HC-070 (C09-1138-242)

HC-070 is an antagonist of TRPC4/TRPC5 , with IC 50 s of 9.3 nM and 46 nM for hTRPC5 and hTRPC4 in cells, respectively.In VitroHC-070 is an antagonist of TRPC4/TRPC5, with IC 50 s of 9.3 nM and 46 nM for hTRPC5 and hTRPC4, respectively. HC-070 weakly inhibits TRPC3 (IC 50 , 1 μM), and is at least 400-fold selective for human TRPC4 and TRPC5-containing channels versus the other channels examined. HC-070 inhibits lanthanum-activated hTRPC5-, mTRPC5-, rTRPC5-mediated currents with IC 50 s of 0.52 nM, 0.55 nM, and 0.32 nM in whole-cell manual patch clamp. Furthermore, HC-070 blocks M2R-activated human TRPC1/TRPC4 channels with an IC 50 of 1.3 nM and La 3+ - and M1R-activated human TRPC1/5 channels with IC 50 s of 1.4 nM and 4.4 nM. HC-070 inhibits human TRPC5 currents activated via muscarinic type 1 (M1R) with an IC 50 of 2.0 nM. HC-070 also suppresses hTRPC4 currents via M2R with an IC 50 of 0.49 nM. HC-070 (20 nM) reduces CCK-4 evoked neuronal activity in the amygdala slices. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoHC-070 (1 mg/kg, p.o.) affects mice with increased evoked anxiety (CCK-4), but shows no effects in the absence of CCK-4. HC-070 (0.3, 1 or 3 mg/kg, p.o.) decreases anxiety in a standard EPM (more light/high anxiety). HC-070 (1 mg/kg) reduces the increased capacity for fear memory in mice subjected to chronic social stress on days 1-15. In addition, HC-070 (1, 3, 10 mg/kg, p.o.) causes reduction in marble burying behavior. HC-070 (0.3, 1, 3, 10 mg/kg, p.o.) also reduces time of immobility in a tail suspension test but does not impact locomotor activity in mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:IC50: 9.3 nM (hTRPC5, cell assay), 46 nM (hTRPC4, cell assay). Specifications and Purity: 99%. Molecular Formula: C22H20Cl2N4O4. Molecular Weight: 475.32. PubChem CID: 85473309. Isomeric SMILES: CN1C2=C(C(=O)N(C1=O)CCCO)N(C(=N2)OC3=CC(=CC=C3)Cl)CC4=CC=C(C=C4)Cl.