Art. -Nr.: HY-10634

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AMG 517

6 Cited Publications

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Based on 6 publication(s) in Google Scholar

AMG 517 is a potent and selective vanilloid receptor-1 (TRPV1) antagonist with an IC₅₀ of 0.5 nM.

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Reinheit: 99.24%
CAS. Nr.: 659730-32-2
Formel: C₂₀H₁₃F₃N₄O₂S
Molecular Weight:430.40

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

AMG 517 Chemical Structure

CAS. Nr.: 659730-32-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (6)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

AMG 517 is a potent and selective vanilloid receptor-1 (TRPV1) antagonist with an IC₅₀ of 0.5 nM.

IC₅₀ & Target

IC50: 0.5 nM (TRPV1)^[1]

Alle TRP Channel Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.5 nM Compound: 1, AMG-517	Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of pH 5 acid-induced 45Ca2+ influx by FLIPR assay Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of pH 5 acid-induced 45Ca2+ influx by FLIPR assay	[PMID: 18722118]
CHO	IC₅₀	0.5 nM Compound: 1	Antagonist activity at rat TRPV1 expressed in CHO cells assessed inhibition of acid induced calcium influx Antagonist activity at rat TRPV1 expressed in CHO cells assessed inhibition of acid induced calcium influx	[PMID: 17937985]
CHO	IC₅₀	0.5 nM Compound: 1, AMG-517	Inhibition of rat TRPV1 expressed in CHO cells assessed as acid-induced Ca2+ influx Inhibition of rat TRPV1 expressed in CHO cells assessed as acid-induced Ca2+ influx	[PMID: 17585751]
CHO	IC₅₀	0.5 nM Compound: 23	Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of acid-induced calcium influx Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of acid-induced calcium influx	[PMID: 17585750]
CHO	IC₅₀	0.5 nM Compound: 3, AMG-517	Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of pH 5 acid-induced calcium influx Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of pH 5 acid-induced calcium influx	[PMID: 18386885]
CHO	IC₅₀	0.62 nM Compound: 23	Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of acid-induced calcium influx Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of acid-induced calcium influx	[PMID: 17585750]
CHO	IC₅₀	0.76 nM Compound: 1	Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium mobilization Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium mobilization	[PMID: 18299195]
CHO	IC₅₀	0.76 nM Compound: 23	Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influx Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influx	[PMID: 17585750]
CHO	IC₅₀	0.9 nM Compound: 1, AMG-517	Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced 45Ca2+ influx by FLIPR assay Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced 45Ca2+ influx by FLIPR assay	[PMID: 18722118]
CHO	IC₅₀	0.9 nM Compound: 1	Antagonist activity at rat TRPV1 expressed in CHO cells assessed inhibition of capsaicin induced calcium influx Antagonist activity at rat TRPV1 expressed in CHO cells assessed inhibition of capsaicin induced calcium influx	[PMID: 17937985]
CHO	IC₅₀	0.9 nM Compound: 1	Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium mobilization Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium mobilization	[PMID: 18299195]
CHO	IC₅₀	0.9 nM Compound: 1, AMG-517	Inhibition of rat TRPV1 expressed in CHO cells assessed as capsaicin-induced Ca2+ influx Inhibition of rat TRPV1 expressed in CHO cells assessed as capsaicin-induced Ca2+ influx	[PMID: 17585751]
CHO	IC₅₀	0.9 nM Compound: 23	Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influx Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influx	[PMID: 17585750]
CHO	IC₅₀	0.9 nM Compound: 3, AMG-517	Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influx Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influx	[PMID: 18386885]
CHO	IC₅₀	1.3 nM Compound: 23	Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of heat-induced calcium influx Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of heat-induced calcium influx	[PMID: 17585750]

In Vitro

AMG 517 retains potency in the capsaicin- and acid-mediated assays with IC₅₀ values of 0.9 and 0.5 nM^[1]. AMG 517 inhibits capsaicin, pH 5, and heat-induced⁴⁵Ca²⁺ uptake into cells expressing TRPV1 with IC₅₀ values of 1 to 2 nM. AMG 517 blocks capsaicin-, proton-, and heat-induced inward currents in TRPV1-expressing cells similarly. AMG 517 inhibits native TRPV1 activation by capsaicin in rat dorsal root ganglion neurons with an IC50 value of 0.68 ± 0.2 nM. AMG 517 is a competitive antagonist of both rat and human TRPV1 with dissociation constant (Kb) values of 4.2 and 6.2 nM, respectively^[2].

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

In Vivo

AMG 517 is shown to be effective in a rodent "on-target" biochemical challenge model (capsaicin-induced flinch, ED₅₀=0.33 mg/kg p.o.) and is antihyperalgesic in a model of inflammatory pain (CFA-induced thermal hyperalgesia, MED=0.83 mg/kg, p.o.)^[1].The minimally effective dose is 0.3 mg/kg for AMG 517 and the corresponding plasma concentration is 90 ng/mL. Oral administration of AMG 517 reverses established thermal hyperalgesia in a dose-dependent manner at 21 h after CFA injection. AMG 517 causes transient hyperthermia in rodents, dogs, and monkeys. AMG 517 induces hyperthermia in a steep dose-dependent manner, with 0.3, 1, and 3 mg/kg associated with 0.5, 0.6, and 1.6°C increases in body temperature, respectively. Body temperatures of rats treated with all doses of AMG 517 return to baseline within 10 to 20 h^[2].

