RQ-00203078
货号：
19075-1mg 基本售价：
350.0 元 规格：
1 mg
产品信息
概述| 货号 | 19075-1mg |
| 描述 | RQ-00203078 is a selective antagonist of transient receptor potential melastatin 8 (TRPM8; IC50s = 8.3 and 5.8 nM in human and rat, respectively), while having little inhibitory action against TRPV1 (IC50 > 30 µM), TRPA1 (IC50 > 10 µM), TRPV4 (IC50 = 10 µM), or TRPM2 channels (IC50 > 10 µM).1 It attenuates icilin-induced wet-dog shakes in rats (ED50 = 0.65 mg/kg) after oral administration.1 RQ-00203078 has been shown to reduce HSC3 and HSC4 oral squamous carcinoma cell migration and invasion in vitro.2 TRPM8, a member of the TRP melastatin subgroup, plays a role in cold hyperalgesia and cold allodynia caused by disease conditions such as chemotherapy-induced peripheral neuropathy, diabetic neuropathy, migraine, and overactive bladder. It is also known to be involved in the tumor progression of certain carcinomas. |
性能| 供应商 | Cayman |
| 应用文献 |
1.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 antagonist. Bioorganic & Medicinal Chemistry Letters 24(23), 5364-5368 (2014).
2.Okamoto, Y.,Ohkubo, T.,Ikebe, T., et al. Blockade of TRPM8 activity reduces the invasion potential of oral squamous carcinoma cell lines. International Journal of Oncology 40(5), 1431-1440 (2016).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 554.8 |
| 分子式 | C21H13ClF6N2O5S |
| CAS号 | 1254205-52-1 |
| 稳定性 | ≥ 2 years |
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