Aficamten(CK274)

Cas No.:	2364554-48-1
Chemical Name:	Aficamten
Synonyms:	Aficamten;Aficamten [INN];Aficamten [USAN];B1I77MH6K1;GTPL11524;WHO 11544;CK3773274;1H-Pyrazole-4-carboxamide, N-((1R)-5-(5-ethyl-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-inden-1-yl)-1-methyl-;N-((1R)-5-(5-Ethyl-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-inden-1-yl)- 1-methyl-1H-pyrazole-4-carboxamide;N-[(1R)-5-(5-ethyl-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-inden-1-yl]-1-methylpyrazole-4-carboxamide;BDBM50575173;N-[(1R)-5-(5-ethyl-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-inden-1-yl]-1-methylpyrazole-4-
SMILES:	O=C(C1C=NN(C)C=1)N[C@H]1C2C=CC(C3=NOC(CC)=N3)=CC=2CC1
Formula:	C18H19N5O2
M.Wt:	337.375763177872
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	[1]. Chihyuan Chuang, et al. Discovery of Aficamten (CK-274), a Next-Generation Cardiac Myosin Inhibitor for the Treatment of Hypertrophic Cardiomyopathy. J Med Chem. 2021 Oct 14;64(19):14142-14152.

Description:	Aficamten (CK-274) is a novel cardiac myosin inhibitor with an IC50 of 1.4 μM. Aficamten can be used for the research of hypertrophic cardiomyopathy (HCM)[1].
Target:	Research Areas >> Cardiovascular Disease Signaling Pathways >> Cytoskeleton >> Myosin
In Vivo:	Aficamten is a next-generation cardiac myosin inhibitor that provides a projected human half-life appropriate for once a day dosing, reaching steady state within two weeks, and demonstrates a wide therapeutic window in vivo with a clear PK/PD relationship[1]. Aficamten exhibits moderate oral bioavailability (mouse 98%, rat 55%, rat 58%,rat 79%, dog 45%, monkey 41%) following oral administration (mouse 1 mg/kg, rat 2 mg/kg, rat 3 mg/kg, rat 8 mg/kg, dog 1 mg/kg and monkey 1 mg/kg)[1]. Aficamten exhibits terminal elimination half-lives (mouse 4.5 h, rat 3.0 h, dog 33.8 h and, monkey 8.1 h) following intravenous administration (mouse 0.5 mg/kg, rat 1 mg/kg, dog 1 mg/kg and monkey 1.0 mg/kg)[1].
References:	[1]. Chihyuan Chuang, et al. Discovery of Aficamten (CK-274), a Next-Generation Cardiac Myosin Inhibitor for the Treatment of Hypertrophic Cardiomyopathy. J Med Chem. 2021 Oct 14;64(19):14142-14152.