For research use only. Not for therapeutic Use.
Emprumapimod (PF-07265803) hydrochloride is an orally active and selective inhibitor of p38α MAPK. Emprumapimod hydrochloride can be used for the research of dilated cardiomyopathy and acute inflammatory pain[1][2].
Emprumapimod hydrochloride (ARRY-797) inhibits LPS-induced IL-6 production in RPMI-8226 cell with an IC50 value of 100 pM[1].
Emprumapimod hydrochloride (ARRY-797) (30 mg/kg; p.o.) inhibits the expression of IL-6 (91%) and TNF-α (95%) in SCID-beige mice, inhibits the phosphorylation of p38 in RPMI-8226 xenografts, inhibits the growth of RPMI-8226 tumour (72%) in multiple myeloma (MM) xenograft models[1].
Emprumapimod hydrochloride (30 mg/kg; p.o.; twice daily for 4 weeks) prevents left ventricular (LV) dilatation and deterioration of fractional shortening (FS) in LmnaH222P/H222P mice[2].
| Catalog Number | I041421 |
| Synonyms | N-[(2S)-1-amino-4-(dimethylamino)-1-oxobutan-2-yl]-5-(2,4-difluorophenoxy)-1-(2-methylpropyl)indazole-6-carboxamide;hydrochloride |
| Molecular Formula | C24H30ClF2N5O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C24H29F2N5O3.ClH/c1-14(2)13-31-20-11-17(24(33)29-19(23(27)32)7-8-30(3)4)22(9-15(20)12-28-31)34-21-6-5-16(25)10-18(21)26;/h5-6,9-12,14,19H,7-8,13H2,1-4H3,(H2,27,32)(H,29,33);1H/t19-;/m0./s1 |
| InChIKey | CMHXIHHSCZRHGF-FYZYNONXSA-N |
| SMILES | CC(C)CN1C2=CC(=C(C=C2C=N1)OC3=C(C=C(C=C3)F)F)C(=O)NC(CCN(C)C)C(=O)N.Cl |
| Reference | [1]. Wright D, et al. ARRY-797, a potent and selective inhibitor of p38 map kinase, inhibits LPS-induced IL-6 and in vivo growth of RPMI-8226 human multiple myeloma cells[J]. 2006. [2]. Antoine Muchir, et al. Abnormal p38α mitogen-activated protein kinase signaling in dilated cardiomyopathy caused by lamin A/C gene mutation. Hum Mol Genet. 2012 Oct 1;21(19):4325-33. |
