| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| Targets |
cccDNA
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|---|---|
| ln Vitro |
In HepDES19 cells, ccc_R08 (0.3, 1.0, 3.2, 10, 32 µM; 5 days) dramatically lowers the levels of cccDNA, protein-free RC-DNA, and double stranded linear DNA (DL-DNA)[1]. The amount of extracellular HBeAg from HepDES19 cells is dose-dependently reduced by ccc_R08 (0 -100 µM), with an IC50 of ~0.1 µM[1].
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| ln Vivo |
In HBVcircle mice, ccc_R08 (20 mg/kg; po; twice daily for 2 weeks) removes cccDNA from the liver[1]. The serum level of pgRNA is significantly reduced by ccc_R08 (10, 15, 20, 30 mg/kg; po; twice daily for 2 weeks), and at different doses, there is a quantitative correlation between the reduction in pgRNA and that in liver cccDNA[1].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: HepDES19 cells Tested Concentrations: 0.3, 1.0, 3.2, 10, 32 µM Incubation Duration: 5 days Experimental Results: decreased the level of cccDNA, protein-free RC-DNA, and double stranded linear DNA (DL-DNA ). |
| Animal Protocol |
Animal/Disease Models: HBVcircle mouse model [1].
Doses: 20 mg/kg Route of Administration: Oral administration; twice per day for 2 weeks Experimental Results: Led to the clearance of cccDNA from HBVcircle mouse livers. Animal/Disease Models: HBVcircle mouse model [1] . Doses: 10, 15, 20, 30 mg/kg Route of Administration: Oral administration; twice per day for 42 days Experimental Results: Led to a sustained reduction in the serum levels of pgRNA. |
| References |
[1]. Wang L, et al. Discovery of a first-in-class orally available HBV cccDNA inhibitor. J Hepatol. 2022 Dec 29:S0168-8278(22)03466-3.
[2]. Ligat G, et al. Targeting Viral cccDNA for Cure of Chronic Hepatitis B. Curr Hepatol Rep. 2020 Sep;19(3):235-244. |
| Molecular Formula |
C22H19CLO6
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|---|---|
| Molecular Weight |
414.84
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| Exact Mass |
414.09
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| CAS # |
2919019-72-8
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| Related CAS # |
trans-ccc_R08;2413192-49-9;cis-ccc_R08;2413192-48-8
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| Appearance |
Powder
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| SMILES |
C1C(CC1OCCOC2=CC=C(C=C2)C3=CC(=O)C4=C(O3)C(=CC=C4)Cl)C(=O)O
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| InChi Key |
JFCQXBCQZCBQSI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H19ClO6/c23-18-3-1-2-17-19(24)12-20(29-21(17)18)13-4-6-15(7-5-13)27-8-9-28-16-10-14(11-16)22(25)26/h1-7,12,14,16H,8-11H2,(H,25,26)
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| Chemical Name |
3-[2-[4-(8-chloro-4-oxochromen-2-yl)phenoxy]ethoxy]cyclobutane-1-carboxylic acid
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| Synonyms |
ccc_R08
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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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 (~241.1 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.03 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. Solubility in Formulation 2: 2.5 mg/mL (6.03 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 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: 2.5 mg/mL (6.03 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4106 mL | 12.0528 mL | 24.1057 mL | |
| 5 mM | 0.4821 mL | 2.4106 mL | 4.8211 mL | |
| 10 mM | 0.2411 mL | 1.2053 mL | 2.4106 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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