AMG 9810

TRPV1 antagonist CAS# 545395-94-6

AMG 9810

Catalog No. BCC7329----Order now to get a substantial discount!

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Chemical structure

AMG 9810

3D structure

Chemical Properties of AMG 9810

Cas No. 545395-94-6 SDF Download SDF
PubChem ID 680502 Appearance Powder
Formula C21H23NO3 M.Wt 337.42
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 33 mg/mL (97.80 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name (E)-3-(4-tert-butylphenyl)-N-(2,3-dihydro-1,4-benzodioxin-6-yl)prop-2-enamide
SMILES CC(C)(C)C1=CC=C(C=C1)C=CC(=O)NC2=CC3=C(C=C2)OCCO3
Standard InChIKey GZTFUVZVLYUPRG-IZZDOVSWSA-N
Standard InChI InChI=1S/C21H23NO3/c1-21(2,3)16-7-4-15(5-8-16)6-11-20(23)22-17-9-10-18-19(14-17)25-13-12-24-18/h4-11,14H,12-13H2,1-3H3,(H,22,23)/b11-6+
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of AMG 9810

DescriptionPotent and selective, competitive vanilloid TRPV1 receptor antagonist (IC50 = 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.

AMG 9810 Dilution Calculator

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Preparing Stock Solutions of AMG 9810

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.9637 mL 14.8183 mL 29.6367 mL 59.2733 mL 74.0916 mL
5 mM 0.5927 mL 2.9637 mL 5.9273 mL 11.8547 mL 14.8183 mL
10 mM 0.2964 mL 1.4818 mL 2.9637 mL 5.9273 mL 7.4092 mL
50 mM 0.0593 mL 0.2964 mL 0.5927 mL 1.1855 mL 1.4818 mL
100 mM 0.0296 mL 0.1482 mL 0.2964 mL 0.5927 mL 0.7409 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on AMG 9810

AMG 9810 is a vanilloid receptor 1 (VR1 or TRPV1) antagonist, with IC50 values for human TRPV1 of 24.5±15.7 nM, for rat TRPV1 of 85.6 ±39.4 nM as a competitive antagonist of capsaicin activation. To block protons, its IC50 values for rat TRPV1 is 294±192 nM, for human TRPV1 is 92.7±72.8 nM. To block heat, its IC50 value for rat TRPV1 is 21±17 nM, for human TRPV1 is 15.8±10.8 nM. It can also block endogenous ligands, such as N-arachidonyl dopamine, anandamide and oleoyldopamine [1].

TRPV1 is expressed by peripheral sensory neurons. It is a membrane-bound, nonselective cation channel [1].

In rat dorsal root ganglia neurons with the presence of endogenous TRPV1, 45Ca2+ uptake was induced by capsaicin in a dose-dependent manner, the EC90 value is 300 nM. In a Ca2+-dependent manner, capsaicin induces CGRP release through the activation of TRPV1. Capsaicin at 300 nM induced a greater level of CGRP release from cultured neurons into the media, compared with the basal level. Capsaicin-induced 45Ca2+ uptake and CGRP release was potently blocked by AMG 9810 with IC50 values of 9±6 nM and 6±3 nM, respectively. AMG 9810 alone up to 10 ?M had no effect on the basal 45Ca2+ uptake or CGRP release of exposed neurons [1].

In animals capsaicin induced eye wipes. Intraperitoneally, AMG 9810 at 3, 10, and 30 mg/kg, dose-dependently decrease this effect at 15 min. Treatment with AMG 9810 at 10 and 30 mg/kg, 30 min before capsaicin treatment, statistically significantly reduced the number of eye wipes. Only treatment with AMG 9810 at 30 mg/kg 60 min before capsaicin administration significantly reduced eye wipes. Vehicle did not affect capsaicin-evoked eye wipes [1].

Reference:
[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.

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References on AMG 9810

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.[Pubmed:15615864]

J Pharmacol Exp Ther. 2005 Apr;313(1):474-84.

The vanilloid receptor 1 (VR1 or TRPV1) is a membrane-bound, nonselective cation channel expressed by peripheral sensory neurons. TRPV1 antagonists produce antihyperalgesic effects in animal models of inflammatory and neuropathic pain. Here, we describe the in vitro and in vivo pharmacology of a novel TRPV1 antagonist, AMG 9810, (E)-3-(4-t-butylphenyl)-N-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)acrylamide. AMG 9810 is a competitive antagonist of capsaicin activation (IC50 value for human TRPV1, 24.5 +/- 15.7 nM; rat TRPV1, 85.6 +/- 39.4 nM) and blocks all known modes of TRPV1 activation, including protons (IC50 value for rat TRPV1, 294 +/- 192 nM; human TRPV1, 92.7 +/- 72.8 nM), heat (IC50 value for rat TRPV1, 21 +/- 17 nM; human TRPV1, 15.8 +/- 10.8 nM), and endogenous ligands, such as anandamide, N-arachidonyl dopamine, and oleoyldopamine. AMG 9810 blocks capsaicin-evoked depolarization and calcitonin gene-related peptide release in cultures of rat dorsal root ganglion primary neurons. Screening of AMG 9810 against a panel of G protein-coupled receptors and ion channels indicated selectivity toward TRPV1. In vivo, AMG 9810 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, AMG 9810 did not show any significant effects on motor function, as measured by open field locomotor activity and motor coordination tests. AMG 9810 is the first cinnamide TRPV1 antagonist reported to block capsaicin-induced eye wiping behavior and reverse hyperalgesia in an animal model of inflammatory pain.

Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides.[Pubmed:15634002]

J Med Chem. 2005 Jan 13;48(1):71-90.

The vanilloid receptor-1 (TRPV1 or VR1) is a member of the transient receptor potential (TRP) family of ion channels and plays a role in regulating the function of sensory nerves. A growing body of evidence demonstrates the therapeutic potential of TRPV1 modulators, particularly in the management of pain. As a result of our screening efforts, we identified (E)-3-(4-tert-butylphenyl)-N-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)acrylamide (1), an antagonist that blocks the capsaicin-induced and pH-induced uptake of (45)Ca(2+) in TRPV1-expressing Chinese hamster ovary cells with IC(50) values of 17 +/- 5 and 150 +/- 80 nM, respectively. In this report, we describe the synthesis and structure-activity relationship of a series of N-aryl cinnamides, the most potent of which (49a and 49b) exhibit good oral bioavailability in rats (F(oral) = 39% and 17%, respectively).

Description

AMG9810 is a selective and competitive vanilloid receptor 1 (TRPV1) antagonist with IC50 values of 24.5 and 85.6 nM for human and rat TRPV1, repectively.

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