HC-070 |
Catalog No.GC30799
One-Click Copy Product Info
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HC-070은 세포에서 hTRPC5 및 hTRPC4에 대해 각각 9.3nM 및 46nM의 IC50을 갖는 TRPC4/TRPC5의 길항제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1628291-95-1
Sample solution is provided at 25 µL, 10mM.
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HC-070 is an antagonist of TRPC4/TRPC5, with IC50s of 9.3 nM and 46 nM for hTRPC5 and hTRPC4 in cells, respectively.
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].
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].
[1]. Just S, et al. Treatment with HC-070, a potent inhibitor of TRPC4 and TRPC5, leads to anxiolytic and antidepressant effects in mice. PLoS One. 2018 Jan 31;13(1):e0191225.
Animal experiment: | 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]. |
References: [1]. Just S, et al. Treatment with HC-070, a potent inhibitor of TRPC4 and TRPC5, leads to anxiolytic and antidepressant effects in mice. PLoS One. 2018 Jan 31;13(1):e0191225. | |
| Cas No. | 1628291-95-1 | SDF | |
| Canonical SMILES | O=C(N1CCCO)N(C)C2=C(N(CC3=CC=C(Cl)C=C3)C(OC4=CC=CC(Cl)=C4)=N2)C1=O | ||
| Formula | C22H20Cl2N4O4 | M.Wt | 475.32 |
| Solubility | DMSO : ≥ 62.5 mg/mL (131.49 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1038 mL | 10.5192 mL | 21.0385 mL |
| 5 mM | 420.8 μL | 2.1038 mL | 4.2077 mL |
| 10 mM | 210.4 μL | 1.0519 mL | 2.1038 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 1 reference(s) in Google Scholar.)