1H-Pyrazole-4-carboxamide, N-[(1R)-5-(5-ethyl-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-inden-1-yl]-1-methyl-
- Product Name
- 1H-Pyrazole-4-carboxamide, N-[(1R)-5-(5-ethyl-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-inden-1-yl]-1-methyl-
- CAS No.
- 2364554-48-1
- Chemical Name
- 1H-Pyrazole-4-carboxamide, N-[(1R)-5-(5-ethyl-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-inden-1-yl]-1-methyl-
- Synonyms
- CK-274;Afkeitai;Aficamten;CK-3773274;Aficamten(CK274);Aficamten (CK-3773274;Aficamten, 10 mM in DMSO;Aficamten (CK-274) ,E1016;(R)-N-(5-(5-Ethyl-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-inden-1-yl)-1-methyl-1H-pyrazole-4-carboxamide;1H-Pyrazole-4-carboxamide, N-[(1R)-5-(5-ethyl-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-inden-1-yl]-1-methyl-
- CBNumber
- CB18366125
- Molecular Formula
- C18H19N5O2
- Formula Weight
- 337.38
- MOL File
- 2364554-48-1.mol
1H-Pyrazole-4-carboxamide, N-[(1R)-5-(5-ethyl-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-inden-1-yl]-1-methyl- Property
- Density
- 1.40±0.1 g/cm3(Predicted)
- solubility
- DMSO : 125 mg/mL (370.50 mM; Need ultrasonic)
- form
- A crystalline solid
- pka
- 13.84±0.20(Predicted)
- color
- White to light brown
- InChI
- InChI=1S/C18H19N5O2/c1-3-16-21-17(22-25-16)12-4-6-14-11(8-12)5-7-15(14)20-18(24)13-9-19-23(2)10-13/h4,6,8-10,15H,3,5,7H2,1-2H3,(H,20,24)/t15-/m1/s1
- InChIKey
- IOVAZWDIRCRMTM-OAHLLOKOSA-N
- SMILES
- N1(C)C=C(C(N[C@H]2C3=C(C=C(C4N=C(CC)ON=4)C=C3)CC2)=O)C=N1
1H-Pyrazole-4-carboxamide, N-[(1R)-5-(5-ethyl-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-inden-1-yl]-1-methyl- Chemical Properties,Usage,Production
Uses
Aficamten can be useful in the study of myosin modulation in cardiovascular medicine.
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].
1H-Pyrazole-4-carboxamide, N-[(1R)-5-(5-ethyl-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-inden-1-yl]-1-methyl- Preparation Products And Raw materials
Raw materials
Preparation Products
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