GSK 2833503A

Name: GSK 2833503A
Brand: Tocris Bioscience
SKU: 6497

Tocris Bioscience, part of Bio-Techne | Catalog # 6497

Citations (2)

COA / SDS

Potent and selective TRPC6 and TRPC3 antagonist

Key Product Details

Description:	Potent and selective TRPC6 and TRPC3 antagonist
Chemical Name:	[2-[(4-Chloro-2-fluorophenyl)amino]-5-methyl-4-thiazolyl][(2S,3S)-2,3-dimethyl-1-piperidinyl]methanone
Purity:	≥98% (HPLC)
Molecular Weight:	381.89

View Full Technical Details for GSK 2833503A

Technical Data
Citations

Biological Activity for GSK 2833503A

GSK 2833503A is a potent and selective TRPC6 and TRPC3 antagonist (IC₅₀ = 3-16 nM and 21-100 nM, respectively). GSK 2833503A exhibits >63-fold selectivity over other ion channels, including other TRP channels, Ca_V1.2, hERG and Na_V1.5. GSK 2833503A suppresses angiotensin II or endothelin-1-induced cardiac hypertrophy signaling in HEK293 cells in vitro and in cardiomyocytes.

Compound Libraries for GSK 2833503A

GSK 2833503A is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for GSK 2833503A

M. Wt	381.89
Formula	C₁₈H₂₁ClFN₃OS
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1366234-01-6
PubChem ID	71818575
InChi Key	ODUIXUGXPFKQLG-QWRGUYRKSA-N
Smiles	C[C@H]1CCCN(C(C2=C(SC(NC3=C(C=C(C=C3)Cl)F)=N2)C)=O)[C@H]1C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for GSK 2833503A

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	38.19	100
	ethanol	7.64	20

Preparing Stock Solutions for GSK 2833503A

The following data is based on the product molecular weight 381.89.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.62 mL	13.09 mL	26.19 mL
5 mM	0.52 mL	2.62 mL	5.24 mL
10 mM	0.26 mL	1.31 mL	2.62 mL
50 mM	0.05 mL	0.26 mL	0.52 mL

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References for GSK 2833503A

References are publications that support the biological activity of the product.

Seo Combined TRPC3 and TRPC6 blockade by selective small-molecule or genetic deletion inhibits pathological cardiac hypertrophy. Proc.Natl.Acad.Sci.U.S.A. 2014 PMID: 24453217
Washburn The discovery of potent blockers of the canonical transient receptor channels, TRPC3 and TRPC6, based on an anilino-thiazole pharmacophore. Bioorg.Med.Chem.Lett. 2013 PMID: 23886683