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AMG21629

Chemical Structure : AMG21629

CAS No.: 939040-79-6

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AMG21629 (AMG-21629)

Catalog No.: PC-49443Not For Human Use, Lab Use Only.

AMG21629 is a potent and selective TRPV1 antagonist, inhibits Ca2+ uptake by CHO cells expressing TRPV1 receptors with IC50 of 0.6 nM and 0.8 nM for capsaicin and acid-induced Ca2+ uptake, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

AMG21629 is a potent and selective TRPV1 antagonist, inhibits Ca2+ uptake by CHO cells expressing TRPV1 receptors with IC50 of 0.6 nM and 0.8 nM for capsaicin and acid-induced Ca2+ uptake, respectively.
AMG21629 displayss >4000-fold selectivity for TRPV1 over other TRP channels.
AMG21629 blocks capsaicin-induced flinch response and causes hyperthermia in rats.

Physicochemical Properties

M.Wt 472.428
Formula C22H19F3N6O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

3-Amino-5-[[2-[(2-methoxyethyl)amino]-6-[4-(trifluoromethyl)phenyl]-4-pyrimidinyl]oxy]-2(1H)-quinoxalinone

References

1. Nuria Tamayo, et al. J Med Chem. 2008 May 8;51(9):2744-57.

2. Matthew I Brier, et al. Sci Rep. 2020 Aug 4;10(1):13096.

3. Narender R Gavva, et al. J Neurosci. 2007 Mar 28;27(13):3366-74.

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