| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| Other Sizes |
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Purity: ≥98%
Remdesivir O-desphosphate acetonide impurity is a Remdesivir impurity and an important intermediate to synthesize antiviral drug remdesivir. Remdesivir (GS-5734), an analogue of a nucleoside with potent antiviral activity, is very successful in suppressing SARS-CoV-2 (COVID-19) infection in vitro. An FDA-approved medication called Remdesivir (GS-5734; Veklury) is used to treat hospital-acquired 2019 COVID-19 pandemic infections caused by the coronavirus. Approved on October 22, 2020, Veklury is the first COVID-19 treatment to be approved by the FDA. For ARS-CoV and MERS-CoV in HAE cells, its EC50 values are 74 nM, while for the murine hepatitis virus in delayed brain tumor cells, they are 30 nM. Potently inhibiting CoVs with intact proofreading is GS-5734. The nsp12 polymerase has two amino acid substitutions at residues that are the same in all CoVs that provide low-level resistance to GS-5734 after selection with the GS-5734 parent nucleoside. Through attenuating pathogenesis in an animal model of infection with SARS-CoV, the resistance mutations reduce the viral fitness of MHV in vitro. When taken as a whole, these studies identify the target of GS-5734 activity, show that resistance is hard to choose, only partially effective, and reduces the fitness and virulence of MHV and SARS-CoV, all of which lend support to the idea that GS-5734 could be developed further and become a potent pan-offensive.
| ln Vitro |
GS-5734 demonstrates broad-spectrum antiviral activity against other pathogenic RNA viruses in vitro and antiviral activity against multiple EBOV variants in cell-based assays (EC50=0.06-0.14 μM).[1] With an EC50 of 0.03 μM for the murine hepatitis virus in delayed brain tumor cells and 0.074 μM for SARS-CoV and MERS-CoV in HAE cells, GS-5734 functions as a broad-spectrum therapeutic to protect against CoVs.[2]
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| ln Vivo |
The administration of 3 mg/kg GS-5734 results in improved survival regardless of the time at which the treatment is started. Following three days of viral exposure, all animals receiving 10 mg/kg GS-5734 treatments reach the end of their in-life phase. Animals given repeated doses of 10 mg/kg GS-5734, however, consistently exhibit stronger antiviral effects. Clinical disease signs and markers of coagulopathy and end organ pathophysiology related to EVD are associated with improvement when treated with the 10 mg/kg D3 regimen (starting 3 days after virus exposure).[1]
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| Cell Assay |
GS-5734 was applied to cells in different concentrations.
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| Animal Protocol |
Rhesus monkeys (Macaca mulatta)
3 mg/kg, 10 mg/kg IV |
| References |
| Molecular Formula |
C15H17N5O4
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|---|---|
| Molecular Weight |
331.326582670212
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| Exact Mass |
331.13
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| Elemental Analysis |
C, 54.38; H, 5.17; N, 21.14; O, 19.31
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| CAS # |
1191237-80-5
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| Related CAS # |
1911579-00-4; 1191237-80-5
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| PubChem CID |
58527338
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
-1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
24
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| Complexity |
565
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC1(O[C@@H]2[C@H](O[C@@]([C@@H]2O1)(C#N)C3=CC=C4N3N=CN=C4N)CO)C
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| InChi Key |
IJCOKJGMVJGKBB-CGEWXTDFSA-N
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| InChi Code |
InChI=1S/C15H17N5O4/c1-14(2)23-11-9(5-21)22-15(6-16,12(11)24-14)10-4-3-8-13(17)18-7-19-20(8)10/h3-4,7,9,11-12,21H,5H2,1-2H3,(H2,17,18,19)/t9-,11-,12-,15+/m1/s1
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| Chemical Name |
(3aR,4R,6R,6aR)-4-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-6-(hydroxymethyl)-2,2-dimethyl-6,6a-dihydro-3aH-furo[3,4-d][1,3]dioxole-4-carbonitrile
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| Synonyms |
Remdesivir related compound 7; Remdesivir-intermediate; ICN37805; ICN 37805; ICN-37805
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| 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 |
| 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: ~100 mg/mL (~301.8 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.55 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 (7.55 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 (7.55 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 | 3.0181 mL | 15.0907 mL | 30.1814 mL | |
| 5 mM | 0.6036 mL | 3.0181 mL | 6.0363 mL | |
| 10 mM | 0.3018 mL | 1.5091 mL | 3.0181 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.
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