RQ-00203078
Cat. No.：YN360654
CAS No. ：1254205-52-1
| 产品名称: | RQ-00203078 |
| CAS No.: | 1254205-52-1 |
| Chemical Name: | 4-[[[3-chloro-5-(trifluoromethyl)-2-pyridinyl][[4-(trifluoromethoxy)phenyl]methyl]amino]sulfonyl]-benzoic acid |
| Synonyms: | |
| 分子量: | 554.85 |
| 分子式: | C₂₁H₁₃ClF₆N₂O₅S |
| SMILES: | 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 |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | RQ-00203078 是一种高选择性，有效且具有口服活性的TRPM8拮抗剂，对大鼠和人类TRPM8通道的IC50分别为 5.3 nM 和 8.3 nM。RQ-00203078 对 TRPV1，TRPA1，TRPV4 或 TRPM2 通道几乎没有抑制作用。 |
| IC50和靶点: | [{name:"TRPM8:5.3 nM (IC50, Rat TRPM8 channels)"},{name: "TRPM8:8.3 nM (IC50, Human TRPM8 channels)"},{name: "TRPV4:10 μM (IC50)"}] |
| In Vitro: | |
| In Vivo: | |
| Clinical Trial: | |
| Solvent & Solubility: |
Ohmi, M., Shishido, Y., Inoue, T., et al.Identification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as a selective and orally active TRPM8 antagonistBioorg. Med. Chem. Lett.24(23),5364-5368(2014)
Okamoto, Y., Ohkubo, T., Ikebe, T., et al.Blockade of TRPM8 activity reduces the invasion potential of oral squamous carcinoma cell linesInt. J. Oncol.40(5),1431-1440(2016)
