Home Transmembrane Transporters TRP Channel antagonist SB366791

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SB366791 TRP Channel antagonist

Cat.No.S8238

SB-366791 is a novel, potent, and selective, cinnamide TRPV1 antagonist with an IC50 of 5.7 nM.
SB366791 TRP Channel antagonist Chemical Structure

Chemical Structure

Molecular Weight: 287.74

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Quality Control

Batch: S823801 DMSO]57 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.74%
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99.74

Solubility

In vitro
Batch:

DMSO : 57 mg/mL (198.09 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 287.74 Formula

C16H14ClNO2

 Storage (From the date of receipt)
CAS No. 472981-92-3 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles COC1=CC=CC(=C1)NC(=O)C=CC2=CC=C(C=C2)Cl

Mechanism of Action

Targets/IC50/Ki
TRPV1
(Cell-based assay)
5.7 nM
In vitro
SB-366791 is a structurally novel and potent TRPV1 antagonist which is capable of inhibiting the capsaicin-, acid- and heat-mediated activation of the receptor but produces little or no effect on a wide range of enzymes, ion channels, GPCRs and other proteins. This compound may prove to be a better tool for unambiguously defining the (patho)physiological role of TRPV1.
In vivo
the TRPV1 antagonist SB366791 reduces the number of flinches but did not improve ambulation and weight-bearing. A sub-analgesic dose of this compound potentiates the effects of morphine at doses of 3.0 and 10.0 mg/kg on flinches and weight-bearing but not ambulation. The combination of morphine and this chemical has potent analgesic effects on bone cancer pain.
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