TC-N 1752 是一种有效和具有口服活性的Nav1.7抑制剂，抑制hNav1.7，hNav1.3，hNav1.4，hNaV1.5和rNav1.8的IC50值分别为 0.17 μM，0.3 μM，0.4 μM，1.1 μM 和 2.2 μM。TC-N 1752 还抑制河豚毒素敏感的钠通道。TC-N 1752 在福尔马林疼痛模型中显示出镇痛效果。
| 生物活性 | TC-N 1752 is a potent and orally active inhibitor ofNav1.7, withIC50s of 0.17 μM, 0.3 μM, 0.4 μM, 1.1 μM and 2.2 μM athNav1.7,hNav1.3,hNav1.4,hNaV1.5andrNav1.8, respectively. TC-N 1752 also inhibits tetrodotoxin-sensitive sodium channels. TC-N 1752 shows analgesic efficacy in the Formalin model of pain[1][2][3]. |
| IC50& Target[1][2] | hNav1.7 0.17 μM (IC50) | hNav1.3 0.3 μM (IC50) | hNav1.4 0.4 μM (IC50) | hNav1.5 1.1 μM (IC50) | hNav1.8 0.1 μM (IC50) |
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体外研究
(In Vitro) | TC-N 1752 (compound 52) state-dependently inhibits Nav1.7, with IC50of 170 nM on channels that are 20% inactivated and IC50of 3.6 μM on fully noninactivated channels[1].
TC-N 1752 inhibits hNav1.7, hNav1.8, hNav1.9, rNav1.9, and mNav1.9 with IC50s of 0.2, 0.1, 1.6, 0.5 and 1.4 μM, respectively[2].
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体内研究
(In Vivo) | TC-N 1752 (compound 52) (3-30 mg/kg; p.o.) dose-dependently shows analgesic effect in the Formalin model[1].
TC-N 1752 (3-30 mg/kg; p.o.) decreases thermal hyperalgesia produced by inflammation[3].
TC-N 1752 (5 mg/mL; 500 μL; i.v.) attenuates complete Freund’s adjuvant (CFA)-induced sensitization of C-fiber nociceptors[3].
| Animal Model: | Rats were injected intraplantar with Formalin[1] | | Dosage: | 3, 10, 20, 30 mg/kg | | Administration: | Administered p.o. 120 min prior to Formalin | | Result: | Showed analgesic efficacy starting at the dose of 3 mg/kg, with full efficacy at 20 mg/kg dose. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 125 mg/mL(242.00 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.9360 mL | 9.6802 mL | 19.3603 mL | | 5 mM | 0.3872 mL | 1.9360 mL | 3.8721 mL | | 10 mM | 0.1936 mL | 0.9680 mL | 1.9360 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
