产品
编 号：F073253
分子式：C25H27F3N6O3
分子量：516.52
分子式：C25H27F3N6O3
分子量：516.52
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 1211866-85-1
产品详情
生物活性：
TC-N 1752 is a potent and orally active inhibitor of Nav1.7, with IC50s of 0.17 μM, 0.3 μM, 0.4 μM, 1.1 μM and 2.2 μM at hNav1.7, hNav1.3, hNav1.4, hNaV1.5 and rNav1.8, respectively. TC-N 1752 also inhibits tetrodotoxin-sensitive sodium channels. TC-N 1752 shows analgesic efficacy in the Formalin model of pain.
体内研究：
TC-N 1752 (compound 52) (3-30 mg/kg; p.o.) dose-dependently shows analgesic effect in the Formalin model.TC-N 1752 (3-30 mg/kg; p.o.) decreases thermal hyperalgesia produced by inflammation.TC-N 1752 (5 mg/mL; 500 μL; i.v.) attenuates complete Freund’s adjuvant (CFA)-induced sensitization of C-fiber nociceptors.Animal Model:Rats were injected intraplantar with Formalin
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.
体外研究：
TC-N 1752 (compound 52) state-dependently inhibits Nav1.7, with IC50 of 170 nM on channels that are 20% inactivated and IC50 of 3.6 μM on fully noninactivated channels.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.
TC-N 1752 is a potent and orally active inhibitor of Nav1.7, with IC50s of 0.17 μM, 0.3 μM, 0.4 μM, 1.1 μM and 2.2 μM at hNav1.7, hNav1.3, hNav1.4, hNaV1.5 and rNav1.8, respectively. TC-N 1752 also inhibits tetrodotoxin-sensitive sodium channels. TC-N 1752 shows analgesic efficacy in the Formalin model of pain.
体内研究：
TC-N 1752 (compound 52) (3-30 mg/kg; p.o.) dose-dependently shows analgesic effect in the Formalin model.TC-N 1752 (3-30 mg/kg; p.o.) decreases thermal hyperalgesia produced by inflammation.TC-N 1752 (5 mg/mL; 500 μL; i.v.) attenuates complete Freund’s adjuvant (CFA)-induced sensitization of C-fiber nociceptors.Animal Model:Rats were injected intraplantar with Formalin
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.
体外研究：
TC-N 1752 (compound 52) state-dependently inhibits Nav1.7, with IC50 of 170 nM on channels that are 20% inactivated and IC50 of 3.6 μM on fully noninactivated channels.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.
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