AMG 9810
Synonym(s):2E-N-(2,3-Dihydro-1,4-benzodioxin-6-yl)-3-[4-(1,1-dimethylethyl)phenyl]-2-Propenamide
- CAS NO.:545395-94-6
- Empirical Formula: C21H23NO3
- Molecular Weight: 337.41
- MDL number: MFCD00955103
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-06-30 15:45:59
What is AMG 9810?
Description
AMG 9810 is a competitive antagonist of capsaicin activation of the vanilloid receptor 1 (TRPV1) (IC50s = 24.5 and 85.6 nM for human and rat, respectively). Additionally, it has been shown to compete with other modes of TRPV1 activation, including protons (IC50s = 92.7 and 294 nM for human and rat, respectively), heat (IC50s = 15.8 and 21 nM for human and rat, respectively), and the endogenous ligands: anandamide, N-
The Uses of AMG 9810
AMG 9810 is a competitive antagonist of capsaicin activation of the vanilloid receptor 1 (TRPV1) (IC50s = 24.5 and 85.6 nM for human and rat, respectively). Additionally, it has been shown to compete with other modes of TRPV1 activation, including protons (IC50s = 92.7 and 294 nM for human and rat, respectively), heat (IC50s = 15.8 and 21 nM for human and rat, respectively), and the endogenous ligands: anandamide, N-arachidonyl dopamine (IC50s = 8.5 and 260 nM for human and rat, respectively), and oleoyldopamine. In a rat model of inflammatory pain induced by intraplantar injection of complete Freund’s adjuvant, 30-100 mg/kg AMG 9810 reverses thermal and mechanical hyperalgesia.[Cayman Chemical]
What are the applications of Application
AMG-9810 is a vanilloid receptor antagonist
Definition
ChEBI: 3-(4-tert-butylphenyl)-N-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-propenamide is a member of cinnamamides and a secondary carboxamide.
Biological Activity
AMG 9810 is a potent and selective, competitive vanilloid TRPV1 receptor antagonist (IC 50 = 17 nM). Inhibits capsaicin-, proton-, heat- and endogenous ligand-induced activation of human and rat recombinant TRPV1 receptors. Displays antihyperalgesic properties in a rat model of inflammatory pain.
Biochem/physiol Actions
AMG 9810?is the cinnamide TRPV1 (vanilloid receptor 1) antagonist, that can prevent eye wiping behavior, stimulated by capsaicin and can inverse hyperalgesia in an animal model of inflammatory pain. It possesses antihyperalgesic properties.
storage
+4°C (desiccate)
References
[1]. gavva nr, tamir r, qu y, et al. amg 9810 [(e)-3-(4-t-butylphenyl)-n-(2, 3-dihydrobenzo[b][1,4] dioxin-6-yl)acrylamide], a novel vanilloid receptor 1 (trpv1) antagonist with antihyperalgesic properties. j pharmacol exp ther, 2005, 313(1):474-84.
Properties of AMG 9810
Boiling point: | 512.5±50.0 °C(Predicted) |
Density | 1.175±0.06 g/cm3(Predicted) |
storage temp. | 2-8°C |
solubility | DMSO: >5mg/mL |
pka | 12.22±0.20(Predicted) |
form | powder |
color | white to beige |
Safety information for AMG 9810
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H413:Hazardous to the aquatic environment, long-term hazard |
Precautionary Statement Codes |
P264:Wash hands thoroughly after handling. P264:Wash skin thouroughly after handling. P270:Do not eat, drink or smoke when using this product. P273:Avoid release to the environment. P301+P312:IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell. P501:Dispose of contents/container to..… |
Computed Descriptors for AMG 9810
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