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- 详细信息
- 文献和实验
- 技术资料
- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名:
Pico145; HC-608
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
1628287-16-0
- 规格:
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg/50 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥1151.0 |
|---|---|---|---|
| 规格: | 1 mg | 产品价格: | ¥490.0 |
| 规格: | 5 mg | 产品价格: | ¥997.0 |
| 规格: | 10 mg | 产品价格: | ¥1410.0 |
| 规格: | 25 mg | 产品价格: | ¥2545.0 |
| 规格: | 50 mg | 产品价格: | ¥4200.0 |
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Pico145
CAS No. : 1628287-16-0
MCE 国际站:Pico145
产品活性:Pico145 (HC-608) 是一种高效的瞬时受体电位通道蛋白 1/4/5 (TRPC1/TRPC4/TRPC5) 抑制剂,在细胞中,能够抑制 (−)-englerin A 活化的 TRPC4/TRPC5 通道,IC50 值分别为 0.349 和 1.3 nM,对 TRPC3,TRPC6,TRPV1,TRPV4,TRPA1,TRPM2 和 TRPM8 无作用。
研究领域:Membrane Transporter/Ion Channel | Neuronal Signaling
作用靶点:TRP Channel
In Vitro: Pico145 (Compound 31, C31) is a remarkable small-molecule inhibitor of TRPC1/4/5 channels, inhibits (−)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells; Pico145 shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8. Pico145 also inhibits human TRPC4-TRPC1 and TRPC5-TRPC1 concatemers expressed in HEK 293 Tet+ cells (IC50, 0.03 nM and 0.2 nM, respectively). The potency of Pico145 can be reduced by increased (−)-englerin A concentration. Furthermore, Pico145 potently inhibits RPC4-TRPC1 channels activated by sphingosine 1-phosphate (S1P), and suppresses S1P-evoked Ca2+ entry through TRPC4-TRPC1 channels with an IC50 of 0.011 nM. Pico145 also sensitizes EA-sensitive cancer cell line (Hs578T cells) (IC50, 0.11 nM). Pico145 (100 nM) lacks effect on store-operated Ca2+ entry and histamine-evoked Ca2+ entry into endothelial cells.
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