Art. -Nr.: HY-162074

Nipamovir

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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-1_RF and HIV-1_92HT599 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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Reinheit: 98.60%
CAS. Nr.: 2651908-78-8
Formel: C₁₄H₁₅N₅O₄S
Molecular Weight:349.37

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Nipamovir Chemical Structure

CAS. Nr.: 2651908-78-8

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Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle HIV Isoform-spezifische Produkte anzeigen :

In Vitro

Nipamovir inhibits the replication of HIV-1_RF in CEM-SS cells, with an EC₅₀ of 3.64 μM and a TC₅₀ > 100 μM^[1].
Nipamovir inhibits the replication of HIV-1_92HT599 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-1_LAI.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.

Parmacokinetics

Species	Dose	Route	AUC_0-inf	AUC_0-t	T_1/2	T_max	C₀	CL	MRT_0-inf	C_max
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

In Vivo

Nipamovir (5-300 mg/kg; i.v., p.o.; single bolus, single oral gavage) exhibits high clearance and short half-life after intravenous administration in SD rats, with moderate oral bioavailability (31.4%) of its active metabolite 2^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Sprague-Dawley (SD) (male, 200-350 g)^[1]
Dosage:

5 mg/kg (i.v.); 300 mg/kg (p.o.)
Administration:

i.v.; single bolus; p.o.; single oral gavage
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

CAS. Nr. 2651908-78-8
Appearance Solid
Molecular Weight 349.37
Formel C₁₄H₁₅N₅O₄S
Color White to yellow
SMILES

O=C(NCCC(N)=O)C1=C(SC2=C([N+]([O-])=O)N=CN2C)C=CC=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8623 mL

14.3115 mL

28.6229 mL

5 mM

0.5725 mL

2.8623 mL

5.7246 mL

10 mM

0.2862 mL

1.4311 mL

2.8623 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (14.31 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Robello M, et al. Prodrug Strategy Extends the Use of Anti-HIV Sulfanylbenzamides for Application In Vivo. ACS Pharmacol Transl Sci. 2023;7(1):259-273. Published 2023 Dec 14. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Nipamovir

Alle HIV Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Nipamovir Related Classifications

HY-162074 Related Classifications