2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. HC-070

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

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HC-070

HC-070 Chemische Struktur

CAS. Nr. : 1628291-95-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 7 publication(s) in Google Scholar

HC-070 Related Antibodies

Top Publications Citing Use of Products

Alle TRP Channel Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
TRPA1 TRPC3 TRPC4 TRPC5 TRPC6 TRPC7 TRPM8 TRPM2 TRPM3 TRPM4 TRPM7 TRPML1 TRPML2 TRPML3 TRPV1 TRPV2 TRPV3 TRPV4 TRPV6

  • Biologische Aktivität

  • Protokoll

  • Reinheit & Dokumentation

  • Verweise

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Beschreibung

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].

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

HC-070 Related Antibodies
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].

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

475.32

Formel

C22H20Cl2N4O4
CAS. Nr.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : ≥ 62.5 mg/mL (131.49 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molaritätsrechner

  • Verdünnungsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.26 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.26 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation

Purity: 99.74%

SDS (393 KB)

COA (250 KB) HNMR (131 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
Verweise
Tierverwaltung
[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 hat die Genauigkeit dieser Methoden nicht unabhängig bestätigt. Sie dienen nur als Referenz.
Verweise

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1038 mL 10.5192 mL 21.0385 mL 52.5961 mL
5 mM 0.4208 mL 2.1038 mL 4.2077 mL 10.5192 mL
10 mM 0.2104 mL 1.0519 mL 2.1038 mL 5.2596 mL
15 mM 0.1403 mL 0.7013 mL 1.4026 mL 3.5064 mL
20 mM 0.1052 mL 0.5260 mL 1.0519 mL 2.6298 mL
25 mM 0.0842 mL 0.4208 mL 0.8415 mL 2.1038 mL
30 mM 0.0701 mL 0.3506 mL 0.7013 mL 1.7532 mL
40 mM 0.0526 mL 0.2630 mL 0.5260 mL 1.3149 mL
50 mM 0.0421 mL 0.2104 mL 0.4208 mL 1.0519 mL
60 mM 0.0351 mL 0.1753 mL 0.3506 mL 0.8766 mL
80 mM 0.0263 mL 0.1315 mL 0.2630 mL 0.6575 mL
100 mM 0.0210 mL 0.1052 mL 0.2104 mL 0.5260 mL
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HC-070 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HC-0701628291-95-1HC070HC 070TRP ChannelTransient receptor potential channelsInhibitorinhibitorinhibit

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