Tenofovir amibufenamide

SKU: orb1691609

Description

Tenofovir amibufenamide (HS-10234) is an orally active prodrug of tenofovir, developed for chronic hepatitis B (CHB) research. It demonstrates potent antiviral activity against HBV in both in vitro and in vivo preclinical studies, supporting its investigation as a therapeutic candidate.

Research Area

Infectious Disease & Virology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1571076-26-0
• MW: 490.49
• Purity: 99.87% (May vary between batches)
• Formula: C₂₂H₃₁N₆O₅P
• SMILES: C([C@H](OCP(OC1=CC=CC=C1)(NC(C(OC(C)C)=O)(C)C)=O)C)N2C=3C(N=C2)=C(N)N=CN3
• Target: HBV
• Solubility: DMSO:180 mg/mL (366.98 mM)

Bioactivity

• Target IC50:
  Anti-HBV:7.29 ± 0.71 nM(EC50)
• In Vivo:
  Safety was evaluated thoroughly focusing on bone, renal, and metabolic parameters between Tenofovir amibufenamide (25 mg, for 96 weeks) and TDF group. Non-indexed estimated glomerular filtration rate for renal safety assessment was adopted, while a smaller decline of which was seen in the Tenofovir amibufenamide group than in the TDF group (p=0.01). For bone mineral density, patients receiving Tenofovir amibufenamide displayed significantly lower reduction levels in the densities of spine, hip, and femur neck at week 96 than those receiving TDF. In addition, the lipid parameters were stable after week 48 in all groups while weight change still showed the opposite trend. Tenofovir amibufenamide maintained similar efficacy at week 96 compared with TDF with continued superior bone and renal safety profiles.
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• In Vitro:
  TMF and Tenofovir amibufenamide exhibited significantly stronger inhibition of HBV DNA replication than did TDF in HBV-positive HepG2.2.15 cells. The anti-HBV activity of TMF was slightly stronger than Tenofovir amibufenamide after 9 days of treatment (EC50 7.29 ± 0.71 nM vs. 12.17 ± 0.56 nM). The callback effects of the three TFV ester prodrugs were ranked as TMF > Tenofovir amibufenamide > TDF. These advantages of TMF were believed to be attributed to its greater bioavailability in preclinical animals (SD rats, C57BL/6 mice and beagle dogs) and better target loading, especially in terms of the higher hepatic level of the pharmacologically active metabolite TFV-DP, which was tightly related to anti-HBV efficacy.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

HS10234, HS-10234, HS 10234, HBV, Tenofovir amibufenamide

Compound Identifiers

PubChem CID

73335908