Nipamovir
Based on 1 Customer Validation
Nipamovir is an orally active anti-HIV prodrug. Nipamovir is cleaved in vivo by glutathione and other active thiols. Nipamovir inhibits the replication of HIV-1RF and HIV-192HT599 in cells, with EC50 values of 3.64 μM and 3.23 μM, respectively. Nipamovir can be used in studies related to HIV infection.
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- Pureté: 98.60%
- CAS No.: 2651908-78-8
- Formule: C14H15N5O4S
- Masse moléculaire:349.37
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Nipamovir inhibits the replication of HIV-1RF in CEM-SS cells, with an EC50 of 3.64 μM and a TC50 > 100 μM[1].
Nipamovir inhibits the replication of HIV-192HT599 in hPBMCs, with an EC50 of 3.23 μM and a TC50 > 100 μM[1].
Nipamovir (0.01-100 μM; 12 days) inhibits the replication of HIV-1LAI.04 in tonsil tissue blocks, with an IC50 of approximately 4.54 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | AUC0-inf | AUC0-t | T1/2 | Tmax | C0 | CL | MRT0-inf | Cmax |
|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 5 mg/kg | i.v. | 499 ng·h/mL | 493 ng·h/mL | 0.14 h | / | 3537 ng/mL | 169 mL/min/kg | 0.13 h | / |
| Rat[1] | 300 mg/kg | p.o. | 577 ng·h/mL | 513 ng·h/mL | 1.54 h | 0.25 h | / | / | 2.85 h | 219 ng/mL |
| Cynomolgus Monkey[1] | 1.1 mg/kg | i.v. | 316 ng·h/mL | 315 ng·h/mL | 0.48 h | 0.08 h | 1659 ng/mL | 60 mL/min/kg | 0.34 h | / |
| Cynomolgus Monkey[1] | 300 mg/kg | p.o. | 94.0 ng·h/mL | 87.7 ng·h/mL | 2.53 h | 1.00 h | / | / | 4.01 h | 26.0 ng/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (SD) (male, 200-350 g)[1]
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Dosage:5 mg/kg (i.v.); 300 mg/kg (p.o.)
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Administration:i.v.; single bolus; p.o.; single oral gavage
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Result:Exhibited an AUC0-inf of 499 ng*h/mL, elimination half-life of 0.14 h, clearance of 169 mL/min/kg, and volume of distribution of 1.3 L/kg after 5 mg/kg i.v. administration.
Had an AUC0-inf of 577 ng*h/mL, elimination half-life of 1.54 h, Cmax of 219 ng/mL, and tmax of 0.25 h after 300 mg/kg p.o. administration.
Active metabolite 2 had an AUC0-inf of 509 ng*h/mL, elimination half-life of 0.35 h, Cmax of 1180 ng/mL, and tmax of 0.08 h after 5 mg/kg i.v. administration.
Active metabolite 2 had an AUC0-inf of 9560 ng*h/mL, elimination half-life of 3.66 h, Cmax of 2950 ng/mL, tmax of 0.25 h, and oral bioavailability of 31.4% after 300 mg/kg p.o. administration.
Inactive metabolite 17 had an AUC0-inf of 1070 ng*h/mL, elimination half-life of 0.84 h, Cmax of 640 ng/mL, and tmax of 0.25 h after 5 mg/kg i.v. administration.
Inactive metabolite 17 had an AUC0-inf of 13700 ng*h/mL, elimination half-life of 3.03 h, Cmax of 1290 ng/mL, and tmax of 2.0 h after 300 mg/kg p.o. administration.
Chemical Information
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CAS No. 2651908-78-8
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Appearance Solid
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Masse moléculaire 349.37
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Formule C14H15N5O4S
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Color White to yellow
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SMILES
O=C(NCCC(N)=O)C1=C(SC2=C([N+]([O-])=O)N=CN2C)C=CC=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (286.23 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (14.31 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (14.31 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8623 mL | 14.3115 mL | 28.6230 mL | 71.5574 mL |
| 5 mM | 0.5725 mL | 2.8623 mL | 5.7246 mL | 14.3115 mL | |
| 10 mM | 0.2862 mL | 1.4311 mL | 2.8623 mL | 7.1557 mL | |
| 15 mM | 0.1908 mL | 0.9541 mL | 1.9082 mL | 4.7705 mL | |
| 20 mM | 0.1431 mL | 0.7156 mL | 1.4311 mL | 3.5779 mL | |
| 25 mM | 0.1145 mL | 0.5725 mL | 1.1449 mL | 2.8623 mL | |
| 30 mM | 0.0954 mL | 0.4770 mL | 0.9541 mL | 2.3852 mL | |
| 40 mM | 0.0716 mL | 0.3578 mL | 0.7156 mL | 1.7889 mL | |
| 50 mM | 0.0572 mL | 0.2862 mL | 0.5725 mL | 1.4311 mL | |
| 60 mM | 0.0477 mL | 0.2385 mL | 0.4770 mL | 1.1926 mL | |
| 80 mM | 0.0358 mL | 0.1789 mL | 0.3578 mL | 0.8945 mL | |
| 100 mM | 0.0286 mL | 0.1431 mL | 0.2862 mL | 0.7156 mL |
Nipamovir Related Classifications
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