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RQ 00203078

Cat. No. 5388 2 篇引用文献 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Potent and selective TRPM8 antagonist; orally active
化学名： 4-[[[3-Chloro-5-(trifluoromethyl)-2-pyridinyl][[4-(trifluoromethoxy)phenyl]methyl]amino]sulfonyl]benzoic acid
纯度： ≥98% (HPLC)
说明书
引用文献 (2)
评论
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for RQ 00203078

RQ 00203078 is a potent TRPM8 antagonist (IC50 values are 5.3 and 8.3 nM for rat and human channels respectively). Exhibits >350-fold selectivity for TRPM8 over TRPV4, TRPV1 and TRPA1. Reduces HSC3 and HSC4 oral squamous carcinoma cell migration and invasion in vitro. Also attenuates icilin-induced wet dog shakes in rats. Orally active.

化合物库 for RQ 00203078

RQ 00203078 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。

技术数据 for RQ 00203078

分子量 554.85
公式 C21H13ClF6N2O5S
储存 Store at +4°C
纯度 ≥98% (HPLC)
CAS Number 1254205-52-1
PubChem ID 49783953
InChI Key IJGQFZYYEHCCIZ-UHFFFAOYSA-N
Smiles ClC1=C(N(S(C3=CC=C(C(O)=O)C=C3)(=O)=O)CC2=CC=C(OC(F)(F)F)C=C2)N=CC(C(F)(F)F)=C1

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for RQ 00203078

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 55.48 100
ethanol 55.48 100

制备储备液 for RQ 00203078

以下数据基于产品分子量 554.85。 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 1.8 mL 9.01 mL 18.02 mL
5 mM 0.36 mL 1.8 mL 3.6 mL
10 mM 0.18 mL 0.9 mL 1.8 mL
50 mM 0.04 mL 0.18 mL 0.36 mL

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参考文献 for RQ 00203078

参考文献是支持产品生物活性的出版物。

Okamoto et al (2012) Blockade of TRPM8 activity reduces the invasion potential of oral squamous carcinoma cell lines. Int.J.Oncol. 40 1431 PMID: 22267123

Ohmi et al (2014) Identification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as a selective and orally active TRPM8 antagonist. Bioorg.Med.Chem.Lett. 24 5364 PMID: 25455182

If you know of a relevant reference for RQ 00203078, please let us know.

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关键词: RQ 00203078, RQ 00203078 supplier, RQ00203078, potent, selective, TRPM8, antagonists, transient, receptors, potential, channels, orally, active, melastatin-related, TRPM, 5388, Tocris Bioscience

2 篇 RQ 00203078 的引用文献

引用文献是使用了 Tocris 产品的出版物。 RQ 00203078 的部分引用包括：

Martin F et al (2020) Mechanoactivation of NOX2-generated ROS elicits persistent TRPM8 Ca2+ signals that are inhibited by oncogenic KRas. Proc Natl Acad Sci U S A 117 26008-26019 PMID: 33020304

Gong and Jasmin (2017) Sustained MOR Administration Induces TRPM8-Dependent Cold Hyperalgesia. J Pain 18 212 PMID: 27845197

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