1. Membrane Transporter/Ion Channel
  2. TRP Channel
  3. HC-070

HC-070 

Cat. No.: HY-112302 Purity: 98.23%
Handling Instructions

HC-070 is an antagonist of TRPC4/TRPC5, with IC50s of 9.3 nM and 46 nM for hTRPC5 and hTRPC4 in cells, respectively.

For research use only. We do not sell to patients.

HC-070 Chemical Structure

HC-070 Chemical Structure

CAS No. : 1628291-95-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2750 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

HC-070 is an antagonist of TRPC4/TRPC5, with IC50s of 9.3 nM and 46 nM for hTRPC5 and hTRPC4 in cells, respectively.

IC50 & Target

IC50: 9.3 nM (hTRPC5, cell assay), 46 nM (hTRPC4, cell assay)[1]

In Vitro

HC-070 is an antagonist of TRPC4/TRPC5, with IC50s of 9.3 nM and 46 nM for hTRPC5 and hTRPC4, respectively. HC-070 weakly inhibits TRPC3 (IC50, 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 IC50s 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 IC50 of 1.3 nM and La3+- and M1R-activated human TRPC1/5 channels with IC50s of 1.4 nM and 4.4 nM. HC-070 inhibits human TRPC5 currents activated via muscarinic type 1 (M1R) with an IC50 of 2.0 nM. HC-070 also suppresses hTRPC4 currents via M2R with an IC50 of 0.49 nM. HC-070 (20 nM) reduces CCK-4 evoked neuronal activity in the amygdala slices[1].

In Vivo

HC-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[1].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 62.5 mg/mL (131.49 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1038 mL 10.5192 mL 21.0385 mL
5 mM 0.4208 mL 2.1038 mL 4.2077 mL
10 mM 0.2104 mL 1.0519 mL 2.1038 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Mice[1]
The room is illuminated with fluorescent lighting on a 12-hour light/dark cycle. The light cycle is reversed, so that the dark cycle is from 6 am-6 pm daily and studies are performed when animals are more active. Groups of male C57/BL6 mice (10 weeks old) are dosed PO with 0.5% methyl cellulose or HC-070 at 0.3, 1 or 3 mg/kg (n = 10). The positive control, 1.5 mg/kg diazepam, is administered IP 30 minutes prior to testing (n = 10). Immediately following dosing, mice are returned to their home cage. At 60 minutes post vehicle or HC-070 administration, and 30 minutes post diazepam administration, mice are placed onto the elevated plus maze, one at a time, and their session recorded for 5 minutes. Videos are manually scored for number of open arm entries by a scorer blinded to treatment. All animals that fall off the maze during the test are removed from analysis[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

475.32

Formula

C₂₂H₂₀Cl₂N₄O₄

CAS No.

1628291-95-1

SMILES

O=C(N1CCCO)N(C)C2=C(N(CC3=CC=C(Cl)C=C3)C(OC4=CC=CC(Cl)=C4)=N2)C1=O

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
HC-070
Cat. No.:
HY-112302
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HC-070

Cat. No.: HY-112302