Name | AMG 21629 |
---|---|
Supplier | Tocris Bioscience |
Catalog | 4179 |
Prices | $345.00 |
Sizes | 1 mg |
Function Type | Antagonist |
Cas Number | 939040-79-6 |
Chemical Name | 3-Amino-5-[[2-[(2-methoxyethyl)amino]-6-[4-(trifluoromethyl)phenyl]-4-pyrimidinyl]oxy]-2(1H)-quinoxalinone |
Formula | C22H19F3N6O3 |
Molecular Weight | 472.42 |
Purity | >97 % |
Description | Potent and selective TRPV1 antagonist. Blocks Ca 2+ uptake by CHO cells expressing TRPV1 receptors (IC 50 values are 0.6 and 0.8 nM for capsaicin (Cat. No. 0462) and acid-induced Ca 2+ 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. |
Supplier Page | Shop |
Walser TC, Rifat S, Ma X, Kundu N, Ward C, Goloubeva O, Johnson MG, Medina JC, Collins TL, Fulton AM. Cancer Res. 2006 Aug 1;66(15):7701-7.
Johnson M, Li AR, Liu J, Fu Z, Zhu L, Miao S, Wang X, Xu Q, Huang A, Marcus A, Xu F, Ebsworth K, Sablan E, Danao J, Kumer J, Dairaghi D, Lawrence C, Sullivan T, Tonn G, Schall T, Collins T, Medina J. Bioorg Med Chem Lett. 2007 Jun 15;17(12):3339-43. Epub 2007 Apr 6.
Cambien B, Karimdjee BF, Richard-Fiardo P, Bziouech H, Barthel R, Millet MA, Martini V, Birnbaum D, Scoazec JY, Abello J, Al Saati T, Johnson MG, Sullivan TJ, Medina JC, Collins TL, Schmid-Alliana A, Schmid-Antomarchi H. Br J Cancer. 2009 Jun 2;100(11):1755-64.