For research use only. Not for therapeutic Use.
Losmapimod (Cat No.:I004186), also known as GW856553X, SB856553, or GSK-AHAB, is a selective and potent inhibitor of p38 mitogen-activated protein kinase (MAPK). It is administered orally and exhibits activity against the alpha and beta isoforms of p38 MAPK. Losmapimod has been investigated for its potential therapeutic applications in various inflammatory and immune-mediated diseases. By inhibiting p38 MAPK, Losmapimod can modulate the activity of downstream inflammatory signaling pathways, making it a promising target for the development of novel anti-inflammatory drugs.
| Catalog Number | I004186 |
| CAS Number | 585543-15-3 |
| Molecular Formula | C22H26FN3O2 |
| Purity | ≥95% |
| Target | p38 |
| Solubility | DMSO: ≥ 58 mg/mL |
| Storage | Store at -20°C |
| IC50 | 8.1/7.6 (pKi, p38α/p38β) |
| IUPAC Name | 6-[5-(cyclopropylcarbamoyl)-3-fluoro-2-methylphenyl]-N-(2,2-dimethylpropyl)pyridine-3-carboxamide |
| InChI | InChI=1S/C22H26FN3O2/c1-13-17(9-15(10-18(13)23)21(28)26-16-6-7-16)19-8-5-14(11-24-19)20(27)25-12-22(2,3)4/h5,8-11,16H,6-7,12H2,1-4H3,(H,25,27)(H,26,28) |
| InChIKey | KKYABQBFGDZVNQ-UHFFFAOYSA-N |
| SMILES | CC1=C(C=C(C=C1F)C(=O)NC2CC2)C3=NC=C(C=C3)C(=O)NCC(C)(C)C |
| Reference | </br>1:Losmapimod does not reduce cardiovascular events in patients with acute myocardial infarction. Aronow WS, Kaple RK.J Thorac Dis. 2016 Sep;8(9):2328-2330. No abstract available. PMID: 27746967 Free PMC Article</br>2:Safety, tolerability, pharmacokinetics, and pharmacodynamics of losmapimod in healthy Japanese volunteers. Ino H, Takahashi N, Terao T, Igarashi H, Sarai N.Clin Pharmacol Drug Dev. 2015 Jul;4(4):262-9. doi: 10.1002/cpdd.190. Epub 2015 May 7. PMID: 27136906 </br>3:Effect of Losmapimod on Cardiovascular Outcomes in Patients Hospitalized With Acute Myocardial Infarction: A Randomized Clinical Trial. O/’Donoghue ML, Glaser R, Cavender MA, Aylward PE, Bonaca MP, Budaj A, Davies RY, Dellborg M, Fox KA, Gutierrez JA, Hamm C, Kiss RG, Kovar F, Kuder JF, Im KA, Lepore JJ, Lopez-Sendon JL, Ophuis TO, Parkhomenko A, Shannon JB, Spinar J, Tanguay JF, Ruda M, Steg PG, Theroux P, Wiviott SD, Laws I, Sabatine MS, Morrow DA; LATITUDE-TIMI 60 Investigators..JAMA. 2016 Apr 19;315(15):1591-9. doi: 10.1001/jama.2016.3609. PMID: 27043082 </br>4:Emerging treatment options to improve cardiovascular outcomes in patients with acute coronary syndrome: focus on losmapimod. Kragholm K, Newby LK, Melloni C.Drug Des Devel Ther. 2015 Aug 5;9:4279-86. doi: 10.2147/DDDT.S69546. eCollection 2015. Review. PMID: 26273189 Free PMC Article</br>5:A post-hoc subgroup analysis of data from a six month clinical trial comparing the efficacy and safety of losmapimod in moderate-severe COPD patients with ≤2% and >2% blood eosinophils. Marks-Konczalik J, Costa M, Robertson J, McKie E, Yang S, Pascoe S.Respir Med. 2015 Jul;109(7):860-9. doi: 10.1016/j.rmed.2015.05.003. Epub 2015 May 20. PMID: 26033641 </br>6:Rationale and design of the LosmApimod To Inhibit p38 MAP kinase as a TherapeUtic target and moDify outcomes after an acute coronary syndromE trial. O/’Donoghue ML, Glaser R, Aylward PE, Cavender MA, Crisp A, Fox KA, Laws I, Lopez-Sendon JL, Steg PG, Theroux P, Sabatine MS, Morrow DA.Am Heart J. 2015 May;169(5):622-630.e6. doi: 10.1016/j.ahj.2015.02.012. Epub 2015 Feb 23. PMID: 25965709 </br>7:A randomized, placebo-controlled trial of the analgesic efficacy and safety of the p38 MAP kinase inhibitor, losmapimod, in patients with neuropathic pain from lumbosacral radiculopathy. Ostenfeld T, Krishen A, Lai RY, Bullman J, Green J, Anand P, Scholz J, Kelly M.Clin J Pain. 2015 Apr;31(4):283-93. doi: 10.1097/AJP.0000000000000122. PMID: 25751578 </br>8:Utility of concentration-effect modeling and simulation in a thorough QT study of losmapimod. Barbour AM, Magee M, Shaddinger B, Arya N, Tombs L, Tao W, Patel BR, Fossler MJ, Glaser R.J Clin Pharmacol. 2015 Jun;55(6):661-70. doi: 10.1002/jcph.465. Epub 2015 Feb 13. PMID: 25612153 </br>9:Acute coronary syndromes: Promising data for losmapimod in NSTEMI. Roberts A.Nat Rev Cardiol. 2014 Aug;11(8):436. doi: 10.1038/nrcardio.2014.96. Epub 2014 Jul 1. No abstract available. PMID: 24981141 </br>10:Losmapimod, a novel p38 mitogen-activated protein kinase inhibitor, in non-ST-segment elevation myocardial infarction: a randomised phase 2 trial. Newby LK, Marber MS, Melloni C, Sarov-Blat L, Aberle LH, Aylward PE, Cai G, de Winter RJ, Hamm CW, Heitner JF, Kim R, Lerman A, Patel MR, Tanguay JF, Lepore JJ, Al-Khalidi HR, Sprecher DL, Granger CB; SOLSTICE Investigators..Lancet. 2014 Sep 27;384(9949):1187-95. doi: 10.1016/S0140-6736(14)60417-7. Epub 2014 Jun 12. Erratum in: Lancet. 2014 Sep 27;384(9949):1186. PMID: 24930728 |
