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RQ-00203078

Catalog No.
B5872
Selective and orally active TRPM8 antagonist
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$110.00
In stock
10mg
$125.00
In stock
50mg
$525.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Description:

IC50: 8.3 and 5.8 nM for hTRPM8 and rTRPM8, respectively

The transient receptor potential melastatin 8 (TRPM8), a member of the TRP melastatin sub-group, is known to play a role in cold hyperalgesia and cold allodynia caused by disease conditions such as chemotherapy-induced peripheral neuropathy (CIPN, using the agents oxaliplatin, vincristine, or paclitaxel), diabetic neuropathy, migraine and overactive bladder (OAB). RQ-00203078 is identified as a selective and orally active TRPM8 antagonist.

In vitro: In the menthol-induced calcium influx assay, RQ-00203078 is a novel and highly potent TRPM8 antagonist with human and rat IC50 values of 8.3 nM and 5.8 nM, respectively. RQ-00203078 was highly selective over other TRP channels [1].

In vivo: RQ-00203078 demonstrated excellent activity in vivo 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].

Clinical trial: Up to now, RQ-00203078 is still in the preclinical development stage.

Reference:
[1] Ohmi M, Shishido Y, Inoue T, Ando K, Fujiuchi A, Yamada A, Watanabe S, Kawamura K.  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.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt554.85
Cas No.1254205-52-1
FormulaC21H13ClF6N2O5S
Solubilityinsoluble in H2O; ≥18.85 mg/mL in DMSO; ≥27.25 mg/mL in EtOH
Chemical Name4-(N-(3-chloro-5-(trifluoromethyl)pyridin-2-yl)-N-(4-(trifluoromethoxy)benzyl)sulfamoyl)benzoic acid
SDFDownload SDF
Canonical SMILESClC1=C(N(CC2=CC=C(OC(F)(F)F)C=C2)S(C3=CC=C(C(O)=O)C=C3)(=O)=O)N=CC(C(F)(F)F)=C1
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control

Chemical structure

RQ-00203078