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Chemical Structure| 1254205-52-1 Chemical Structure| 1254205-52-1

Structure of RQ-00203078
CAS No.: 1254205-52-1

Chemical Structure| 1254205-52-1

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RQ-00203078 is a selective antagonist of TRPM8 with IC50 of 8.3 nM.

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Product Details of RQ-00203078

CAS No. :1254205-52-1
Formula : C21H13ClF6N2O5S
M.W : 554.85
SMILES Code : 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
MDL No. :MFCD29049510
InChI Key :IJGQFZYYEHCCIZ-UHFFFAOYSA-N
Pubchem ID :49783953

Safety of RQ-00203078

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Description
RQ-00203078, a potent, orally active, and highly selective antagonist of TRPM8 channels, exhibits IC50s of 5.3 nM and 8.3 nM for rat and human TRPM8 channels, respectively, while showing minimal inhibitory effects on TRPV1, TRPA1, TRPV4, and TRPM2 channels[1].[2].

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Chronic morphine-induced cold hyperalgesia model Intraperitoneal injection 3 mg/kg Single administration, tested 2 hours post-administration To verify the inhibitory effect of the TRPM8 selective antagonist RQ-00203078 on morphine-induced cold hyperalgesia. Results showed that RQ-00203078 significantly reduced the number of paw lifts in morphine-treated rats, indicating a key role of TRPM8 channels in cold hyperalgesia. J Pain. 2017 Feb;18(2):212-221

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.80mL

0.36mL

0.18mL

9.01mL

1.80mL

0.90mL

18.02mL

3.60mL

1.80mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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