| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| Targets |
EC50: 5-28 nM (HCV)[1] EC90: 0.47 μM (SARS-CoV-2)[2]
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|---|---|
| ln Vitro |
Bemnifosbuvir exhibits pan-genotypic antiviral activities: it inhibits the replication of HCV genotype 1a (HCV GT1a), HCV GT1b, HCV GT2a, HCV GT3a, HCV GT4a, and HCV GT5a with EC50 values of 12.8 nM, 12.5 nM, 9.2 nM, 10.3 nM, 14.7 nM, and 28.5 nM, respectively[1]. The dose of Bemnifosbuvir needed to prevent SARS-CoV-2 replication via EC90 in normal human airway epithelial cells is 0.47 μM, which is comparable to the concentration of EC90 needed to prevent HCoV-229E, HCoV-OC43, and SARS-CoV in Huh-7 cells[2].
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| ln Vivo |
Bemnifosbuvir preferentially delivers high amounts of AT-9010 in the liver in vivo when given orally to rats (500 mg/kg) and monkeys (30 mg/kg, 100 mg/kg, or 300 mg/kg)[1].
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| References |
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| Additional Infomation |
Bemnifosbuvir is an orally bioavailable direct-acting antiviral and purine nucleotide prodrug, with potential antiviral activity against a variety of RNA viruses. Upon oral administration, bemnifosbuvir, being a prodrug, is metabolized into its active form. The active form inhibits the activity of viral RNA-dependent RNA polymerase. This results in the termination of viral RNA transcription, decreases viral RNA production and inhibits viral RNA replication.
Mechanism of Action AT-527 is a prodrug of a guanosine nucleotide analog which has the potential to potently inhibit the in vitro replication of SARS-CoV-2. It also inhibits the NS5B polymerase in the Hepatitis C Virus. This drug is currently being investigated against COVID-19 and has also been investigated against Hepatitis C infections. |
| Molecular Formula |
C24H33FN7O7P
|
|---|---|
| Molecular Weight |
581.533689260483
|
| Exact Mass |
581.216
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| CAS # |
1998705-64-8
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| Related CAS # |
Bemnifosbuvir hemisulfate;2241337-84-6;HCV-IN-31;1998705-62-6
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| PubChem CID |
122527275
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
1.7
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
14
|
| Rotatable Bond Count |
12
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| Heavy Atom Count |
40
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| Complexity |
919
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| Defined Atom Stereocenter Count |
6
|
| SMILES |
P(N[C@H](C(=O)OC(C)C)C)(=O)(OC1C=CC=CC=1)OC[C@@H]1[C@H]([C@](C)(C(N2C=NC3C(NC)=NC(N)=NC2=3)O1)F)O
|
| InChi Key |
OISLSHLAXHALQZ-LZEIJKKFSA-N
|
| InChi Code |
InChI=1S/C24H33FN7O7P/c1-13(2)37-21(34)14(3)31-40(35,39-15-9-7-6-8-10-15)36-11-16-18(33)24(4,25)22(38-16)32-12-28-17-19(27-5)29-23(26)30-20(17)32/h6-10,12-14,16,18,22,33H,11H2,1-5H3,(H,31,35)(H3,26,27,29,30)/t14-,16+,18+,22+,24+,40-/m0/s1
|
| Chemical Name |
propan-2-yl (2S)-2-[[[(2R,3R,4R,5R)-5-[2-amino-6-(methylamino)purin-9-yl]-4-fluoro-3-hydroxy-4-methyloxolan-2-yl]methoxy-phenoxyphosphoryl]amino]propanoate
|
| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 200 mg/mL (343.92 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.30 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.30 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7196 mL | 8.5980 mL | 17.1960 mL | |
| 5 mM | 0.3439 mL | 1.7196 mL | 3.4392 mL | |
| 10 mM | 0.1720 mL | 0.8598 mL | 1.7196 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
A Phase 2 Study Assessing the Safety and Efficacy of AT-527 in Combination with Daclatasvir in Subjects with Chronic HCV Infection
CTID: null
Phase: Phase 2 Status: Completed
Date: 2019-05-20
Products are for research use only; We do not sell to patients
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