3-[4-(2-morpholin-4-ylethoxy)naphthalen-1-yl]urea |
| InChI | InChI=1S/C31H37N5O3/c1-22-9-11-23(12-10-22)36-29(21-28(34-36)31(2,3)4)33-30(37)32-26-13-14-27(25-8-6-5-7-24(25)26)39-20-17-35-15-18-38-19-16-35/h5-14,21H,15-20H2,1-4H3,(H2,32,33,37) |
| InChIKey | MVCOAUNKQVWQHZ-UHFFFAOYSA-N |
| SMILES | CC1=CC=C(C=C1)N2C(=CC(=N2)C(C)(C)C)NC(=O)NC3=CC=C(C4=CC=CC=C43)OCCN5CCOCC5 |
| Reference | 1:J Pharmacol Sci. 2015 Nov;129(3):135-42. doi: 10.1016/j.jphs.2015.06.008. Epub 2015 Jul 3. In vitro anti-osteoclastogenic activity of p38 inhibitor doramapimod via inhibiting migration of pre-osteoclasts and NFATc1 activity.Moon SH,Choi SW,Kim SH, PMID: 26232862 DOI: 10.1016/j.jphs.2015.06.008 </br><span>Abstract:</span> The mitogen activated protein kinase p38 plays a role in the receptor activator of NF-ĸB ligand (RANKL)-induced osteoclast differentiation. In this study, we investigated the effect of p38 inhibitor doramapimod on the osteoclast differentiation. Doramapimod significantly inhibited the osteoclastogenesis of bone marrow macrophages (BMMs) via attenuating the activation of p38 induced by M-CSF and RANKL. Importantly, doramapimod blocked the migration and fusion in pre-osteoclasts via the down-regulating NFATc1. The inhibitory effect of doramapimod on the migration/fusion of pre-osteoclasts via inhibiting NFATc1 activity were confirmed by measuring NFATc1 luciferase activity and evaluating the mRNA expression of NFATc1-responsive genes related to the osteoclastic migration/fusion. These results suggested anti-osteoclastogenic activity of doramapimod via inhibiting migration/fusion of pre-osteoclasts and NFATc1 activity. Copyright © 2015 The Authors. Production and hosting by Elsevier B.V. All rights reserved. |
