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Reverse transcriptase-IN-1

Catalog No. T12715 CAS 2380001-43-2

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.

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Reverse transcriptase-IN-1 Chemical Structure

Reverse transcriptase-IN-1, CAS 2380001-43-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 97.00
5 mg	In stock	$ 222.00
10 mg	In stock	$ 322.00
25 mg	In stock	$ 547.00
50 mg	In stock	$ 788.00
100 mg	In stock	$ 1,080.00
500 mg	In stock	$ 2,180.00
1 mL * 10 mM (in DMSO)	In stock	$ 243.00

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Purity: 99.14%

Biological Description

Chemical Properties

Storage & Solubility Information

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].

Molecular Weight	447.45
Formula	C25H17N7O2
CAS No.	2380001-43-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

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

References and Literature

1. Han S, et al. Molecular Hybridization-Inspired Optimization of Diarylbenzopyrimidines as HIV-1 Nonnucleoside Reverse Transcriptase Inhibitors with Improved Activity against K103N and E138K Mutants and Pharmacokinetic Profiles. ACS Infect Dis. 2019 Oct 24.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Viral Compound Library Bioactive Compounds Library Max Bioactive Compound Library Covalent Inhibitor Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid 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 master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Reverse transcriptase-IN-1 2380001-43-2 Microbiology/Virology Proteases/Proteasome HIV Protease Human immunodeficiency virus Reverse transcriptaseIN1 Inhibitor Reverse transcriptase IN 1 inhibit HIV inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.