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Submit ReviewGSK 1702934A
说明： Potent and selective TRPC3/6 activator
化学名： 1,3-Dihydro-1-[1-[(5,6,7,8-tetrahydro-4H-cyclohepta[b]thien-2-yl)carbonyl]-4-piperidinyl]-2H-benzimidazol-2-one
纯度： ≥98% (HPLC)
生物活性 for GSK 1702934A
GSK 1702934A is a potent and selective TRPC3/6 activator (EC50 = 80 and 440 nM for TRPC3 and 6, respectively). Exhibits no activity at TRPV4, TRPA1, M1, M4, CaV1.2, hERG, NaV1.5, or CXCR5 receptors at concentrations <10 μmol/L. Induces TRPC3/6-currents in HEK293 cells transduced with recombinant human TRPC3/6. Directly activates TRPC channels through by-passing phospholipase-C signaling. Also induces calcium signals in HEK-TRPC6 cells (pEC50 = 6.6).
化合物库 for GSK 1702934A
GSK 1702934A is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for GSK 1702934A
| 分子量 | 395.52 |
| 公式 | C22H25N3O2S |
| 储存 | Store at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 924377-85-5 |
| PubChem ID | 16376051 |
| InChI Key | AXWRAIIIBRLXBP-UHFFFAOYSA-N |
| Smiles | O=C(C1=CC2=C(S1)CCCCC2)N3CCC(N4C(NC5=CC=CC=C45)=O)CC3 |
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.
溶解性数据 for GSK 1702934A
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 39.55 | 100 | |
| ethanol | 39.55 | 100 |
制备储备液 for GSK 1702934A
以下数据基于产品分子量 395.52。 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 | 2.53 mL | 12.64 mL | 25.28 mL |
| 5 mM | 0.51 mL | 2.53 mL | 5.06 mL |
| 10 mM | 0.25 mL | 1.26 mL | 2.53 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.51 mL |
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产品说明书 for GSK 1702934A
参考文献 for GSK 1702934A
参考文献是支持产品生物活性的出版物。
Doleschal et al (2015) TRPC3 contributes to regulation of cardiac contractility and arrhythmogenesis by dynamic interaction with NCX1. Cardiovasc.Res. 106 163 PMID: 25631581
Guedes de la Cruz et al (2017) Intensified microwave-assisted N-acylation procedure - Synthesis and activity evaluation of TRPC3 channel agonists with a 1,3-dihydro-2H-benzo[d]imidazol-2-one core. Synlett. 28 695 PMID: 28413263
Wajdner et al (2017) Orai and TRPC channel characterization in FceRI-mediated calcium signaling and mediator secretion in human mast cells. Physiol.Rep. 5 e13166 PMID: 28292887
If you know of a relevant reference for GSK 1702934A, please let us know.
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关键词: GSK 1702934A, GSK 1702934A supplier, GSK1702934A, potent, selective, TRPC3, TRPC6, activators, activates, agonists, agonism, TRPC, 6508, Tocris Bioscience
1 篇 GSK 1702934A 的引用文献
引用文献是使用了 Tocris 产品的出版物。 GSK 1702934A 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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GSK 1702934A 的评论
平均评分: 4 (Based on 1 Review.)
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Activates TRPC channels.
By
Sinayat Mahzabeen on 01/29/2021
分析类型： In Vitro
种属： Human
细胞系/组织： HEK 293, Jurkat T cells
I used this product to actvate TRPC channels in HEK293 and Jurkat T cells.