Molecular Formula | C16H14ClNO2 |
Molar Mass | 287.74 |
Melting Point | 165-167℃ |
Solubility | DMSO |
Appearance | solid |
Color | off-white |
Storage Condition | Sealed in dry,Room Temperature |
Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
Use | SB-366791 is a new and selective cinnamide TRPV1 antagonist. |
Target | hTRPV1 |
In vitro study | SB-366791 is a novel and potent TRPV1 antagonist. This compound is capable of inhibiting capsaicin-, acid- and heat-mediated activation of TRPV1, but has no or little effect on most enzymes, ion channels, GPCRs and proteins. SB-366791 may be a powerful tool to study and understand the pathophysiological role of TRPV1. |
In vivo study | The TRPV1 antagonist SB366791 reduced spontaneous pain behavior (withdrawal) but did not improve mobility and weight-bearing. A sub-analgesic dose of SB366791 potentiated the effects of 3 mg/kg and 10 mg/kg morphine on spontaneous pain response and weight bearing, but had no effect on locomotion. The combined use of morphine and SB366791 has an effective analgesic effect on bone cancer pain. |
Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. |
WGK Germany | 3 |
Reference Show more | 1. Lappin SC, et al. TRPV1 antagonist, SB-366791, inhibits glutamatergic synaptic transmission in rat spinal dorsal horn following peripheral inflammation. Eur J Pharmacol. 2006;540(1-3):73-81.2. Gunthorpe MJ, et al. Identification and characterisation of SB-366791, a potent and selective vanilloid receptor (VR1/TRPV1) antagonist [published correction appears in Neuropharmacology. 2004 May;46(6):905]. Neuropharmacology. 2004;46(1):133-149. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.475 ml | 17.377 ml | 34.754 ml |
5 mM | 0.695 ml | 3.475 ml | 6.951 ml |
10 mM | 0.348 ml | 1.738 ml | 3.475 ml |
5 mM | 0.07 ml | 0.348 ml | 0.695 ml |
biological activity | SB-366791 is a novel potent and selective TRPV1 antagonist. The IC50 was 5.7 nM. |
Target | TargetValue TRPV1 (Cell-based assay) 5.7 nM |
Target | Value |
TRPV1 (Cell-based assay) | 5.7 nM |
in vitro study | SB-366791 is a novel and potent TRPV1 antagonist. This compound is capable of inhibiting capsaicin-, acid- and heat-mediated activation of TRPV1, but has no or little effect on most enzymes, ion channels, GPCRs and proteins. SB-366791 may be a powerful tool to study and understand the pathophysiological role of TRPV1. |
in vivo study | The TRPV1 antagonist SB366791 reduces spontaneous painful behavior (paw withdrawal), but there was no improvement on mobility and weight-bearing. A sub-analgesic dose of SB366791 potentiated the effects of 3 mg/kg and 10 mg/kg morphine on spontaneous pain response and weight bearing, but had no effect on locomotion. The combined use of morphine and SB366791 has an effective analgesic effect on bone cancer pain. |