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

Chemical Information

CAS. Nr. 659730-32-2
Appearance Solid
Molecular Weight 430.40
Formel C₂₀H₁₃F₃N₄O₂S
Color White to off-white
SMILES

CC(NC1=NC2=C(OC3=NC=NC(C4=CC=C(C(F)(F)F)C=C4)=C3)C=CC=C2S1)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (6)

All In Vivo Efficacy StudyOthers

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Journal Impact Factor

Neuron

TRPV1 analgesics disturb core body temperature via a biased allosteric mechanism involving conformations distinct from that for nociception. [Abstract]

2024 Jun 5;112(11):1815-1831.e4. PMID: 38492574

AMG 517 purchased from MedChemExpress. Usage Cited in: Neuron. 2024 Jun 5;112(11):1815-1831.e4. [Abstract]

Rectal temperature measurements on Trpv1+/+ and Trpv1−/− mice at the specified time points following intraperitoneal injections of 5 mg/kg AMG517.
Int J Biol Macromol

Born with Silurian global warming: Defensive role of TRPV1 in caudal neurosecretory system (CNSS) in flounder. [Abstract]

2025 May 9:144092. PMID: 40350111
EMBO Rep

TRPA1 and TRPV1 contribute to iodine antiseptics-associated pain and allergy. [Abstract]

2016 Oct;17(10):1422-1430. PMID: 27566753

AMG 517 purchased from MedChemExpress. Usage Cited in: EMBO Rep. 2016 Oct;17(10):1422-1430. [Abstract]

Quantification of the nociceptive responses in TRPA1−/− mice within 5 min after intraplantar injection of control saline or 1,000 ppm iodine, following intraperitoneal injection of AMG517 (3 mg/kg) or vehicle.
Front Pharmacol

Ca2+-Permeable Channels/Ca2+ Signaling in the Regulation of Ileal Na+/Gln Co-Transport in Mice. [Abstract]

2022 Feb 23;13:816133. PMID: 35281933

AMG 517 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2022 Feb 23;13:816133. [Abstract]

Serosal application of AMG 517 (100 µM), a selective blocker of TRPV1 channels, significantly attenuated ileal Gln-I sc.
Biophys J

Full-Spectral Multiplexing of Bioluminescence Resonance Energy Transfer in Three TRPV Channels. [Abstract]

2017 Jan 10;112(1):87-98. PMID: 28076819

AMG 517 purchased from MedChemExpress. Usage Cited in: Biophys J. 2017 Jan 10;112(1):87-98. [Abstract]

In HEK293T cells expressing the YFP-TRPV1-Luc BRET probe, the dose-response curve of CAPS-induced BRET changes was measured. Cells were pre-incubated with PBS, DMSO (solvent), 1 μM CPZ, or 1 μM AMG517 before CAPS activation.
Pain Res Manag

Exploring the Analgesic Initiation Mechanism of Tuina in the Dorsal Root Ganglion of Minor CCI Rats via the TRPV1/TRPA1-cGMP Pathway. [Abstract]

2024 Jul 24:2024:2437396. PMID: 39104725

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 41.67 mg/mL (96.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3234 mL

11.6171 mL

23.2342 mL

5 mM

0.4647 mL

2.3234 mL

4.6468 mL

10 mM

0.2323 mL

1.1617 mL

2.3234 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

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

Solubility: ≥ 2.5 mg/mL (5.81 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (5.81 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Animal Administration^[2]

Rats: After multiple days of full habituation to the testing equipment and paradigm, CFA-induced thermal hyperalgesia is evaluated by measuring paw withdrawal latencies in male Sprague-Dawley rats. Twenty-one hours after CFA injection (50 μL of 0.1%), animals are dosed (p.o.) with AMG 517 or AMG8163 at a dose range of 0.001 to 30 mg/kg in a volume of 5 mL/kg. Two hours after drug dosing (23 h after CFA injection), paw withdrawal latencies are measured using modified Hargreaves hot boxes by investigators fully blinded to treatment conditions^[2].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Doherty EM, et al. Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. J Med Chem. 2007 Jul 26;50(15):3515-27. [Content Brief]

[2]. Gavva NR, et al. Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade. J Pharmacol Exp Ther. 2007 Oct;323(1):128-37. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3234 mL	11.6171 mL	23.2342 mL	58.0855 mL
	5 mM	0.4647 mL	2.3234 mL	4.6468 mL	11.6171 mL
	10 mM	0.2323 mL	1.1617 mL	2.3234 mL	5.8086 mL
	15 mM	0.1549 mL	0.7745 mL	1.5489 mL	3.8724 mL
	20 mM	0.1162 mL	0.5809 mL	1.1617 mL	2.9043 mL
	25 mM	0.0929 mL	0.4647 mL	0.9294 mL	2.3234 mL
	30 mM	0.0774 mL	0.3872 mL	0.7745 mL	1.9362 mL
	40 mM	0.0581 mL	0.2904 mL	0.5809 mL	1.4521 mL
	50 mM	0.0465 mL	0.2323 mL	0.4647 mL	1.1617 mL
	60 mM	0.0387 mL	0.1936 mL	0.3872 mL	0.9681 mL
	80 mM	0.0290 mL	0.1452 mL	0.2904 mL	0.7261 mL

Keywords

AMG 517

6 Cited Publications

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AMG 517

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Clinical Compound Library

Mechanoreceptors Compound Library

Human Metabolite Library

Heterocyclic Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) AMG 517

Alle TRP Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AMG 517

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Clinical Compound Library

Mechanoreceptors Compound Library

Human Metabolite Library

Heterocyclic Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) AMG 517

Alle TRP Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AMG 517 Related Classifications

HY-10634 Related Classifications