| Field | Specification |
|---|---|
| Mfr No | |
| Activity | |
| Cas No. | |
| Concentration | |
| Form | Lyophilized powder. |
| Product Type | |
| Purity | |
| Reconstitution | |
| Shipping | |
| Solubility | 100 mM in DMSO or 50 mM in ethanol. Centrifuge all product preparations before use (10000 x g 5 min). |
| Source | Synthetic |
| Storage | |
| Target |
Product details
- Chemical name: 1-[3-(trifluoromethyl)pyridin-2-yl]-N-[4-(trifluoromethylsulfonyl)phenyl]-3,6-dihydro-2H-pyridine-4-carboxamide.
- Also known as: CHEMBL482834
- CAS number: 824982-41-4
- Molecular formula: C19H15F6N3O3S.
- Purity: >99%
- Concentration: 10 nM - 1 µM.
- Form: Lyophilized powder.
- Solubility: 100 mM in DMSO or 50 mM in ethanol. Centrifuge all product preparations before use (10000 x g 5 min).
- Reconstitution: 100 mM in DMSO or 50 mM in ethanol. Centrifuge all product preparations before use (10000 x g 5 min).
- Shipping: Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
- Target: TRPV1 channel
- Source: Synthetic
- Activity: A 784168 is a potent TRPV1 antagonist, inhibiting human TRPV1 activation by 50 nM capsaicin with IC50 of 25 nM1.
- Alternative names: CHEMBL482834
Scientific background
A 784168 is a synthetic and potent antagonist of the TRPV1 channel. A 784168 inhibits human TRPV1 activation by 50 nM capsaicin with an IC50 of 25 nM. A 784168 was found to produce inhibition in 1321N1 astrocytoma cells expressing recombinant human TRPV1 and also in HEK 293 cells. In addition to its inhibition of TRPV1, A 784168 was found to be a very weak antagonist of TRPM8 (IC50 = 20.8 µM) with no effect on TRPA1 channels and a variety of receptors including adenosine, angiotensin, α- and β-adrenergic receptors. A 784168 has a plasma binding capacity of 93.5±0.9% and oral bioavailability of 33%. A 784168 volume of distribution is 12.4L/kg and it has high blood-brain barrier penetrance. Administration of oral A 784168 reduces acute nociceptive behavior induced by capsaicin injection and chronic thermal hyperalgesia induced by CFA injection in a rat model1.
Lead time: 1-2 Business Days
Country of origin: Israel/IL
Applications key
Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.
Bioassay tested: Yes
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