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HCoV-229E-IN-1 2639757-13-2

HCoV-229E-IN-1 2639757-13-2

CAS No.: 2639757-13-2

HCoV-229E-IN-1 is a potent inhibitor of HCoV-229E replication, with EC50s of 0.65 μM and 0.6 μM in MTS and CPE cells,
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HCoV-229E-IN-1 is a potent inhibitor of HCoV-229E replication, with EC50s of 0.65 μM and 0.6 μM in MTS and CPE cells, respectively.

Physicochemical Properties


CAS # 2639757-13-2
Appearance Off-white to light yellow solid powder
HS Tariff Code 2934.99.9001
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)

Biological Activity


Targets IC50: 0.65 μM (HCoV-229E)[1]
ln Vitro HCoV-229E-IN-1 (compound 5h) completely inhibits HCoV-229E replication potential in a dose-dependent manner, ranging from 0.01 to 100 μM[1]. The generation of dsRNA intermediates of CoV RNA synthesis is completely prevented by HCoV-229E-IN-1 (12 μM)[1].
References

[1]. Betulonic Acid Derivatives Interfering with Human Coronavirus 229E Replication via the nsp15 Endoribonuclease. J Med Chem. 2021 May 13;64(9):5632-5644.


Solubility Data


Solubility (In Vitro) DMSO : 12.5 mg/mL (21.41 mM)
Solubility (In Vivo) Solubility in Formulation 1: 1.67 mg/mL (2.86 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 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: ≥ 1.25 mg/mL (2.14 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 12.5 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.

Solubility in Formulation 3: ≥ 1.25 mg/mL (2.14 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 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)