Agenerase Inhibitor CAS No. 161814-49-9

Cat. No.	Name	Size	Price	Add Cart
KI0855	Agenerase	250 mg	$784

Chemical Characteristic

Product Name	Agenerase
Synonyms	Vertex 478, 141W94, VX-478,amprenavir
CAS No.	161814-49-9
Molecular Weight	505.63
Formula	C₂₅H₃₅N₃O₆S
Chemical Structure

Biological activities

Agenerase is a highly stereoselective synthesis of the HIV protease inhibitor. The IC50 of agenerase ranges from 2.5 to 2.9 µM against HIV proteases. Pre-incubation of microsomes with agenerase increases inhibitory potency with an IC50 of 1.4µM.^[1]Agenerase blocks the catalytic activity of XMRV protease.^[2] Agenerase has 2-to 23-fold higher transport rates from the basolateral to apical direction than from the apical to basolateral direction across Caco-2 monolayers.^[3] Agenerase is highly bound to human plasma proteins (∼90%). Agenerase primarily binds to α1-acid glycoprotein (AAG) and albumin, with fractional binding of 89 and 42%, respectively.^[4] The clearance index of agenerase is 0.38 and 0.14 at peak and trough concentrations, respectively.^[5] Agenerase metabolism in rat liver microsomes is strongly inhibited by indinavir.^[6]

References

[1] von Moltke LL, et al. Potent mechanism-based inhibition of human CYP3A in vitro by amprenavir and ritonavir: comparison with ketoconazole. Eur J Clin Pharmacol. 2000, 56(3): 259-261. 閵嗏偓閵嗏偓 [2] Matsunaga S, et al. Molecular and enzymatic characterization of XMRV protease by a cell-free proteolytic analysis. J Proteomics. 2012, 75(15): 4863-4873. 閵嗏偓閵嗏偓 [3] Polli JW, et al.Role of P-glycoprotein on the CNS disposition of amprenavir (141W94), an HIV protease inhibitor. Pharm Res. 1999, 16(8): 1206-1212. 閵嗏偓閵嗏偓 [4] Sadler BM, et al. In vivo effect of α1-acid glycoprotein on pharmacokinetics of amprenavir, a human immunodeficiency virus protease inhibitor. Antimicrob Agents Chemother. 2001, 45(3): 852閳?56. 閵嗏偓閵嗏偓 [5] Bawdon RE. The ex vivo human placental transfer of the anti-HIV nucleoside inhibitor abacavir and the protease inhibitor amprenavir. Infect Dis Obstet Gynecol. 1998, 6(6): 244-246. 閵嗏偓閵嗏偓 [6] Shibata N, et al. In-vitro and in-vivo pharmacokinetic interactions of amprenavir, an HIV protease inhibitor, with other current HIV protease inhibitors in rats. J Pharm Pharmacol. 2002, 54(2): 221-229. 閵嗏偓閵嗏偓

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