AMG 517

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Description: Potent TRPV1 antagonist
Chemical Name: N-[4-[[6-[4-(Trifluoromethyl)phenyl]-4-pyrimidinyl]oxy]-2-benzothiazolyl]acetamide
Purity: ≥98% (HPLC)
Reviews (1)

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
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
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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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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Currently there are no citations for AMG 517. Do you know of a great paper that uses AMG 517 from Tocris? Please let us know.

Reviews for AMG 517

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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

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