| Identification | Back Directory | [Name]
Methanone, (3,4-dihydro-2(1H)-isoquinolinyl)[2-[(4-methoxyphenyl)amino]-4-thiazolyl]- | [CAS]
736945-96-3 | [Synonyms]
GSK417651A
TRPC3/6-IN-1
(3,4-dihydroisoquinolin-2(1H)-yl)(2-((4-methoxyphenyl)amino)thiazol-4-yl)methanone
Methanone, (3,4-dihydro-2(1H)-isoquinolinyl)[2-[(4-methoxyphenyl)amino]-4-thiazolyl]- | [Molecular Formula]
C20H19N3O2S | [MOL File]
736945-96-3.mol | [Molecular Weight]
365.45 |
| Chemical Properties | Back Directory | [Boiling point ]
579.8±60.0 °C(Predicted) | [density ]
1.318±0.06 g/cm3(Predicted) | [storage temp. ]
RT (des.) | [solubility ]
Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 15 mg/ml with warming). | [form ]
solid | [pka]
2.24±0.10(Predicted) | [color ]
Yellow | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months. |
| Hazard Information | Back Directory | [Description]
GSK417651A (736945-96-3) is a TRPC blocker. In whole-cell patch-clamp experiments in HEK293 cells transfected with recombinant human TRPC3 or TRPC6, GSK417651A blocked both TRPC3 and TRPC6 current with IC50 of ~0.04 μM.1?Combined pharmacological blockade of TRPC3 and TRPC6 inhibits cardiac hypertrophy.2 Cell permeable | [Uses]
GSK417651A is an inhibitor of transient receptor channels 3 & 6. | [in vivo]
TRPC3/6-IN-1 (compound 3) has good pharmacokinetic in rats[1].
Pharmacokinetic Parameters of TRPC3/6-IN-1 in rats [1].
| Compd | Dose(iv)(mg/kg) | Cmax(iv)(ng/ml) | CL(iv)(ml/min/kg) | MRT(iv)(h) | DNAUC(iv)(h?kg/L) | %F | | 3 | 0.93 | 250 | 120 | 0.3 | 0.14 | ~1 |
| [IC 50]
hTRPC3: 1260 nM (IC50); hTRPC6: 500 nM (IC50) | [References]
1) Xu et al. (2013), Characterization of small molecule TRPC3 and TRPC6 agonists and antagonists; Biophys. J., 104 Supp 1 454a
2) Seo et al. (2014) Combined TRPC3 and TRPC6 blockade by selective small-molecule or genetic deletion inhibits pathological cardiac hypertrophy; Proc. Natl. Acad. Sci. USA, 111 1551 |
|
|