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Reverse transcriptase-IN-1 [2380001-43-2]

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Cat# NB-64-04209-1mg

Size : 1mg

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Reverse transcriptase-IN-1

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Synonyms:

Catalog No. T12715 Copy Product Info

Purity: 99.61%

Reverse transcriptase-IN-1 is a diarylbenzopyrimidine (DABP) analogue and a potent inhibitor of HIV-1 nonnucleoside reverse transcriptase with an IC50of 13.7 nM.

Cas No. 2380001-43-2

With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.61%

Appearance:Solid

Color:Yellow

Product Introduction

Bioactivity

Description	Reverse transcriptase-IN-1 is a diarylbenzopyrimidine (DABP) analogue and a potent inhibitor of HIV-1 nonnucleoside reverse transcriptase with an IC50of 13.7 nM.
Targets & IC50	HIV-1 RT:13.7 nM
In vitro	Reverse transcriptase-IN-1 has antiviral activity with EC50 values of 3.4 nM, 4.3 nM and 3.6 nM for HIV-1 IIIB, E138K and K103N mutants, respectively[1].
In vivo	The PK study and safety assessment of Reverse transcriptase-IN-1 shows that it is absorbed with mean residence times (MRTs) of 11.8 hours (5 mg/kg, p.o.) and 11.4 hours (1 mg/kg, i.v.) at these two doses. The Cmax of Reverse transcriptase-IN-1 is 39.9 ng/mL at a dose of 5 mg/kg. The oral bioavailability of Reverse transcriptase-IN-1 is significantly improved to 16.5% at a dose of 5 mg/kg in rats. The intrinsic rat microsome clearance of Reverse transcriptase-IN-1 is 33.2 μL/min/mg proteins[1].

Chemical Properties

Molecular Weight	447.45
Formula	C₂₅H₁₇N₇O₂
Cas No.	2380001-43-2
Smiles	Cc1cc(\C=C\C#N)cc(c1Nc1nc(Nc2ccc(cc2)C#N)nc2ccccc12)[N+]([O-])=O
Relative Density.	1.42 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 12 mg/mL (26.82 mM), Sonication and heating to 60℃ are recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.23 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2349 mL	11.1744 mL	22.3489 mL	111.7443 mL
5 mM	0.4470 mL	2.2349 mL	4.4698 mL	22.3489 mL
10 mM	0.2235 mL	1.1174 mL	2.2349 mL	11.1744 mL
20 mM	0.1117 mL	0.5587 mL	1.1174 mL	5.5872 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

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Keywords

Reverse transcriptase-IN-1Reverse transcriptaseIN1Reverse transcriptase IN 1InhibitorinhibitHuman immunodeficiency virusHIVProteaseHIV-1 reverse transcriptaseHIV-1HIV ProteaseHIV

Related Tags: Reverse transcriptase-IN-1 chemical structure | Reverse transcriptase-IN-1 in vivo | Reverse transcriptase-IN-1 in vitro | Reverse transcriptase-IN-1 formula | Reverse transcriptase-IN-1 molecular weight