Mpro inhibitor N3

Names

[ CAS No. ]:
884650-98-0

[ Name ]:
Mpro inhibitor N3

[Synonym ]:
N-[(5-Methyl-3-isoxazolyl)carbonyl]-L-alanyl-L-valyl-N-[(1S,2E)-4-oxo-1-[[(3S)-2-oxo-3-pyrrolidinyl]methyl]-4-(phenylmethoxy)-2-buten-1-yl]-L-leucinamide

Biological Activity

[Description]:

Mpro inhibitor N3 is a potent SARS-CoV-2 MPro inhibitor with an EC50 value of 16.77 µM. Mpro inhibitor N3 shows antiviral activities against HCoV-229E, FIPV, IBV and MHV-A59[1][2][3].

[Related Catalog]:

Research Areas >> Infection
Signaling Pathways >> Anti-infection >> SARS-CoV

[In Vitro]

Mpro inhibitor N3 (0-100 µM) 具有抗病毒活性,对 SARS-CoV-2 的 EC50 值为 16.77 µM[1]。 Mpro inhibitor N3 (0-50 µM; 14 h) 抑制病毒生长,对 HCoV-229E、FIPV 和 MHV-A59 的 IC50 值分别为 4、8.8、2.7 µM[2]。

[In Vivo]

Mpro inhibitor N3 (0-0.64 µM; 3, 6 h) 在鸡胚胎中表现出抗 IBV 的抗病毒活性[3]。 Animal Model: Chicken embryos[3] Dosage: 0-0.64 µM Administration: 3, 6 h with 100-EID50 titer of IBV M41 virus Result: Showed that N3 is able to penetrate cells to inhibit the replication of IBV viruses, probably at the beginning of infection, with the PD50 of 0.13 μmol for the 3-h group and 0.17 μmol for the 6-h group.

[References]

[1]. Jin Z, et al. Structure of Mpro from SARS-CoV-2 and discovery of its inhibitors. Nature. 2020 Jun;582(7811):289-293.  

[2]. Yang H, et al. Design of wide-spectrum inhibitors targeting coronavirus main proteases. PLoS Biol. 2005 Oct;3(10):e324.  

[3]. Xue X, et al. Structures of two coronavirus main proteases: implications for substrate binding and antiviral drug design. J Virol. 2008 Mar;82(5):2515-27.  

Chemical & Physical Properties

[ Density]:
1.192±0.06 g/cm3(Predicted)

[ Boiling Point ]:
990.8±65.0 °C(Predicted)

[ Molecular Formula ]:
C35H48N6O8

[ Molecular Weight ]:
680.8


Related Compounds