| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
RdRp, RSV,SARS-CoV-2, HCV, COVID-19, LCMV[1][2][3].
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|---|---|
| ln Vitro |
EIDD-2749 causes RSV and SARS-CoV-2 RdRP to stop the synthesis of phosphodiester bonds later than expected[1]. In disease-relevant, well-differentiated HAE cells, EIDD-2749 is quickly anabolized, metabolically stable, and potently antiviral[1]. Compared to HEp-2 cells, EIDD-2749 has an anti-RSV potency that is approximately 17 times more potent. Despite this, the low cytotoxicity levels (CC50 169 mM) remain unchanged, resulting in a high SI (SI = EC50/CC50) of approximately 1877[1]. EIDD-2749 has an EC50 value between 0.2 and 0.6 M, which suppresses SARS-CoV-2[2]. EIDD-2749 exhibits stability in human plasma, cytotoxicity with a CC50 of 380 μM, and an EC50 of 1.86 μM in the Vero E6 cell line[3].
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| ln Vivo |
In an RSV infection mouse model, EIDD-2749 (0.2, 1, 5 mg/kg; po; once daily for 4 days) exhibits good oral efficacy in a dose-dependent manner[1]. In comparison to molnupiravir given twice daily in vivo, EIDD-2749 exhibits high efficacy against SARS-CoV-2 infection and can be delivered as a single daily dose[2].
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| Animal Protocol |
Animal/Disease Models: Balb/cJ mice (RSV infection model )[1].
Doses: 0.2, 1, 5 mg/kg Route of Administration: Oral administration; single daily for 4 days Experimental Results: Resulted in a statistically significant reduction in lung virus load. |
| References |
[1]. Sourimant J, et al. 4'-Fluorouridine is an oral antiviral that blocks respiratory syncytial virus and SARS-CoV-2 replication. Science. 2022 Jan 14;375(6577):161-167.
[2]. Abas AH, et al. 4’-fluorouridine and its derivatives as potential COVID-19 oral drugs: a review [version 1; peer review: 1 approved with reservations, 1 not approved]. F1000Research 2022, 11:410. [3]. George R. Painter, et al. 4'-halogen containing nucleotide and nucleoside therapeutic compositions and uses related thereto. Patent WO2019173602A1. |
| Molecular Formula |
C9H11FN2O6
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|---|---|
| Molecular Weight |
262.19
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| CAS # |
1613589-24-4
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| SMILES |
OC[C@@]1(F)O[C@@H](N2C=CC(=O)NC2=O)[C@H](O)[C@@H]1O
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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) |
H2O : 62.5 mg/mL (238.38 mM)
DMSO : 25 mg/mL (95.35 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 25 mg/mL (95.35 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 250.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.54 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.54 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. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8140 mL | 19.0701 mL | 38.1403 mL | |
| 5 mM | 0.7628 mL | 3.8140 mL | 7.6281 mL | |
| 10 mM | 0.3814 mL | 1.9070 mL | 3.8140 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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