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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-TRP Channel-Pico145
Pico145

Chemical Structure : Pico145

CAS No.: 1628287-16-0

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Pico145 (Pico-145, HC-608)

货号: PC-60846Not For Human Use, Lab Use Only.

Pico145 is a highly potent, subtype-selective TRPC1/4/5 channels inhibitor with potency ranged from 9 to 1300 pM, depending on the TRPC1/4/5 subtype and activation mechanism.

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25 mg ￥4580 In stock
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纯度 & COA & 质检文件 纯度: 99.5% (LCMS) Select Batch:

生物&药学活性

Pico145 (HC-608) is a highly potent, subtype-selective TRPC1/4/5 channels inhibitor with potency ranged from 9 to 1300 pM, depending on the TRPC1/4/5 subtype and activation mechanism.
Pico145 shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8, and store-operated Ca2+ entry mediated by Orai1.
Pico145 prevents Ca2+ entry through TRPC5-TRPC1 and TRPC4-TRPC1 with IC50 of 0.199 and 0.033 nM, respectively.
Pico145 inhibits S1P-activated TRPC4 channels at −100 and +100 mV with IC50 of 0.012 and 0.03 nM, respectively.
Pico145 strongly inhibits Icat and EA-induced cytotoxicity in synovial sarcoma cells.

物理化学性质&存储条件

分子量 524.881
分子式 C23H20ClF3N4O5
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

7-(4-chlorobenzyl)-1-(3-hydroxypropyl)-3-methyl-8-(3-(trifluoromethoxy)phenoxy)-3,7-dihydro-1H-purine-2,6-dione

参考文献

1. Rubaiy HN, et al. J Biol Chem. 2017 May 19;292(20):8158-8173.

2. Rubaiy HN, et al. Channels (Austin). 2017 Sep 3;11(5):362-364.

3. Muraki K, et al. Sci Rep. 2017 Dec 5;7(1):16988.

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