Palvanil

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Palvanil 是 TRPV1 的快速脱敏激动剂。它可能是治疗 IBS 的有前途的化合物，因为它可以调节肠道蠕动并减少内脏疼痛。

Palvanil is a fast desensitizing agonist of TRPV1. it may be promising agents in the therapy of IBS since it modulates intestinal motility and reduces visceral pain.

Palvanil (0.1-1000 nM; 0-300 min) leads to calcium increasment in HEK-293 intracellular.Palvanil (1-10 nM; 5 min) treatment desensitizes TRPV1 to the effect of Capsaicin significantly.Cell Viability Assay Cell Line:HEK-293 cells Concentration:0.1, 0.5, 1, 5, 10, 50, 100 and 1000 nM Incubation Time:0-300 min Result:Produced a dose-dependent increase in intracellular calcium with a EC50 of 0.65 nM.Cell Viability Assay Cell Line:HEK-293-TPRV1 cells Concentration:1-10 nM Incubation Time:5 min Result:Desensitized TRPV1 to the effect of Capsaicin significantly (IC50=0.81 nM).

Palvanil (subcutaneous injection; 1 or 10 mg/kg; once) treatment shows hypothermic effect.Palvanil (intraperitoneal injection; 100 μL (15 nM) per mouse; once) treatment reduces Capsaicin-induced bronchoconstriction. Palvanil (intravenous injection; 0.5, 0.75, and 1 mg/kg; once) treatment shows antinociceptive effects on Formalin-induced nocifensive behavior.Palvanil (intravenous injection; 0.5, 0.75, and 1 mg/kg; once) treatment inhibits Carrageenan-induced inflammation.Palvanil (intravenous injection; 0.5 and 1 mg/kg; once daily; 7 days) reduces mechanical allodynia and thermal hyperalgesia inspared nerve injury (SNI) mice. Animal Model:Male CD-1 miceDosage:1 or 10 mg/kg Administration:Subcutaneous injection; 1 or 10 mg/kg; once Result:Led to a slight and short lasting hypothermic effect, produced late hyperthermia.Animal Model:Female BALB/C mice Dosage:100 μL (15 nM) per mouse Administration:Intraperitoneal injection; 100 μL (15 nM) per mouse; once Result:Induced a significantly lower bronchoconstriction (from 0.47 to 0.605 cm H2O/L/s).Animal Model:Male CD-1 mice received formalin Dosage:0.5, 0.75, and 1 mg/kg Administration:Intravenous injection; 0.5, 0.75, and 1 mg/kg; once Result:Reduced the second phase of Formalin-induced nociceptive behaviour in a dose-dependent manner.Animal Model:Male C57BL/6J mice with acute inflammation induced by Carrageenan Dosage:2.5 mg/kg Administration:Intravenous injection; 2.5 mg/kg; once Result:Reduced the volume of the oedema in the ipsilateral hind paw (64%).Animal Model:Male CD-1 miceDosage:0.5 and 1 mg/kg Administration:Intravenous injection; 0.5 and 1 mg/kg; once daily; 7 days Result:Reduced mechanical allodynia and thermal hyperalgesia at 3 and 7 days after nerve injury in a dose-dependent manner.

Hexadecanamide

Membrane Transporter/Ion Channel

TRP/TRPV Channel

TRPV1

——

——

69693-13-6

391.59

C24H41NO3

>98% (HPLC)

——

CCCCCCCCCCCCCCCC(NCc(cc1)cc(OC)c1O)=O

——

(-20℃)

With Ice Pack

≥ 2 years