Bulevirtide

• CAT Number: I042543
• CAS Number: 2012558-47-1
• Molecular Formula: C248H355N65O72
• Molecular Weight: 5398.86
• Purity: ≥95%

Bulevirtide (Myrcludex B) is a NTCP inhibitor, a linear lipopeptide of 47 amino acids. Bulevirtide inhibits HBV and HDV entry into liver cells, blocks HBV infection in hepatocytes, and participates in HBV transcriptional suppression. Bulevirtide can be used in HDV infection and compensated cirrhosis research[1][2].
Bulevirtide (200 nM, 24 h) inihibits NTCP through non-covalent binding in a time- and dose-dependent manner, transfer to a newly synthesized NTCP molecule[3].
Bulevirtide (Huh7-NTCP cells, 2 μM, 9 days) exhibits potential antiviral activity as replication inhibitor, which blocks upregulation of NTCP mediated-HBV replication in Huh7-NTCP cells [5].
Bulevirtide (2 μg/g, s.c. for everyday) prevents HBV spreading from infected human hepatocytes in uPA/SCID mice, hinders amplification of the cccDNA pool in initially infected hepatocytes[4].
Bulevirtide (2 μg/g/d, s.c. for 3 weeks) blocks HBV cell entry in uPA/SCID mice through addressing the hepatocyte component rather than affecting virion productivity within the infected hepatocyte or the half-life of these cells[4].
Bulevirtide (5 μg,s.c., twice a day for 4 days) blocks upregulation of NTCP mediated-HBV replication in C57BL/6 mice as a replication inhibitor[5].

Reference

[1]. Masetti C, et al. Bulevirtide for treatment of patients with HDV infection and compensated cirrhosis: A (huge?) step in the right direction. Liver Int. 2021 Jul;41(7):1441-1442.
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[2]. Cheng D, et al. Clinical effects of NTCP-inhibitor myrcludex B. J Viral Hepat. 2021 Jun;28(6):852-858.
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[3]. Donkers JM, et al., Mechanistic insights into the inhibition of NTCP by myrcludex B. JHEP Rep. 2019 Aug 1;1(4):278-285.
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[4]. Volz T, et al., The entry inhibitor Myrcludex-B efficiently blocks intrahepatic virus spreading in humanized mice previously infected with hepatitis B virus. J Hepatol. 2013 May;58(5):861-7.
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[5]. Zhao K, et al., Upregulation of HBV transcription by sodium taurocholate cotransporting polypeptide at the postentry step is inhibited by the entry inhibitor Myrcludex B. Emerg Microbes Infect. 2018 Nov 21;7(1):186.
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