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Submit ReviewGSK 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, CaV1.2, hERG and NaV1.5. GSK 2833503A suppresses angiotensin II or endothelin-1-induced cardiac hypertrophy signaling in HEK293 cells in vitro and in cardiomyocytes.
GSK 2833503A is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 381.89 |
公式 | C18H21ClFN3OS |
储存 | Store at -20°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 38.19 | 100 | |
ethanol | 7.64 | 20 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
Washburn et al (2013) The discovery of potent blockers of the canonical transient receptor channels, TRPC3 and TRPC6, based on an anilino-thiazole pharmacophore. Bioorg.Med.Chem.Lett. 23 4979 PMID: 23886683
Seo et al (2014) Combined TRPC3 and TRPC6 blockade by selective small-molecule or genetic deletion inhibits pathological cardiac hypertrophy. Proc.Natl.Acad.Sci.U.S.A. 111 1551 PMID: 24453217
If you know of a relevant reference for GSK 2833503A, please let us know.
关键词: GSK 2833503A, GSK 2833503A supplier, GSK2833503A, GSK503A, TRPC3, TRPC6, transient, receptor, potential, canonical, channel, anatagonists, potent, selective, TRPC, 6497, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 GSK 2833503A 的部分引用包括:
Jonathan H et al (2022) Genetic- and diet-induced ω-3 fatty acid enrichment enhances TRPV4-mediated vasodilation in mice. Cell Rep 40 111306 PMID: 36070688
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