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ln Vitro |
SARS-CoV-2-IN-34 (0.1-100 μM; 30 min) inhibits PsV infection of SARS variants on Huh-7 and Caco-2 cells with IC50 values ranging from 0.54 to 10.23 μM. It also inhibits infection of pseudotyped SARS-CoV, MERS-CoV, HCoV-229E, HCoV-NL63, and bat SARSr-CoV WIV1 with IC50 values ranging from 1.30 to 12.02 μM[1]. With an IC50 value of 8.14 μM, SARS-CoV-2-IN-34 (0.1-100 μM; 30 min) suppresses the replication of authentic SARS-CoV 2 on the Caco-2 cell line. It also inhibits the infection of RD cells and Huh-7 cells with HCoV-OC43 and HCoV-229E, respectively, with IC50 values of 6.25 and 9.46 μM [1]. With IC50 values ranging from 1.47 to 5.44 μM, SARS-CoV-2-IN-34 (0.1-100 μM; 2-4 h) effectively suppresses cell-cell fusion caused by S protein of SARS-CoV-2, SARS-CoV, MERS CoV, HCoV-229E, and HCoV-NL63[1]. Early viral entrance of SARS-CoV-2 infection is inhibited by SARS-CoV-2-IN-34 (50 μM; 1 h)[1]. With a Kd value of 67, 61, and 277 nM, respectively, SARS-CoV-2-IN-34(0-2 μM) exhibits binding actions to S1, RBD, and HR[1].
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ln Vivo |
SARS-CoV-2-IN-34 efficiently shields mice from infection when administered intraperitoneally at doses of 60 and 80 mg/kg, either 0.5 hours before or after the challenge with HCoV-OC43 and SARS-CoV-2 Delta[1]. Predicted to have potential oral bioavailability, SARS-CoV-2-IN-34 (50 mg/kg; ip and po once) exhibits good oral bioavailability and a better absorption rate under fed conditions.
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Cell Assay |
Cell Cytotoxicity Assay[1]
Cell Types: Huh-7, Caco-2 and RD cell lines Tested Concentrations: 0-1000 μM Incubation Duration: 12 hrs (hours) Experimental Results: demonstrated low on Huh-7, Caco-2 and RD cells with CC50s of >800, 692.7 and 274.2 μM, respectively. |
Animal Protocol |
Animal/Disease Models: C57BL/6 mice with HCoV-OC43 infection[1]
Doses: 80 mg/kg Route of Administration: Intranasal route; 80 mg/kg 0.5 h pre- or post-challenge with HCoV-OC43 Experimental Results: Dramatically diminished relative HCoV-OC43 RNA level of both prevention and treatment group . Animal/Disease Models: hACE2-transgenic C57BL/6 mice with SARS-CoV-2 Delta variant infection[1]. Doses: 60 mg/kg Route of Administration: Intranasal route; 60 mg/kg 0.5 h pre- or post-challenge with SARS- CoV-2 Delta Experimental Results: demonstrated prophylactic and therapeutic effect against SARS-CoV-2 Delta infection with intranasally administered. |
References |
[1]. Xue S, et al. A novel cyclic γ-AApeptide-based long-acting pan-coronavirus fusion inhibitor with potential oral bioavailability by targeting two sites in spike protein. Cell Discov. 2022 Sep 8;8(1):88.
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Molecular Formula |
C91H119N13O16S
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Molecular Weight |
1683.06
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 0.5942 mL | 2.9708 mL | 5.9416 mL | |
5 mM | 0.1188 mL | 0.5942 mL | 1.1883 mL | |
10 mM | 0.0594 mL | 0.2971 mL | 0.5942 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.