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Palvanil

SKU: orb1940895

Description

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.

Images & Validation

Key Properties

CAS Number69693-13-6
MW391.59
Purity>98% (HPLC)
FormulaC24H41NO3
SMILESCCCCCCCCCCCCCCCC(NCc(cc1)cc(OC)c1O)=O
TargetTRP/TRPV Channel

Bioactivity

In Vivo
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 mice. Dosage: 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 mice. Dosage: 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.
In Vitro
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).

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Hexadecanamide

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Palvanil (orb1940895)

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100 mg
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2 mg
$ 290.00
5 mg
$ 410.00
10 mg
$ 610.00
25 mg
$ 980.00
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$ 1,370.00