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Submit ReviewAMG 517
Description: Potent TRPV1 antagonist
Chemical Name: N-[4-[[6-[4-(Trifluoromethyl)phenyl]-4-pyrimidinyl]oxy]-2-benzothiazolyl]acetamide
Purity: ≥98% (HPLC)
Biological Activity for AMG 517
AMG 517 is a potent TRPV1 antagonist (IC50 = 0.9 nM). Inhibits capsaican-induced flinching and reverses analgesia in an inflammatory pain model in rats. Orally bioavailable.
Compound Libraries for AMG 517
AMG 517 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for AMG 517
| M. Wt | 430.41 |
| Formula | C20H13F3N4O2S |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 659730-32-2 |
| PubChem ID | 16007367 |
| InChI Key | YUTIXVXZQIQWGY-UHFFFAOYSA-N |
| Smiles | O=C(NC(S1)=NC(C1=CC=C2)=C2OC3=NC=NC(C4=CC=C(C(F)(F)F)C=C4)=C3)C |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for AMG 517
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 4.3 | 10 |
Preparing Stock Solutions for AMG 517
The following data is based on the product molecular weight 430.41. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 23.23 mL | 116.17 mL | 232.34 mL |
| 0.5 mM | 4.65 mL | 23.23 mL | 46.47 mL |
| 1 mM | 2.32 mL | 11.62 mL | 23.23 mL |
| 5 mM | 0.46 mL | 2.32 mL | 4.65 mL |
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Product Datasheets for AMG 517
References for AMG 517
References are publications that support the biological activity of the product.
Gavva et al (2007) Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade. J.Pharmacol.Exp.Ther. 323 128 PMID: 17652633
Wang et al (2007) Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties. J.Med.Chem. 50 3528 PMID: 17585751
Doherty et al (2007) Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. J.Med.Chem. 50 3515 PMID: 17585750
If you know of a relevant reference for AMG 517, please let us know.
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Keywords: AMG 517, AMG 517 supplier, AMG517, potent, TRPV1, transient, potential, channels, antagonists, pain, antihyperalgesia, TRPV, 5995, Tocris Bioscience
Citations for AMG 517
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Reviews for AMG 517
Average Rating: 5 (Based on 1 Review.)
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AMG517 blocks TRPV1 function.
By
Anonymous on 01/10/2018
Assay Type: In Vivo
Species: Mouse
AMG517 was used to relieve SADBE-induced chronic itch in mice via inhibition of TRPV1 function.
AMG517 should be used at the dose of 30mg/kg in in vivo experiments
