AMG 517

Pricing Availability   Qty
Cat.No. 5995 - AMG 517 | C20H13F3N4O2S | CAS No. 659730-32-2
Description: Potent TRPV1 antagonist
Chemical Name: N-[4-[[6-[4-(Trifluoromethyl)phenyl]-4-pyrimidinyl]oxy]-2-benzothiazolyl]acetamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews (1)
Literature

Biological Activity

Potent TRPV1 antagonist (IC50 = 0.9 nM). Inhibits capsaican-induced flinching and reverses analgesia in an inflammatory pain model in rats. Orally bioavailable.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 43.04 100

Preparing Stock Solutions

The following data is based on the product molecular weight 430.41. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.32 mL 11.62 mL 23.23 mL
5 mM 0.46 mL 2.32 mL 4.65 mL
10 mM 0.23 mL 1.16 mL 2.32 mL
50 mM 0.05 mL 0.23 mL 0.46 mL

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References

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


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Citations for AMG 517

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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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Literature in this Area

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