In vivo
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AMG 9810

In vivo
Product Name
AMG 9810
CAS No.
545395-94-6
Chemical Name
AMG 9810
Synonyms
9810;CS-2548;AMG 9810;AMG 9810;AMG-9810;AMG 9810 >=98% (HPLC), powder;(2E)-N-(2,3-Dihydro-1,4-benzodi;3-[4-(TERT-BUTYL)PHENYL]-N-(2,3-DIHYDRO-1,4-BENZODIOXIN-6-YL)ACRYLAMIDE;3-(4-tert-Butyl-phenyl)-N-(2,3-dihydro-benzo[1,4]dioxin-6-yl)-acrylamide;(2E)-3-(4-tert-butylphenyl)-N-(2,3-dihydro-1,4-benzodioxin-6-yl)prop-2-enamide;(2E)-N-(2,3-DIHYDRO-1,4-BENZODIOXIN-6-YL)-3-[4-(1,1-DIMETHYLETHYL)PHENYL]-2-PROPENAMIDE
CBNumber
CB0306302
Molecular Formula
C21H23NO3
Formula Weight
337.41
MOL File
545395-94-6.mol
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AMG 9810 Property

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
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Safety

Hazard Codes 
Xn
Risk Statements 
22
WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H413May cause long lasting harmful effects to aquatic life

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P273Avoid release to the environment.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
A2731
Product name
AMG 9810
Purity
≥98% (HPLC), powder
Packaging
10mg
Price
$227
Updated
2024/03/01
Sigma-Aldrich
Product number
A2731
Product name
AMG 9810
Purity
≥98% (HPLC), powder
Packaging
50mg
Price
$357.6
Updated
2024/03/01
Alfa Aesar
Product number
J64202
Product name
AMG 9810
Packaging
25mg
Price
$308
Updated
2023/06/20
Cayman Chemical
Product number
14715
Product name
AMG 9810
Purity
≥98%
Packaging
5mg
Price
$57
Updated
2024/03/01
Cayman Chemical
Product number
14715
Product name
AMG 9810
Purity
≥98%
Packaging
10mg
Price
$95
Updated
2024/03/01
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AMG 9810 Chemical Properties,Usage,Production

In vivo

AMG9810 is effective at preventing capsaicin-induced eye wiping in a dose-dependent manner, and it reverses thermal and mechanical hyperalgesia in a model of inflammatory pain induced by intraplantar injection of complete Freund's adjuvant. At effective doses, AMG9810 does not show any significant effects on motor function. AMG9810 is the first cinnamide TRPV1 antagonist reported to block capsaicin-induced eye wiping behavior and reverse hyperalgesia in an animal model of inflammatory pain. AMG9810, promotes mouse skin tumor development. The topical application of AMG9810 results in a significant increase in the expression level of the epidermal growth factor receptor (EGFR) and its downstream Akt/mammalian target of rapamycin (mTOR)-signaling pathway.

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-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.

Uses

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]

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.

AMG 9810 Preparation Products And Raw materials

Raw materials

Preparation Products

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AMG 9810 Suppliers

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View Lastest Price from AMG 9810 manufacturers

Career Henan Chemical Co
Product
(2E)-N-(2,3-DIHYDRO-1,4-BENZODIOXIN-6-YL)-3-[4-(1,1-DIMETHYLETHYL)PHENYL]-2-PROPENAMIDE 545395-94-6
Price
US $9.80/KG
Min. Order
1g
Purity
≥99%
Supply Ability
100kg
Release date
2020-01-12

545395-94-6, AMG 9810Related Search:


  • 3-[4-(TERT-BUTYL)PHENYL]-N-(2,3-DIHYDRO-1,4-BENZODIOXIN-6-YL)ACRYLAMIDE
  • AMG 9810
  • CS-2548
  • AMG 9810;AMG-9810
  • (2E)-N-(2,3-DIHYDRO-1,4-BENZODIOXIN-6-YL)-3-[4-(1,1-DIMETHYLETHYL)PHENYL]-2-PROPENAMIDE
  • 3-(4-tert-Butyl-phenyl)-N-(2,3-dihydro-benzo[1,4]dioxin-6-yl)-acrylamide
  • 9810
  • (2E)-N-(2,3-Dihydro-1,4-benzodioxin-6-yl)-3-[4-(1,1-dimethylethyl)phenyl]-2-propanamide
  • 2-PropenaMide, N-(2,3-dihydro-1,4-benzodioxin-6-yl)-3-[4-(1,1-diMethylethyl)phenyl]-, (2E)-
  • AMG 9810 >=98% (HPLC), powder
  • (2E)-3-(4-tert-butylphenyl)-N-(2,3-dihydro-1,4-benzodioxin-6-yl)prop-2-enamide
  • Transient receptor potential channels,inhibit,Inhibitor,AMG-9810,AMG9810,AMG 9810,TRP Channel
  • (2E)-N-(2,3-Dihydro-1,4-benzodi
  • 545395-94-6
  • Vanilloid/TRPV channel