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Purity: ≥98%
Remdesivir impurity x (GS-441524-intermediate), is a key and major intermediate chemical to synthesize antiviral drugs remdesivir and GS441524. Remdesivir (GS-5734; Veklury) is an FDA approved drug for the treatment of 2019-nCoV (COVID-19 pandemic, CoronaVirus) infections requiring hospitalization. Veklury (approved on Oct 22, 2020) is the first treatment for COVID-19 to receive FDA approval. It has EC50s of 74 nM for ARS-CoV and MERS-CoV in HAE cells, and 30 nM for murine hepatitis virus in delayed brain tumor cells. GS-5734 potently inhibits CoVs with intact proofreading. Following selection with the GS-5734 parent nucleoside, 2 amino acid substitutions in the nsp12 polymerase at residues that are identical across CoVs provide low-level resistance to GS-5734. The resistance mutations decrease viral fitness of MHV in vitro and attenuate pathogenesis in a SARS-CoV animal model of infection. Together, these studies define the target of GS-5734 activity and demonstrate that resistance is difficult to select, only partial, and impairs fitness and virulence of MHV and SARS-CoV, supporting further development of GS-5734 as a potential effective pan-CoV antiviral.
| Molecular Formula |
C33H31N5O4
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|---|---|
| Molecular Weight |
561.642
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| Exact Mass |
561.2376
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| Elemental Analysis |
C, 70.57; H, 5.56; N, 12.47; O, 11.39
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| CAS # |
1355357-49-1
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| SMILES |
N#C[C@@]1(C2=CC=C3C(N)=NC=NN32)O[C@H](COCC4=CC=CC=C4)[C@@H](OCC5=CC=CC=C5)
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| InChi Key |
PJXBLWLWNWGFJO-TXLSGFARSA-N
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| InChi Code |
InChI=1S/C33H31N5O4/c34-22-33(29-17-16-27-32(35)36-23-37-38(27)29)31(41-20-26-14-8-3-9-15-26)30(40-19-25-12-6-2-7-13-25)28(42-33)21-39-18-24-10-4-1-5-11-24/h1-17,23,28,30-31H,18-21H2,(H2,35,36,37)/t28-,30-,31-,33+/m1/s1
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| Chemical Name |
(2R,3R,4R,5R)-2-(4-Aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-3,4-bis(benzyloxy)-5-((benzyloxy)methyl)tetrahydrofuran-2-carbonitrile
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| Synonyms |
GS441524-intermediate GS 441524-intermediate GS-441524-intermediate remdesivir-intermediate Remdesivir related compound 5
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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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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7805 mL | 8.9025 mL | 17.8050 mL | |
| 5 mM | 0.3561 mL | 1.7805 mL | 3.5610 mL | |
| 10 mM | 0.1781 mL | 0.8903 mL | 1.7805 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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