AMG 21629

Pricing Availability Delivery Time Qty
Cat.No. 4330 - AMG 21629 | C22H19F3N6O3 | CAS No. 939040-79-6
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

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

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 472.42. 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 2.12 mL 10.58 mL 21.17 mL
5 mM 0.42 mL 2.12 mL 4.23 mL
10 mM 0.21 mL 1.06 mL 2.12 mL
50 mM 0.04 mL 0.21 mL 0.42 mL

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Product Datasheets

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References are publications that support the products' biological activity.

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

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

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