2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. RQ-00203078

RQ-00203078 is a highly selective, potent and orally active TRPM8 antagonist with IC50s of 5.3 nM and 8.3 nM for rat and human TRPM8 channels, respectively. RQ-00203078 shows little inhibitory action against TRPV1, TRPA1, TRPV4, or TRPM2 channels.

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

RQ-00203078 Chemical Structure

RQ-00203078 Chemical Structure

CAS No. : 1254205-52-1

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 67 In-stock
Solution
10 mM * 1 mL in DMSO USD 67 In-stock
Solid
1 mg USD 26 In-stock
5 mg USD 55 In-stock
10 mg USD 90 In-stock
50 mg USD 250 In-stock
100 mg USD 450 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

RQ-00203078 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

RQ-00203078 is a highly selective, potent and orally active TRPM8 antagonist with IC50s of 5.3 nM and 8.3 nM for rat and human TRPM8 channels, respectively. RQ-00203078 shows little inhibitory action against TRPV1, TRPA1, TRPV4, or TRPM2 channels[1][2].

IC50 & Target[1][2]

TRPM8

5.3 nM (IC50, Rat TRPM8 channels)

TRPM8

8.3 nM (IC50, Human TRPM8 channels)

TRPV4

10 μM (IC50)

In Vitro

Intracellular Ca2+ imaging reveals that menthol induced both intracellular Ca2+ release and store-operated Ca2+ entry, with RQ-00203078 inhibiting each effect. RQ-00203078 (1-10 μM) inhibits HSC3 and HSC4 oral squamous carcinoma cell migration and invasion in vitro[2].

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

RQ-00203078 Related Antibodies
In Vivo

RQ-00203078 (compound 36) demonstrates excellent in vivo activity in a dose dependent manner with an ED50 value of 0.65 mg/kg in the Icilin-induced wet-dog shakes model in rats after oral administration[1].
Excellent oral exposure of RQ-00203078 (compound 36) is confirmed independently in rat pharmacokinetics studies at 3 mg/kg (p.o.) administration, with a Cmax value of 2300 ng/mL and 86% bioavailability[1].

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

554.85

Formula

C21H13ClF6N2O5S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)C1=CC=C(S(=O)(N(C2=NC=C(C(F)(F)F)C=C2Cl)CC3=CC=C(OC(F)(F)F)C=C3)=O)C=C1
Shipping

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

DMSO : 100 mg/mL (180.23 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8023 mL 9.0114 mL 18.0229 mL
5 mM 0.3605 mL 1.8023 mL 3.6046 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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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 (4.51 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 (4.51 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.
Purity & Documentation

Purity: 99.84%

COA (250 KB) LCMS (110 KB)

Handling Instructions (2659 KB)
References

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 1.8023 mL 9.0114 mL 18.0229 mL 45.0572 mL
5 mM 0.3605 mL 1.8023 mL 3.6046 mL 9.0114 mL
10 mM 0.1802 mL 0.9011 mL 1.8023 mL 4.5057 mL
15 mM 0.1202 mL 0.6008 mL 1.2015 mL 3.0038 mL
20 mM 0.0901 mL 0.4506 mL 0.9011 mL 2.2529 mL
25 mM 0.0721 mL 0.3605 mL 0.7209 mL 1.8023 mL
30 mM 0.0601 mL 0.3004 mL 0.6008 mL 1.5019 mL
40 mM 0.0451 mL 0.2253 mL 0.4506 mL 1.1264 mL
50 mM 0.0360 mL 0.1802 mL 0.3605 mL 0.9011 mL
60 mM 0.0300 mL 0.1502 mL 0.3004 mL 0.7510 mL
80 mM 0.0225 mL 0.1126 mL 0.2253 mL 0.5632 mL
100 mM 0.0180 mL 0.0901 mL 0.1802 mL 0.4506 mL
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RQ-00203078 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:

RQ-002030781254205-52-1RQ00203078RQ 00203078TRP ChannelTransient receptor potential channelsTRPM8migrationinvasionoralmentholCa2+Inhibitorinhibitorinhibit

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