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Methanone, (3,4-dihydro-2(1H)-isoquinolinyl)[2-[(4-methoxyphenyl)amino]-4-thiazolyl]-

Product Name
Methanone, (3,4-dihydro-2(1H)-isoquinolinyl)[2-[(4-methoxyphenyl)amino]-4-thiazolyl]-
CAS No.
736945-96-3
Chemical Name
Methanone, (3,4-dihydro-2(1H)-isoquinolinyl)[2-[(4-methoxyphenyl)amino]-4-thiazolyl]-
Synonyms
GSK417651A;TRPC3/6-IN-1;(3,4-Dihydro-2(1H)-isoquinolinyl)[2-[(4-methoxyphenyl)amino]-4-thiazolyl]methanone;(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]-
CBNumber
CB58346718
Molecular Formula
C20H19N3O2S
Formula Weight
365.45
MOL File
736945-96-3.mol
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Methanone, (3,4-dihydro-2(1H)-isoquinolinyl)[2-[(4-methoxyphenyl)amino]-4-thiazolyl]- Property

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.
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Hazard and Precautionary Statements (GHS)

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Methanone, (3,4-dihydro-2(1H)-isoquinolinyl)[2-[(4-methoxyphenyl)amino]-4-thiazolyl]- Chemical Properties,Usage,Production

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].

CompdDose(iv)(mg/kg)Cmax(iv)(ng/ml)CL(iv)(ml/min/kg)MRT(iv)(h)DNAUC(iv)(h?kg/L)%F
30.932501200.30.14~1

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]- Preparation Products And Raw materials

Raw materials

Preparation Products

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Methanone, (3,4-dihydro-2(1H)-isoquinolinyl)[2-[(4-methoxyphenyl)amino]-4-thiazolyl]- Suppliers

China 5 United States 2 Global 7
Shanghai Yifei Biotechnology Co. , Ltd.
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021-65675885 18964387627
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customer_service@efebio.com
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China
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11973
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TargetMol Chemicals Inc.
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15002134094
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marketing@targetmol.cn
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China
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29423
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Cayman Chemical Company
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800-364-9897
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sales@caymanchem.com
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China
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6838
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Biosynth Biological Technology (Suzhou) Co Ltd
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51288865780
Email
sales@biosynth.com
Country
China
ProdList
6051
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736945-96-3, Methanone, (3,4-dihydro-2(1H)-isoquinolinyl)[2-[(4-methoxyphenyl)amino]-4-thiazolyl]-Related Search:

4'-CHLORO-3-METHOXYCINNAMANILIDE POLYGODIAL SKF 96365 HYDROCHLORIDE Nitrendipine

  • 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
  • 736945-96-3