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10mg |
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50mg |
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Purity: ≥98%
EIDD-1931 (EIDD1931; Beta-d-N4-hydroxycytidine; NHC) is a novel and potent ribonucleoside analog with antiviral activity. EIDD-1931 is an active metabolite of the UK-approved anti-COVID-19 drug Molnupiravir (EIDD2801; prodrug-EIDD1931; MK-4482; Lagevrio), thus has the potential to be used as an anti-COVID-19 drug. EIDD-1931 has a broad spectrum antiviral activity and can inhibit replication of severe acute respiratory syndrome coronavirus (SARS-CoV) in Vero 76 cells, Middle East respiratory syndrome coronavirus (MERS-CoV) in Calu-3 2B4 cells, and SARS-CoV-2 in Vero cells (IC 50 s =0.1, 0.15 and 0.3 μM, respectively. It has increased potency against a coronavirus bearing resistance mutations to the nucleoside analog inhibitor remdesivir.
ln Vitro |
The anti-VEEV (venezuelan equine encephalitis virus) agent beta-d-N4-hydroxycytidine has EC50, EC90, and EC99 values of 0.426, 1.036, and 2.5 μM, respectively[1].
In the Huh-7–CHIKV replicon cell line, beta-d-N4-hydroxycytidine inhibits CHIKV replicon activity and the 50% effective concentration (EC50) is 0.8 μM. Comparable outcomes have been reported regarding the replicon in BHK-21 cells (EC50=1.8 μM).According to MTT assays, NHC does not cause any cytotoxicity in the Huh-7 cell culture system up to 100 μM. For peripheral blood mononuclear (PBM), Vero, and CEM cells, the 50% cytotoxic concentration (CCsub>50) values for NHC are found to be 30.6 μM, 7.7 μM, and 2.5 μM, respectively.NHC functions as a pyrimidine analog; exogenous nucleosides, such as pyrimidines C and U, can reverse NHC-mediated inhibition of the CHIKV replicon; however, the replicon is unaffected by dA, dC, dG, dU, or T. Pyrimidines A and G have a role in replicon inhibition both with and without NHC [2]. |
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References |
Molecular Formula |
C9H13N3O6
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Molecular Weight |
259.21602
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Exact Mass |
259.08
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Elemental Analysis |
C, 41.70; H, 5.06; N, 16.21; O, 37.03
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CAS # |
3258-02-4
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Appearance |
Solid powder
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SMILES |
C1(N2C=C/C(=N\O)/NC2=O)OC(CO)C(O)C1O
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InChi Key |
XCUAIINAJCDIPM-XVFCMESISA-N
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InChi Code |
InChI=1S/C9H13N3O6/c13-3-4-6(14)7(15)8(18-4)12-2-1-5(11-17)10-9(12)16/h1-2,4,6-8,13-15,17H,3H2,(H,10,11,16)/t4-,6-,7-,8-/m1/s1
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Chemical Name |
N4-Hydroxycytidine
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Synonyms |
EIDD-1931; EIDD 1931; EIDD1931; N4-Hydroxycytidine; β-D-N4-hydroxycytidine; Uridine, 4-oxime; NHC; EIDD-2801-metabolite; Molnupiravir-,etabolite
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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 Note: This product is not stable in solution, please use freshly prepared working solution for optimal results. |
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 (~385.77 mM)
H2O : ≥ 25 mg/mL (~96.44 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.02 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 20.8 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: ≥ 2.08 mg/mL (8.02 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 20.8 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: ≥ 2.08 mg/mL (8.02 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 | 3.8577 mL | 19.2886 mL | 38.5773 mL | |
5 mM | 0.7715 mL | 3.8577 mL | 7.7155 mL | |
10 mM | 0.3858 mL | 1.9289 mL | 3.8577 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.
NHC has a strong negative effect on VEEV TC-83 replication. [1].J Virol. 2018 Jan 17;92(3). td> |
The antiviral effect of NHC depends on its application time. [1].J Virol. 2018 Jan 17;92(3). td> |
The first 4 h p.i. are a critical time for the antiviral effect of NHC. [1].J Virol. 2018 Jan 17;92(3). td> |
NHC is a potent anti-VEEV compound with low cytotoxicity. [1].J Virol. 2018 Jan 17;92(3). td> |
VEEV TC-83 accumulates a large number of mutations when exposed to NHC. [1].J Virol. 2018 Jan 17;92(3). td> |
NHC has stronger negative effects on the release and infectivity of VEEV TC-83 and PREV1 particles than those of the PP2 mutant. [1].J Virol. 2018 Jan 17;92(3). td> |
Drug-resistant VEEV isolate PP2 replicates more efficiently than parental VEEV TC-83 and pseudorevertant PREV1 in the presence, but not in the absence of NHC. [1].J Virol. 2018 Jan 17;92(3). td> |
VEEV TC-83 passaging in the presence of increasing concentrations of NHC leads to rapid accumulation of mutations in viral pool.[1].J Virol. 2018 Jan 17;92(3). td> |
The mutations that lead to NHC-resistant and NHC-sensitive phenotypes of VEEV TC-83 are closely located in the 3D structure of the catalytic domain of VEEV nsP4. [1].J Virol. 2018 Jan 17;92(3). td> |