Submit a Review & Earn an Amazon Gift Card
You can now submit reviews for your favorite Tocris products. Your review will help other researchers decide on the best products for their research. Why not submit a review today?!
Submit ReviewRQ 00203078
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)
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.
产品说明书 for RQ 00203078
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
按产品操作查看相关产品
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
RQ 00203078 的评论
目前没有该产品的评论。 Be the first to review RQ 00203078 and earn rewards!
Have you used RQ 00203078?
Submit a review and receive an Amazon gift card.
$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image