Art. -Nr.: HY-18662

RQ-00203078

9 Cited Publications

Kundenbewertung

Based on 9 publication(s) in Google Scholar

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.

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Reinheit: 99.62%
CAS. Nr.: 1254205-52-1
Formel: C₂₁H₁₃ClF₆N₂O₅S
Molecular Weight:554.85

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

RQ-00203078 Chemical Structure

CAS. Nr.: 1254205-52-1

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (9)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]^[2]

TRPM8

5.3 nM (IC₅₀, Rat TRPM8 channels)

TRPM8

8.3 nM (IC₅₀, Human TRPM8 channels)

TRPV4

10 μM (IC₅₀)

Alle TRP Channel Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	>10 μM Compound: 36	Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of AITC-induced Ca2+ influx Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of AITC-induced Ca2+ influx	[PMID: 25455182]
HEK293	IC₅₀	>10 μM Compound: 36	Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced Ca2+ influx Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced Ca2+ influx	[PMID: 25455182]
HEK293	IC₅₀	>10 μM Compound: 36	Antagonist activity at rat TRPA1 expressed in HEK293 cells assessed as inhibition of AITC-induced Ca2+ influx Antagonist activity at rat TRPA1 expressed in HEK293 cells assessed as inhibition of AITC-induced Ca2+ influx	[PMID: 25455182]
HEK293	IC₅₀	>3 μM Compound: 36	Antagonist activity at human TRPV4 expressed in HEK293 cells assessed as inhibition of hypotonic solution-induced Ca2+ influx Antagonist activity at human TRPV4 expressed in HEK293 cells assessed as inhibition of hypotonic solution-induced Ca2+ influx	[PMID: 25455182]
HEK293	IC₅₀	>3 μM Compound: 36	Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced Ca2+ influx Antagonist activity at rat TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced Ca2+ influx	[PMID: 25455182]
HEK293	IC₅₀	8.3 nM Compound: 36	Antagonist activity at human TRPM8 expressed in HEK293 cells assessed as inhibition of menthol induced Ca2+ influx Antagonist activity at human TRPM8 expressed in HEK293 cells assessed as inhibition of menthol induced Ca2+ influx	[PMID: 25455182]

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.

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 C_max 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.

Chemical Information

CAS. Nr. 1254205-52-1
Appearance Solid
Molecular Weight 554.85
Formel C₂₁H₁₃ClF₆N₂O₅S
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
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

Publications (9)

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Journal Impact Factor

Chem Eng J

2026 Feb 5.
Int J Biol Macromol

Neuregulin 1 mitigated prolactin deficiency through enhancing TRPM8 signaling under the influence of melatonin in senescent pituitary lactotrophs. [Abstract]

2024 Aug;275(Pt 1):133659. PMID: 38969045
J Ethnopharmacol

Borneol exerts its antipruritic effects by inhibiting TRPA1 and activating TRPM8. [Abstract]

2024 Mar 25:322:117581. PMID: 38103845
Sci Rep

Targeting CB1 and TRPM8 receptors to counteract CD8+ T cell exhaustion. [Abstract]

2026 Apr 10;16(1):16876. PMID: 41963448
Cell Calcium

Activation of TRPM8 promotes K+ secretion in rat epididymal epithelium. [Abstract]

2026 Mar:134:103117. PMID: 41539212
Sci Rep

Control of motor coordination by transient receptor potential melastatin 8 through γ-aminobutyric acidergic circuit modulation in the male mouse cerebellum. [Abstract]

2025 Jul 1;15(1):22293. PMID: 40595448
Neuropharmacology

Deficiency of KIF15 contributes to oxaliplatin-induced cold hypersensitivity by limiting annexin A2 and enhancing TRPA1 localization in DRG neuronal membrane. [Abstract]

2025 May 15:269:110343. PMID: 39914618
Environ Toxicol Pharmacol

Exposure to formaldehyde at low temperatures aggravates allergic asthma involved in transient receptor potential ion channel. [Abstract]

2020 Nov:80:103469. PMID: 32798733
bioRxiv

Clonazepam activates the transient receptor potential melastatin 8 (TRPM8) ion channel. [Abstract]

2026 Jan 22:2026.01.19.700423. PMID: 41648152

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8023 mL

9.0114 mL

18.0229 mL

5 mM

0.3605 mL

1.8023 mL

3.6046 mL

10 mM

0.1802 mL

0.9011 mL

1.8023 mL

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

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Masashi Ohmi, et al. Identification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as a selective and orally active TRPM8 antagonist. Bioorg Med Chem Lett. 2014 Dec 1;24(23):5364-8. [Content Brief]

[2]. Yoshihiko Okamoto, et al. Blockade of TRPM8 activity reduces the invasion potential of oral squamous carcinoma cell lines. Int J Oncol. 2012 May;40(5):1431-40. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

RQ-00203078

9 Cited Publications

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RQ-00203078

Orally Active Compound Library

Mechanoreceptors Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Publications Citing Use of MedChemExpress (MCE) RQ-00203078

Alle TRP Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (9)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

RQ-00203078

Orally Active Compound Library

Mechanoreceptors Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Publications Citing Use of MedChemExpress (MCE) RQ-00203078

Alle TRP Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (9)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

RQ-00203078 Related Classifications

HY-18662 Related Classifications