RQ-00203078
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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).


Chemical Structure

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RQ-00203078
CAS# 1254205-52-1

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

Size Price Shipping out time Quantity
10mg USD 90 Same day
25mg USD 150 Same day
50mg USD 250 Same day
100mg USD 450 Same day
200mg USD 750 Same day
500mg USD 1250 Same day
1g USD 2150 Same day
2g USD 3850 Same day
5g USD 5850 Same day
Inquire bulk and customized quantity

Pricing updated 2021-03-02. Prices are subject to change without notice.

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

Appearance:
Solid powder

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

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).

Solubility:
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).

HS Tariff Code:
2934.99.9001

Preparing Stock Solutions

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.

Select a batch to recalculate based on the batch molecular weight:
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

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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.