AMG 21629

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Description: Potent and selective TRPV1 antagonist
Chemical Name: 3-Amino-5-[[2-[(2-methoxyethyl)amino]-6-[4-(trifluoromethyl)phenyl]-4-pyrimidinyl]oxy]-2(1H)-quinoxalinone
Purity: ≥97% (HPLC)

Biological Activity for AMG 21629

AMG 21629 is a potent and selective TRPV1 antagonist. Blocks Ca2+ uptake by CHO cells expressing TRPV1 receptors (IC50 values are 0.6 and 0.8 nM for capsaicin (Cat. No. 0462) and acid-induced Ca2+ uptake, respectively). Exhibits >4000-fold selectivity for TRPV1 over other TRP channels. Blocks capsaicin-induced flinch response and causes hyperthermia in rats. Orally available and non-CNS penetrant.

Technical Data for AMG 21629

M. Wt 472.42
Formula C22H19F3N6O3
Storage Store at -20°C
Purity ≥97% (HPLC)
CAS Number 939040-79-6
PubChem ID 24858024
Smiles NC(C(N4)=O)=NC(C4=CC=C3)=C3OC1=CC(C2=CC=C(C(F)(F)F)C=C2)=NC(NCCOC)=N1

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 21629

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 23.62 50

Preparing Stock Solutions for AMG 21629

The following data is based on the product molecular weight 472.42. 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
0.5 mM 4.23 mL 21.17 mL 42.34 mL
2.5 mM 0.85 mL 4.23 mL 8.47 mL
5 mM 0.42 mL 2.12 mL 4.23 mL
25 mM 0.08 mL 0.42 mL 0.85 mL

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References for AMG 21629

References are publications that support the biological activity of the product.

Tamayo et al (2008) Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists. J.Med.Chem. 51 2744 PMID: 18386885

Gavva et al (2007) The vanilloid receptor TRPV1 is tonically activated in vivo and involved in body temperature regulation. J.Neurosci. 27 3366 PMID: 17392452

If you know of a relevant reference for AMG 21629, please let us know.

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Keywords: AMG 21629, AMG 21629 supplier, AMG21629, transient, receptor, potential, vanilloid, TRPV1, antagonists, antagonism, orally, available, potent, selective, hyperthermia, TRPV, 4330, Tocris Bioscience

Citations for AMG 21629

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