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Bulevirtide, also known by its developmental code name Myrcludex B, is a synthetic lipopeptide inhibitor of the sodium taurocholate cotransporting polypeptide (NTCP) that effectively inhibits the cellular entry of both hepatitis B virus (HBV) and hepatitis D virus (HDV) into hepatocytes, even in cases of compensated cirrhosis, showing significant potential for the treatment of chronic hepatitis D.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $499 | In Stock |
Description | Bulevirtide, also known by its developmental code name Myrcludex B, is a synthetic lipopeptide inhibitor of the sodium taurocholate cotransporting polypeptide (NTCP) that effectively inhibits the cellular entry of both hepatitis B virus (HBV) and hepatitis D virus (HDV) into hepatocytes, even in cases of compensated cirrhosis, showing significant potential for the treatment of chronic hepatitis D. |
Targets&IC50 | NTCP:∼80 pM |
In vitro | Bulevirtide (2 μM, 9 days) treatment of Huh7-NTCP cells exhibits antiviral activity by inhibiting viral replication and blocking NTCP-mediated upregulation of HBV replication in Huh7-NTCP cells.[3] |
In vivo | Methods: Bulevirtide (2.5 mg/kg, subcutaneous injection, 100 mg/kg) was administered to OATP1a/1b-deficient mice to investigate the plasma bile acid dynamics after Bulevirtide inhibited NTCP. Results: Peak plasma bile salt concentrations were achieved 4 hours after Bulevirtide administration (Figure 1A), at which time most Bulevirtide had been cleared from the circulation. [2] |
Synonyms | Myrcludex B, MyrB |
Molecular Weight | 5398.86 |
Formula | C248H355N65O72 |
Cas No. | 2012558-47-1 |
Smiles | NC(CNC([C@@H](NC([C@@H](NC([C@@H](NC([C@H](C)NC([C@@H](NC([C@@H]1CCCN1C([C@H](CC2=CNC3=C2C=CC=C3)NC([C@H](CC4=CN=CN4)NC([C@H](CC(O)=O)NC([C@@H](NC([C@@H](NC([C@@H]5CCCN5C([C@@H](NC([C@H](CC6=CC=CC=C6)NC([C@H](CC(O)=O)NC([C@H](CC7=CNC8=C7C=CC=C8)NC([C@H](CC(O)=O)NC([C@@H]9CCCN9C([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@H](C)NC(CNC([C@H](CC%10=CC=CC=C%10)NC([C@H](C)NC([C@@H]%11CCCN%11C([C@H](CC(O)=O)NC([C@@H](NC([C@@H](NC([C@H](CC%12=CN=CN%12)NC([C@H](CC(O)=O)NC([C@@H]%13CCCN%13C([C@H](CC%14=CC=CC=C%14)NC([C@H](CC%15=CC=CC=C%15)NC(CNC([C@@H](NC([C@@H]%16CCCN%16C([C@@H](NC([C@@H]%17CCCN%17C([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@]([H])(NC(CNC(CCCCCCCCCCCCC)=O)=O)[C@H](O)C)=O)CC(N)=O)=O)CC(C)C)=O)CO)=O)C(C)C)=O)=O)CC(N)=O)=O)=O)CC(C)C)=O)=O)=O)=O)=O)=O)=O)CCC(N)=O)=O)CC(C)C)=O)=O)=O)=O)=O)=O)=O)CC(N)=O)=O)CO)=O)CC(N)=O)=O)CC(N)=O)=O)=O)=O)=O)=O)=O)CC(N)=O)=O)=O)CC(N)=O)=O)CCCCN)=O)=O)=O)=O)=O)CCC(O)=O)=O)=O)CC(N)=O)=O)CCCCN)=O)C(C)C)=O)=O |
Sequence | {Myr}-Gly-Thr-Asn-Leu-Ser-Val-Pro-Asn-Pro-Leu-Gly-Phe-Phe-Pro-Asp-His-Gln-Leu-Asp-Pro-Ala-Phe-Gly-Ala-Asn-Ser-Asn-Asn-Pro-Asp-Trp-Asp-Phe-Asn-Pro-Asn-Lys-Asp-His-Trp-Pro-Glu-Ala-Asn-Lys-Val-Gly-NH2 |
Sequence Short | {Myr}-GTNLSVPNPLGFFPDHQLDPAFGANSNNPDWDFNPNKDHWPEANKVG-NH2 |
Storage | keep away from moisture,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
Solubility Information | H2O: 65 mg/mL (12.04 mM), when pH is adjusted to 8 with NH3·H2O. Sonication is recommended. DMSO: 40 mg/mL (7.41 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO/H2O
H2O
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