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AMG-517

Cat. No. M2383
AMG-517 Structure
Size Price Availability Quantity
5mg USD 115  USD115 In stock
10mg USD 170  USD170 In stock
25mg USD 380  USD380 In stock
50mg USD 620  USD620 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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

Customer Product Validations & Biological Datas
Source Bioanalysis (2014). Figure 2. AMG-517
Method PK analysis
Cell Lines Male CD-1 mice
Concentrations 1 mg/kg
Incubation Time 48 h
Results AMG 517 plasma concentration–time profiles for both collection techniques were superimposable
Source Bioanalysis (2014). Figure 1. AMG-517
Method PK analysis
Cell Lines Male CD-1 mice
Concentrations 1 mg/kg
Incubation Time 48 h
Results Following sample extraction and LC–MS/MS analysis to determine the AMG 517 concentrations, the concentration–time profiles from manual DBS and whole blood were nearly indistinguishable
Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
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)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 430.4
Formula C20H13F3N4O2S
CAS Number 659730-32-2
Purity >98%
Solubility DMSO 68 mg/mL
Storage at -20°C
References

[1] Gao P, et al. J Pharm Sci. Characterization and optimization of AMG 517 supersaturatable self-emulsifying drug delivery system (S-SEDDS) for improved oral absorption.

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Keywords: AMG-517 supplier, TRP Channel, inhibitors

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