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Chemical Structure : AM237
CAS No.: 1628289-29-1
Catalog No.: 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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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.
| M.Wt | 559.323 | |
| Formula | C23H19Cl2F3N4O5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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1. Aisling Minard, et al. Br J Pharmacol. 2019 Oct;176(20):3924-3938.
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