| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
NNRT-IN-13 (compound 15k) showed excellent antiviral activity against wild-type HIV-1 (EC₅₀ = 0.0046 μM) and broad-spectrum activity against a range of drug-resistant mutants, including L100I (0.0053 μM), K103N (0.0034 μM), Y181C (0.010 μM), Y188L (0.026 μM), E138K (0.015 μM), F227L/V106A (0.033 μM) and K103N/Y181C (0.029 μM), while showing low cytotoxicity in MT-4 cells (CC₅₀ = 26.64 μM)[1]. NNRT-IN-13 binds to HIV-1 reverse transcriptase in a unique “Y” shape and forms novel hydrogen bonds with E138 and K101 residues at the p51-p66 interface [1]. NNRT-IN-13 has no inhibitory effect on CYP1A2, CYP2C9, CYP2C19 and CYP2D6 (IC₅₀ values are all greater than 50 μM), and only shows weak inhibition on CYP3A4 (IC₅₀ = 13.6 μM) [1].
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|---|---|
| ln Vivo |
NNRT-IN-13 (50 and 2000 mg/kg, intraperitoneal injection, single dose or every other day for 14 days) did not show toxicity in the Kunming mouse model and did not cause organ damage [1].
|
| Animal Protocol |
Animal/Disease Models: Kunming mice[1]
Doses: 2000 mg/kg Route of Administration: i.p., single dose Experimental Results: Showed no mortality or adverse toxicity signs, including anorexia, lethargy, alopecia, or dyspnea. Exhibited steady weight gain over the seven-day observation period, with no significant differences compared to control. Animal/Disease Models: Kunming mice[1] Doses: 50 mg/kg Route of Administration: i.p., every other day for 14 days Experimental Results: Showed no apparent toxicity signs or behavioral abnormalities (such as lethargy, clonic convulsions, anorexia, and ruffled fur. Gained normal body weight and were equivalent to those of the control group. Exhibited no visible pathological changes or lesions were detected in the heart, liver, spleen, lungs, or kidneys. |
| References |
| Molecular Formula |
C31H34N8O4S
|
|---|---|
| Molecular Weight |
614.72
|
| 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 | 1.6268 mL | 8.1338 mL | 16.2676 mL | |
| 5 mM | 0.3254 mL | 1.6268 mL | 3.2535 mL | |
| 10 mM | 0.1627 mL | 0.8134 mL | 1.6268 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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