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Nav1.8-IN-7 (Example 116) 为一种选择性Nav1.8抑制剂,当浓度达到100 nM时,其对Nav1.8的抑制效果超过50%。该化合物对hERG的抑制作用的IC50值为15.6 μM,显示出在疼痛研究中的应用潜力。
Nav1.8-IN-7 (Example 116) 为一种选择性Nav1.8抑制剂,当浓度达到100 nM时,其对Nav1.8的抑制效果超过50%。该化合物对hERG的抑制作用的IC50值为15.6 μM,显示出在疼痛研究中的应用潜力。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
10 mg | 询价 | 10-14周 | |
50 mg | 询价 | 10-14周 |
产品描述 | Nav1.8-IN-7 (Example 116) serves as a selective inhibitor of Nav1.8, demonstrating more than 50% inhibition at 100 nM specifically for Nav1.8. It exhibits an IC50 of 15.6 μM for the hERG channel. This compound holds promise in the field of pain research [1]. |
体外活性 | Nav1.8-IN-9 (Example 116; 1 μM) demonstrates inhibition rates of 1.2% for Nav1.1, 3.7% for Nav1.3, <1% for Nav1.4, <1% for Nav1.5, 2.6% for Nav1.6, and <1% for Nav1.7 [1]. |
体内活性 | Pharmacokinetic Parameters of Nav1.8-IN-7 in male Sprague-Dawley rats [1]: PO (100 mg/kg), C_max (ng/mL) 2566, AUC_0-24 (ng/mL∗h) 42454, t_1/2 (h) 8.7. |
分子量 | 515.84 |
分子式 | C22H18ClF4N3O5 |
CAS No. | 2761181-58-0 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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