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Chemical Structure| 659730-32-2 Chemical Structure| 659730-32-2

Structure of AMG 517
CAS No.: 659730-32-2

Chemical Structure| 659730-32-2

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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.

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Product Details of AMG 517

CAS No. :659730-32-2
Formula : C20H13F3N4O2S
M.W : 430.40
SMILES Code : CC(NC1=NC2=C(OC3=NC=NC(C4=CC=C(C(F)(F)F)C=C4)=C3)C=CC=C2S1)=O
MDL No. :MFCD14584859
InChI Key :YUTIXVXZQIQWGY-UHFFFAOYSA-N
Pubchem ID :16007367

Safety of AMG 517

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
C2C12 myotubes 1 μM 1 day TRPV1 inhibition weakened the increase in intracellular Ca2+ levels induced by eugenol, suggesting that eugenol acts via TRPV1. PMC11196110
DRG cells 1 μM 1 h AMG 517 inhibited PSM a3-induced SP release from DRG cells PMC11617324

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Wild-type and Trpv1 knockout mice Intraperitoneal injection 250 ng/kg Three injections, spaced 3 days apart To evaluate the effect of AMG517 on core body temperature, results showed that AMG517 elicited a characteristic hyperthermia in control animals, reaching a peak of ~0.5°C within 2 hr after injection, while this response was completely abolished in sensory neuron-specific knockout mice. PMC9377796
Rats Wistar rats Intravenous injection ≥16 nmol/kg Not specified AMG 517 caused dose-dependent hyperthermia at doses ≥16 nmol/kg, with a saturation of the response occurring at doses≥256 nmol/kg PMC2824913
Rats Sciatic nerve crush injury model Subcutaneous injection 300 µg/kg Single injection, observed for 1 and 2 weeks To investigate the effect of AMG517 on nerve regeneration after sciatic nerve injury. Results showed that AMG517 pretreatment significantly promoted nerve regeneration, reduced TRPV1 expression, and accelerated axon regeneration. PMC4590249
mice MRGPRX2-KI mice oral 20 mg single dose, lasting 7 minutes AMG 517 inhibited PSM a3-induced MRGPRX2-dependent vascular hyperpermeability PMC11617324

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.32mL

0.46mL

0.23mL

11.62mL

2.32mL

1.16mL

23.23mL

4.65mL

2.32mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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