2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. AMG9810

AMG9810 

Cat. No.: HY-101736 Purity: 99.83%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

AMG9810 Chemical Structure

AMG9810 Chemical Structure

CAS No. : 545395-94-6

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 61 In-stock
Solution
10 mM * 1 mL in DMSO USD 61 In-stock
Solid
5 mg USD 55 In-stock
10 mg USD 72 In-stock
50 mg USD 286 In-stock
100 mg USD 506 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 2 publication(s) in Google Scholar

AMG9810 Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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.

IC50 & Target

IC50: 24.5 nM (human TRPV1), 85.6 nM (rat TRPV1)[1]
In Vitro

AMG9810 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. AMG9810 blocks capsaicin-evoked depolarization and calcitonin gene-related peptide release in cultures of rat dorsal root ganglion primary neurons. AMG9810 inhibits capsaicin-, proton-, heat-, and endogenous ligand-induced uptake of 45Ca2+ into TRPV1-expressing cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AMG9810 Related Antibodies
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[1]. 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[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

337.41

Appearance

Solid

Formula

C21H23NO3
CAS No.
SMILES

O=C(NC1=CC=C(OCCO2)C2=C1)/C=C/C3=CC=C(C(C)(C)C)C=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 33 mg/mL (97.80 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9638 mL 14.8188 mL 29.6375 mL
5 mM 0.5928 mL 2.9638 mL 5.9275 mL
10 mM 0.2964 mL 1.4819 mL 2.9638 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation
References
Kinase Assay
[1]

Cultured adult rat dorsal root ganglia neurons in 96-well plates are washed twice with release buffer to initiate the assay. CGRP release is induced by incubation of neurons with capsaicin for 10 min at room temperature. The cultures are preincubated with increasing concentrations of capsazepine or AMG9810 for 15 min, followed by 300 nM capsaicin activation for 10 min at room temperature. The extracellular medium is collected and the CGRP content is determined using a commercially kit[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[2]

To assess cyotoxicity of AMG9810, N/TERT1 cells are treated with different concentrations of AMG9810 (0.25, 0.5, 1, 5 μM) and cultured for various periods of time (24, 48, 72 h). The CellTiter 96 AQueous One Solution is added to each well and then cells are kept in a 37°C, 5% CO2 incubator for 1 h. Absorbance is then measured at 492 and 690 nm with a plate reader[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Rats: AMG9810 is dissolved in DMSO. Rats are acclimated for 30 to 45 min in a 30×30×30-cm Plexiglas chambers before the intraperitoneal injection of either vehicle (DMSO) or AMG 9810. Injections are made over a 5-s period in the lower right ventral quadrant of the abdomen either 15, 30, or 60 min before intraocular application of capsaicin. Intraocular application of capsaicin (3 μg/20 μL in 10% ethanol/PBS) or vehicle (20 μL in 10% ethanol/PBS) is done with a pipette, and the number of front paw eye wipes is counted over a 5-min period in 1-min intervals [1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
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AMG9810 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

AMG9810545395-94-6AMG 9810AMG-9810TRP ChannelTransient receptor potential channelsInhibitorinhibitorinhibit

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