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Reverse transcriptase-IN-1

Reverse transcriptase-IN-1 Structure
Reverse transcriptase-IN-1 structure
CAS No.
2380001-43-2
Chemical Name:
Reverse transcriptase-IN-1
Synonyms
Reverse transcriptase-IN-1;Benzonitrile, 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2-methyl-6-nitrophenyl]amino]-2-quinazolinyl]amino]-;Human immunodeficiency virus,Reverse transcriptaseIN1,Inhibitor,Reverse transcriptase IN 1,inhibit,HIV
CBNumber:
CB68054520
Molecular Formula:
C25H17N7O2
Molecular Weight:
447.45
MDL Number:
MFCD32263435
MOL File:
2380001-43-2.mol
Last updated:2023-05-21 10:59:17
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Reverse transcriptase-IN-1 Properties

Boiling point 708.3±70.0 °C(Predicted)
Density 1.42±0.1 g/cm3(Predicted)
storage temp. Store at -20°C
pka 7.22±0.30(Predicted)

Reverse transcriptase-IN-1 Chemical Properties,Uses,Production

Biological Activity

Reverse transcriptase-IN-1 (Compound 12z), a diarylbenzopyrimidine (DABP) analogue, is a potent, orally active HIV-1 nonnucleoside reverse transcriptase inhibitor. 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. Reverse transcriptase-IN-1 also has an IC50of 13.7 nM against HIV-1 reverse transcriptase enzyme[1]. The oral bioavailability of Reverse transcriptase-IN-1 (Compound 12z) 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. 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. A single-dose toxicity test of Reverse transcriptase-IN-1 in rats shows no mortality, and there is no abnormal body weight decrease in the animals in the week following an intragastrical dose at 293 mg/kg body weigh. The above results indicate that Reverse transcriptase-IN-1 could be an orally bioavailable candidate for human HIV-1 infection research[1].

References

[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.

Reverse transcriptase-IN-1 Preparation Products And Raw materials

Raw materials

Preparation Products

Reverse transcriptase-IN-1 Suppliers

Global( 8)Suppliers
Supplier Tel Email Country ProdList Advantage
ATK CHEMICAL COMPANY LIMITED 		+undefined-21-51877795 ivan@atkchemical.com China 32480 60
TargetMol Chemicals Inc. 		+1-781-999-5354 +1-00000000000 marketing@targetmol.com United States 19892 58
Shanghai SuperLan Chemcial Technique Centre 021-2022843681 15618226720 chaolaichem@foxmail.com China 7565 58
cjbscvictory 13348960310 13348960310 3003867561@qq.com China 9946 58
TargetMol Chemicals Inc. 4008200310 marketing@tsbiochem.com China 24131 58
Yantai Lianhua Technology Co., Ltd 15552437730 1701654643@qq.com China 11397 58
RD International Technology Co., Limited 18988968278 sales@ubiochem.com China 9146 58
Nanjing Shizhou Biology Technology Co.,Ltd 025-85560043 15850508050 cindy.huang@synzest.com China 12007 58
Supplier Advantage
ATK CHEMICAL COMPANY LIMITED 		60
TargetMol Chemicals Inc. 		58
Shanghai SuperLan Chemcial Technique Centre 58
cjbscvictory 58
TargetMol Chemicals Inc. 58
Yantai Lianhua Technology Co., Ltd 58
RD International Technology Co., Limited 58
Nanjing Shizhou Biology Technology Co.,Ltd 58
Reverse transcriptase-IN-1 Human immunodeficiency virus,Reverse transcriptaseIN1,Inhibitor,Reverse transcriptase IN 1,inhibit,HIV Benzonitrile, 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2-methyl-6-nitrophenyl]amino]-2-quinazolinyl]amino]- 2380001-43-2