WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 407141

CAS#: 1254205-52-1

Description: RQ-00203078 is a potent, selective and orally active TRPM8 antagonist (IC50 values are 5.3 and 8.3 nM for rat and human channels respectively). RQ-00203078 blocks TRPM8 activity and reduces the invasion potential of oral squamous carcinoma cell lines. RQ-00203078 (RQ) profoundly reduced such agonist-induced cation currents. TRPM8 is reportedly an important player in carcinogenesis in human prostate cancer. 6).

Price and Availability


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RQ-00203078, purity > 98%, purity > 98%, is in stock. The same day shipping out after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee: from $30.00 (USA); from $45.00 (Canada); from $70.00 (international).

Chemical Structure


Theoretical Analysis

MedKoo Cat#: 407141
Name: RQ-00203078
CAS#: 1254205-52-1
Chemical Formula: C21H13ClF6N2O5S
Exact Mass: 554.01379
Molecular Weight: 554.84
Elemental Analysis: C, 45.46; H, 2.36; Cl, 6.39; F, 20.54; N, 5.05; O, 14.42; S, 5.78

Synonym: RQ-00203078; RQ 00203078; RQ00203078.

IUPAC/Chemical Name: 4-(N-(3-chloro-5-(trifluoromethyl)pyridin-2-yl)-N-(4-(trifluoromethoxy)benzyl)sulfamoyl)benzoic acid

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

Technical Data

Solid powder

>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (MSDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:


1: Ito H, Aizawa N, Sugiyama R, Watanabe S, Takahashi N, Tajimi M, Fukuhara H, Homma Y, Kubota Y, Andersson KE, Igawa Y. Functional role of the transient receptor potential melastatin 8 (TRPM8) ion channel in the urinary bladder assessed by conscious cystometry and ex vivo measurements of single-unit mechanosensitive bladder afferent activities in the rat. BJU Int. 2015 Jul 18. doi: 10.1111/bju.13225. [Epub ahead of print] PubMed PMID: 26189966.

2: 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. doi: 10.1016/j.bmcl.2014.10.074. Epub 2014 Oct 29. PubMed PMID: 25455182.

3: Okamoto Y, Ohkubo T, Ikebe T, Yamazaki J. Blockade of TRPM8 activity reduces the invasion potential of oral squamous carcinoma cell lines. Int J Oncol. 2012 May;40(5):1431-40. doi: 10.3892/ijo.2012.1340. Epub 2012 Jan 20. PubMed PMID: 22267123.

4: Al-Shamahi A, Kirkham K, Hookes L. Society for Neuroscience - 39th Annual Meeting. Part 1 - Novel therapies for the treatment of CNS disorders and pain. IDrugs. 2009 Dec;12(12):731-3. PubMed PMID: 19943210.