| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
(Rac)-Adibelivir (Example 7) inhibits the replication of wild-type HSV-1, HSV-2 and ACV-resistant HSV-1 in Vero cells [1].
|
|---|---|
| ln Vivo |
(Rac)-Adibelivir (Example C7) (2-10 mg/kg; oral, intravenous; single dose) enantiomer Example 4/2 showed 201% oral bioavailability and 188 mL/(h*kg) systemic clearance in male C57Bl/6N mice [1]. (Rac)-Adibelivir (10 mg/kg; oral; single dose) enantiomer Example 4/2 achieved a brain-to-plasma ratio of 1.57 after oral administration in mice, with both plasma and brain exposures improved compared to the non-deuterated matched pair [1].
|
| Cell Assay |
Cell viability assay [1]
Cell Types: Vero cells Tested Concentrations: IC50 Incubation Duration: / Experimental Results: In Vero cells, the replication of wild-type HSV-1, HSV-2 and ACV-resistant HSV-1 was inhibited, with IC50 values of 25-100 nM, 25-100 nM and 25-100 nM, respectively. |
| Animal Protocol |
Animal/Disease Models:C57Bl/6N mice (male, 21-25 g)[1]
Doses: 10 mg/kg (oral); 2 mg/kg (intravenous) Route of Administration: Oral; single dose; intravenous; single dose Experimental Results: After oral administration, the mean Cmax was 4607 ng/mL, the mean AUC(0-tz) was 80231 ngh/mL, and the mean bioavailability was 201%. Following intravenous administration, the mean CO was 16.2 ng/mL, the mean AUC(0-tz) was 7997 ngh/mL, the mean AUC(0-inf) was 10648 ngh/mL, the mean elimination half-life (t1/2z) was 11.3 hours, the mean clearance (CL) was 188 mL/(hkg), and the mean volume of distribution (Vz) was 3074 mL/kg. Animal/Disease Models:C57Bl/6N mice (21-26 g)[1] Doses: 10 mg/kg Route of Administration: Oral; Single dose Experimental Results: Four hours after administration, the average plasma concentration reached 5474 ng/mL, the average brain concentration reached 8609 ng/mL, and the brain-plasma ratio was 1.57. |
| References |
| Molecular Formula |
C20H19F2N3O2S2
|
|---|---|
| Molecular Weight |
435.51
|
| CAS # |
2137928-83-5
|
| Appearance |
Powder
|
| SMILES |
FC(C=CC(F)=C1)=C1C(C=C2)=CC=C2CC(N(C3=NC(C)=C(S(C)(=N)=O)S3)C)=O
|
| Synonyms |
(Rac)-IM-250
|
| 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
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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 | 2.2962 mL | 11.4808 mL | 22.9616 mL | |
| 5 mM | 0.4592 mL | 2.2962 mL | 4.5923 mL | |
| 10 mM | 0.2296 mL | 1.1481 mL | 2.2962 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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