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).


Price and Availability

Size
Price

10mg
USD 90
100mg
USD 450
1g
USD 2150
Size
Price

25mg
USD 150
200mg
USD 750
2g
USD 3850
Size
Price

50mg
USD 250
500mg
USD 1250
5g
USD 5850

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

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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

Appearance:
Solid powder

Purity:
>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).

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).

Harmonized System Code:
293490


References

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.