| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
CAB7-3 (0.001-1 μM, 6 days) showed antiviral activity in multiple cell models: in HepAD38 cells, EC50 = 1 nM, CC50 = 26.54 μM, SI = 26540; in HepDES19 cells, EC50 = 7 nM, CC50 = 32 μM, SI = 481; in HBV-infected HLCZ01 cells, EC50 = 2 nM, CC50 = 30.73 μM, SI = 15365[1]. CAB7-3 (0.0003-1 μM, 6 days) was able to block the formation of new cccDNA in HepAD38 and HLCZ01 cells without affecting the secretion of HBsAg produced by existing cccDNA[1]. CAB7-3 (0.006-4 μM, 3 days) can induce HBV core protein degradation and disrupt capsid assembly in HepG2 cells [1]. The metabolic stability parameters of CAB7-3 (1 μM, 0-60 min) in human liver microsomes are: half-life (T1/2) = 169 min, microsomal intrinsic clearance (CLint(mic)) = 8.2 μL/min/mg, liver intrinsic clearance (CLint(liver)) = 7.4 mL/min/kg, and residual amount after 60 min = 78.0% [1]. CAB7-3 (10 μM) does not induce CYP3A4 expression in human primary hepatocytes [1]. CAB7-3 (0.3-100 μM) showed significantly lower hERG channel inhibition rates in HEK293 cells expressing hERG channels: the inhibition rates at concentrations of 0.3, 1, 3, 10, 30 and 100 μM were 3.52%, 14.59%, 31.84%, 61.05%, 83.05% and 94.76%, respectively [1].
|
|---|---|
| ln Vivo |
CAB7-3 (head, 15 mg/kg, once daily for 18 days) inhibited the head of viral DNA in HBV wild animal models by inhibiting the HBV capsid[1].
|
| Cell Assay |
ELISA Assay[1]
Cell Types: HepAD38 and HLCZ01 cells Tested Concentrations: 0.0003, 0.001, 0.003, 0.1, 0.03, 0.1 and 0.3 μM Incubation Duration: 6 days Experimental Results: Had minimal impact on the production of HBsAg in both HepAD38 cells and HLCZ01 cells. Western Blot Analysis[1] Cell Types: HepG2 cells Tested Concentrations: 0.06, 0.13, 0.25, 0.5, 1.0, 2.0, 4.0 μM Incubation Duration: 3 days Experimental Results: Reduced intracellular Cp expression in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models: pAAVHBV1.2 plasmid (6 μg, hydrodynamic injection ) induced-male C57BL/6J (6 weeks)[1]
Doses: 15 mg/kg Route of Administration: p.o., once daily for 18 days Experimental Results: Significantly reduced serum HBV DNA levels from the vehicle baseline of 1.02 × 105 IU/mL to 1.06 × 104 IU/mL. Displayed enhanced anti-HBV activity, reducing hepatic HBcAg expression despite not noticeably affecting serum HBsAg expression. Showed no significant change in the Serum ALT and AST levels, as well as HE staining of liver tissue. |
| References |
| Molecular Formula |
C28H28BBRFN5O5S
|
|---|---|
| Molecular Weight |
656.33
|
| CAS # |
3014372-17-6
|
| Appearance |
Typically exists as solids at room temperature
|
| 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)
|
| 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
|
|---|---|
| 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 | 1.5236 mL | 7.6181 mL | 15.2362 mL | |
| 5 mM | 0.3047 mL | 1.5236 mL | 3.0472 mL | |
| 10 mM | 0.1524 mL | 0.7618 mL | 1.5236 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
