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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-TRP Channel-AM237
AM237

Chemical Structure : AM237

CAS No.: 1628289-29-1

AM237 (AM 237, AM-237)

货号: PC-72123Not For Human Use, Lab Use Only.

AM237 is a selective TRPC5 channel activator that potently activated homomeric TRPC5:C5 channels (EC50=15–20 nM in Ca2+i assays).

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2 mg ¥1980 In stock
5 mg ¥3280 In stock
10 mg ¥5280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

AM237 is a selective TRPC5 channel activator that potently activated homomeric TRPC5:C5 channels (EC50=15–20 nM in Ca2+i assays).
AM237 did not activate TRPC4:C4, TRPC4-C1, TRPC5-C1, TRPC1:C5, and TRPC1:C4 channels, or native TRPC1:C4 channels in A498 cells, but potently inhibited EA‐dependent activation of these channels with IC50 values ranging from 0.9 to 7 nM.
AM237 (300 nM) did not activate or inhibit TRPC3, TRPC6, TRPV4, or TRPM2 channels.
AM237 potentiated TRPC5:C5 channels activation by sphingosine‐1‐phosphate but suppressed activation evoked by (−)‐englerin A (EA).
AM237 concentration‐dependently suppressed further activation of Ca2+ influx mediated by EA with IC50 of 13 nM, potentiated TRPC5:C5 activation by S1P.
Pico145 is a competitive antagonist of AM237‐mediated TRPC5:C5 activation.

物理化学性质&存储条件

分子量 559.323
分子式 C23H19Cl2F3N4O5
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

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

参考文献

1. Aisling Minard, et al. Br J Pharmacol. 2019 Oct;176(20):3924-3938.

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