A TRPM8 antagonist
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RQ-00203078

Item No. 19075

Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[[3-chloro-5-(trifluoromethyl)-2-pyridinyl][[4-(trifluoromethoxy)phenyl]methyl]amino]sulfonyl]-benzoic acid
CAS Number
1254205-52-1
Molecular Formula
C21H13ClF6N2O5S
Formula Weight
554.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 25 mg/mlEthanol: 25 mg/ml
λmax
234, 278 nm
SMILES
OC(C1=CC=C(S(N(CC2=CC=C(OC(F)(F)F)C=C2)C3=NC=C(C(F)(F)F)C=C3Cl)(=O)=O)C=C1)=O
InChi Code
InChI=1S/C21H13ClF6N2O5S/c22-17-9-14(20(23,24)25)10-29-18(17)30(11-12-1-5-15(6-2-12)35-21(26,27)28)36(33,34)16-7-3-13(4-8-16)19(31)32/h1-10H,11H2,(H,31,32)
InChi Key
IJGQFZYYEHCCIZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $36

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    5 mg

    $135

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    10 mg

    $219

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    Cayman Chemical
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    Product Description

    RQ-00203078 is a selective antagonist of transient receptor potential melastatin 8 (TRPM8; IC50s = 8.3 and 5.8 nM in human and rat, respectively), while having little inhibitory action against TRPV1 (IC50 > 30 µM), TRPA1 (IC50 > 10 µM), TRPV4 (IC50 = 10 µM), or TRPM2 channels (IC50 > 10 µM).1 It attenuates icilin-induced wet-dog shakes in rats (ED50 = 0.65 mg/kg) after oral administration.1 RQ-00203078 has been shown to reduce HSC3 and HSC4 oral squamous carcinoma cell migration and invasion in vitro.2 TRPM8, a member of the TRP melastatin subgroup, plays a role in cold hyperalgesia and cold allodynia caused by disease conditions such as chemotherapy-induced peripheral neuropathy, diabetic neuropathy, migraine, and overactive bladder. It is also known to be involved in the tumor progression of certain carcinomas.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

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