Catalog No.S7115

AMG 517 is a potent and selective TRPV1 antagonist, and antagonizes capsaicin, proton, and heat activation of TRPV1 with IC50 of 0.76 nM, 0.62 nM and 1.3 nM, respectively.

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AMG-517 Chemical Structure

AMG-517 Chemical Structure
Molecular Weight: 430.4

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Quality Control & MSDS

Product Information

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Product Description

Biological Activity

Description AMG 517 is a potent and selective TRPV1 antagonist, and antagonizes capsaicin, proton, and heat activation of TRPV1 with IC50 of 0.76 nM, 0.62 nM and 1.3 nM, respectively.
Targets TRPV1 [1]
IC50 1 nM-2 nM
In vitro AMG 517 inhibits CAP- (500 nM), acid- (pH 5.0), or heat-(45 °C) induced 45Ca2+ influx into human TRPV1-expressing CHO Cells with IC50 of 0.76 nM, 0.62 nM and 1.3 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 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. AMG 517 is a highly selective TRPV1 antagonist. The IC50 value for AMG 517 is >20 μM against 2-APB-activated TRPV2 and TRPV3, 4-αPDD-activated TRPV4, allyl isothiocyanate-activated TRPA1, and icilin-activated TRPM8 in cell-based assays that measure agonist-induced increases in intracellular calcium in CHO cells recombinantly expressing the appropriate TRP channel. [1]
In vivo Oral administration of AMG 517 produces a dose-dependent increase in plasma concentrations, it also produces a dose-dependent decrease in the number of flinches induced by capsaicin treatment. The minimally effective dose (MED), based on a statistically significant difference in number of flinches from the vehicle versus capsaicin-administered group, is 0.3 mg/kg for AMG 517. The corresponding plasma concentrations are 90 to 100 ng/mL for AMG 517. AMG 517 (3 mg/kg) exhibits significant reductions in capsaicin-induced flinch up to 24 h after dosing. AMG 517 blocks thermal hyperalgesia in CFA model of pain.[1] AMG 517 elicits hyperthermia in rodents, dogs and monkeys but not in TRPV1 knockout mice. Interestingly, hyperthermia evoked by TRPV1-selective antagonists is attenuated after repeated dosing of these antagonists to rats, dogs and monkeys, and TRPV1 knockout mice does not exhibit an impairment of thermoregulation.[2]
Features Does not activate TRPV1 at concentrations ≤40 μM (measured by 45Ca2+ uptake into TRPV1-expressing cells), indicating that it is not a partial agonist.

Protocol(Only for Reference)

Kinase Assay: [1]

Agonist-Induced 45Ca2+ Uptake Assay Two days before the assay, cells are seeded in Cytostar 96-well plates at a density of 20,000 cells/well. The activation of TRPV1 and TRPV2 is followed as a function of cellular uptake of radioactive calcium. Capsaicin (0.5 μM), pH 5, and heat (45°C) are used as agonists for TRPV1, and 2-APB (200 μM) is used as the agonist for TRPV2. All of the antagonist 45Ca2+ uptake assays are conducted as reported previously and had a final 45Ca2+ concentration of 10 μCi/ml. Radioactivity is measured using a MicroBeta Jet. Data are analyzed using GraphPad Prism 4.01.

Animal Study: [1]

Animal Models Male Sprague-Dawley rats
Formulation Ora-Plus-5% Tween 80
Dosages 0.003-3 mg/kg
Administration p.o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Gavva NR, et al. J Pharmacol Exp Ther, 2007, 323(1), 128-137.

[2] Gavva NR, et al. Pain, 2008, 136(1-2), 202-210.

Chemical Information

Download AMG-517 SDF
Molecular Weight (MW) 430.4


CAS No. 659730-32-2
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 86 mg/mL (199.81 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 10% Tween 80 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Acetamide, N-[4-[[6-[4-(trifluoromethyl)phenyl]-4-pyrimidinyl]oxy]-2-benzothiazolyl]-

Tech Support

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