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).
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
RQ-00203078, purity > 98%, purity > 98%, is in stock. The same day shipping out after order is received.
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
InChi Key: IJGQFZYYEHCCIZ-UHFFFAOYSA-N
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)
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
The following data is based on the product molecular weight 554.84 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
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.
