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Tenofovir amibufenamide

Catalog No. T39043   CAS 1571076-26-0
Synonyms: HS-10234

Tenofovir amibufenamide (HS-10234) (HS-10234) is a Tenofovir prodrug, an antiviral compound with oral activity. Tenofovir amibufenamide inhibits hepatitis B virus (HBV) and can be used in chronic hepatitis B (CHB) studies.

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Tenofovir amibufenamide Chemical Structure
Tenofovir amibufenamide, CAS 1571076-26-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 293.00
5 mg In stock $ 719.00
10 mg In stock $ 987.00
25 mg In stock $ 1,490.00
50 mg In stock $ 1,980.00
100 mg In stock $ 2,750.00
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Purity: 99.86%
ee: 100%
Purity: 99.19%
ee: 100%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Tenofovir amibufenamide (HS-10234) (HS-10234) is a Tenofovir prodrug, an antiviral compound with oral activity. Tenofovir amibufenamide inhibits hepatitis B virus (HBV) and can be used in chronic hepatitis B (CHB) studies.
Targets&IC50 Anti-HBV:7.29 ± 0.71 nM(EC50)
In vitro TMF and TAF 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 TAF 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 > TAF > 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. [1]
In vivo Safety was evaluated thoroughly focusing on bone, renal, and metabolic parameters between TMF (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 TMF group than in the TDF group (p=0.01). For bone mineral density, patients receiving TMF 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. TMF maintained similar efficacy at week 96 compared with TDF with continued superior bone and renal safety profiles.[2]
Synonyms HS-10234
Molecular Weight 490.49
Formula C22H31N6O5P
CAS No. 1571076-26-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 180.0 mg/mL (367.0 mM), Sonification is recommended.

TargetMolReferences and Literature

1. Hong X, et al. Improved pharmacokinetics of tenofovir ester prodrugs strengthened the inhibition of HBV replication and the rebalance of hepatocellular metabolism in preclinical models. Front Pharmacol. 2022;13:932-934. 2. Liu Z, et al. Randomised clinical trial: 48 weeks of treatment with tenofovir amibufenamide versus tenofovir disoproxil fumarate for patients with chronic hepatitis B. Aliment Pharmacol Ther. 2021;54(9):1134-1149. 3. Zhihong Liu, et al. Randomised clinical trial: 48 weeks of treatment with tenofovir amibufenamide versus tenofovir disoproxil fumarate for patients with chronic hepatitis B. Aliment Pharmacol Ther. 2021 Nov;54(9):1134-1149. 4. Hong Zhang, et al. Randomised clinical trial: safety, efficacy and pharmacokinetics of HS-10234 versus tenofovir for the treatment of chronic hepatitis B infection. Aliment Pharmacol Ther. 2021 Jan;53(2):243-252.

Related compound libraries

This product is contained In the following compound libraries:
Drug Repurposing Compound Library FDA-Approved Drug Library Bioactive Compounds Library Max FDA-Approved & Pharmacopeia Drug Library Bioactive Compound Library Anti-Viral Compound Library Approved Drug Library

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Keywords

Tenofovir amibufenamide 1571076-26-0 Microbiology/Virology HBV HS10234 HS-10234 HS 10234 inhibitor inhibit

 

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