[CAS NO. 1628287-16-0] Pico145
PRODUCTS SPECIFICATIONS [1628287-16-0]
DESCRIPTION [1628287-16-0]
Overview
| MDL | MFCD31657331 |
|---|---|
| Molecular Weight | 524.88 |
| Molecular Formula | C23H20ClF3N4O5 |
| SMILES | O=C1C2=C(N=C(OC3=CC=CC(OC(F)(F)F)=C3)N2CC4=CC=C(Cl)C=C4)N(C)C(N1CCCO)=O |
4 Publications Citing Use of MCE
Summary
Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (−)-englerin A-activated TRPC4/TRPC5 channels, with IC 50 s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8 [1] .
IC50 & Target
IC50: 0.349 nM (TRPC4, cell assay), 1.3 nM (TRPC5, cell assay), 0.03 nM (TRPC4-TRPC1, cell assay), 0.2 nM (TRPC5-TRPC1, cell assay) [1]
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 IC 50 s 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 (IC 50 , 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 Ca 2+ entry through TRPC4-TRPC1 channels with an IC 50 of 0.011 nM. Pico145 also sensitizes EA-sensitive cancer cell line (Hs578T cells) (IC 50 , 0.11 nM). Pico145 (100 nM) lacks effect on store-operated Ca 2+ entry and histamine-evoked Ca 2+ entry into endothelial cells [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 100 mg/mL ( 190.52 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.9052 mL | 9.5260 mL | 19.0520 mL |
| 5 mM | 0.3810 mL | 1.9052 mL | 3.8104 mL |
| 10 mM | 0.1905 mL | 0.9526 mL | 1.9052 mL |
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Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.76 mM); Clear solution
