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Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, specifically inhibiting ( )-englerin A-activated TRPC4/TRPC5 channels with IC50s of 0.349 and 1.3 nM in cells, while showing no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, or TRPM8.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $118 | In Stock | |
5 mg | $291 | In Stock | |
10 mg | $457 | In Stock | |
25 mg | $753 | In Stock | |
50 mg | $1,060 | In Stock | |
100 mg | $1,430 | In Stock | |
1 mL x 10 mM (in DMSO) | $332 | In Stock |
Description | Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, specifically inhibiting ( )-englerin A-activated TRPC4/TRPC5 channels with IC50s of 0.349 and 1.3 nM in cells, while showing no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, or TRPM8. |
Targets&IC50 | TRPC5-TRPC1:0.2 nM (cell assay), TRPC5:1.3 nM (cell assay), TRPC4:0.349 nM (cell assay), TRPC4-TRPC1:0.03 nM (cell assay) |
In vitro | Pico145 is a remarkable small-molecule inhibitor of TRPC1/4/5 channels. Pico145 displays no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8. Pico145 inhibits (?)-englerin A-activated TRPC4/TRPC5 channels (IC50s: 0.349 and 1.3 nM in cells). 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). Pico145 effectively inhibits RPC4-TRPC1 channels activated by sphingosine 1-phosphate (S1P) and suppresses S1P-evoked Ca2+ entry through TRPC4-TRPC1 channels (IC50: 0.011 nM). The potency of Pico145 can be reduced by increased (?)-englerin A concentration. 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[1]. |
Alias | HC-608 |
Molecular Weight | 524.88 |
Formula | C23H20ClF3N4O5 |
Cas No. | 1628287-16-0 |
Smiles | Cn1c2nc(Oc3cccc(OC(F)(F)F)c3)n(Cc3ccc(Cl)cc3)c2c(=O)n(CCCO)c1=O |
Relative Density. | 1.48 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 99 mg/mL (188.61 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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