Methanone, (3,4-dihydro-2(1H)-isoquinolinyl)[2-[(4-methoxyphenyl)amino]-4-thiazolyl]-
Methanone, (3,4-dihydro-2(1H)-isoquinolinyl)[2-[(4-methoxyphenyl)amino]-4-thiazolyl]- Basic information
- Product Name:
- Methanone, (3,4-dihydro-2(1H)-isoquinolinyl)[2-[(4-methoxyphenyl)amino]-4-thiazolyl]-
- Synonyms:
-
- Methanone, (3,4-dihydro-2(1H)-isoquinolinyl)[2-[(4-methoxyphenyl)amino]-4-thiazolyl]-
- GSK417651A
- TRPC3/6-IN-1
- (3,4-dihydroisoquinolin-2(1H)-yl)(2-((4-methoxyphenyl)amino)thiazol-4-yl)methanone
- (3,4-Dihydro-2(1H)-isoquinolinyl)[2-[(4-methoxyphenyl)amino]-4-thiazolyl]methanone
- CAS:
- 736945-96-3
- MF:
- C20H19N3O2S
- MW:
- 365.45
- Mol File:
- 736945-96-3.mol
Methanone, (3,4-dihydro-2(1H)-isoquinolinyl)[2-[(4-methoxyphenyl)amino]-4-thiazolyl]- Chemical Properties
- 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).
- pka
- 2.24±0.10(Predicted)
- form
- solid
- 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.
Methanone, (3,4-dihydro-2(1H)-isoquinolinyl)[2-[(4-methoxyphenyl)amino]-4-thiazolyl]- Usage And Synthesis
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] XIAOPING XU. Characterization of Small Molecule TRPC3 and TRPC6 agonist and Antagonists[J]. Biophysical journal, 2013, 24 1. DOI:10.1016/j.bpj.2012.11.2513
[2] KINYA SEO. Combined TRPC3 and TRPC6 blockade by selective small-molecule or genetic deletion inhibits pathological cardiac hypertrophy.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2014, 111 4: 1551-1556. DOI:10.1073/pnas.1308963111
Methanone, (3,4-dihydro-2(1H)-isoquinolinyl)[2-[(4-methoxyphenyl)amino]-4-thiazolyl]-Supplier
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