1. Membrane Transporter/Ion Channel
  2. TRP Channel

AMG 517 

Cat. No.: HY-10634 Purity: 99.46%
Data Sheet SDS Handling Instructions

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

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AMG 517 Chemical Structure

AMG 517 Chemical Structure

CAS No. : 659730-32-2

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $131 In-stock
5 mg $119 In-stock
10 mg $165 In-stock
50 mg $570 In-stock
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Description

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]

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].

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].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
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.
Animal Administration
[2]

Rat: 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

430.4

Formula

C₂₀H₁₃F₃N₄O₂S

CAS No.

659730-32-2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 12.91 mg/mL (Need ultrasonic)

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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AMG 517
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HY-10634
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