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

RQ-00203078 

Cat. No.: HY-18662 Purity: 99.84%
Handling Instructions

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
10 mM * 1 mL in DMSO USD 67 In-stock
Estimated Time of Arrival: December 31
5 mg USD 55 In-stock
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
50 mg USD 250 In-stock
Estimated Time of Arrival: December 31
100 mg USD 450 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

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 Cmax value of 2300 ng/mL and 86% bioavailability[1].

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

Molecular Weight

554.85

Formula

C₂₁H₁₃ClF₆N₂O₅S

CAS No.

1254205-52-1

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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 38 mg/mL (68.49 mM)

*"≥" means soluble, but saturation unknown.

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
10 mM 0.1802 mL 0.9011 mL 1.8023 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.51 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

RQ-00203078RQ00203078RQ 00203078TRP ChannelTransient receptor potential channelsTRPM8migrationinvasionoralmentholCa2+Inhibitorinhibitorinhibit

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Product Name:
RQ-00203078
Cat. No.:
HY-18662
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