| CAS NO: | 1254205-52-1 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| Cas No. | 1254205-52-1 |
| 化学名 | 4-(N-(3-chloro-5-(trifluoromethyl)pyridin-2-yl)-N-(4-(trifluoromethoxy)benzyl)sulfamoyl)benzoic acid |
| Canonical SMILES | ClC1=C(N(CC2=CC=C(OC(F)(F)F)C=C2)S(C3=CC=C(C(O)=O)C=C3)(=O)=O)N=CC(C(F)(F)F)=C1 |
| 分子式 | C21H13ClF6N2O5S |
| 分子量 | 554.85 |
| 溶解度 | ≥ 18.85mg/mL in DMSO |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Description: IC50: 8.3 and 5.8 nM for hTRPM8 and rTRPM8, respectively The transient receptor potential melastatin 8 (TRPM8), a member of the TRP melastatin sub-group, is known to play a role in cold hyperalgesia and cold allodynia caused by disease conditions such as chemotherapy-induced peripheral neuropathy (CIPN, using the agents oxaliplatin, vincristine, or paclitaxel), diabetic neuropathy, migraine and overactive bladder (OAB). RQ-00203078 is identified as a selective and orally active TRPM8 antagonist. In vitro: In the menthol-induced calcium influx assay, RQ-00203078 is a novel and highly potent TRPM8 antagonist with human and rat IC50 values of 8.3 nM and 5.8 nM, respectively. RQ-00203078 was highly selective over other TRP channels [1]. In vivo: RQ-00203078 demonstrated excellent activity in vivo in a dose dependent manner with an ED50 value of 0.65 mg/kg in the icilin-induced wet-dog shakes model in rats after oral administration [1]. Clinical trial: Up to now, RQ-00203078 is still in the preclinical development stage. Reference: |
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