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Shanghai Chaolan Chemical Technology Center
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Product Name:Reverse transcriptase-IN-1
CAS:2380001-43-2
Purity:98% Package:5MG;10MG;50MG;100MG,1G,5G,100G
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Reverse transcriptase-IN-1 manufacturers
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| | Reverse transcriptase-IN-1 Basic information |
| Product Name: | Reverse transcriptase-IN-1 | | Synonyms: | 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]- | | CAS: | 2380001-43-2 | | MF: | C25H17N7O2 | | MW: | 447.45 | | EINECS: | | | Product Categories: | | | Mol File: | 2380001-43-2.mol |  |
| | Reverse transcriptase-IN-1 Chemical Properties |
| Boiling point | 708.3±70.0 °C(Predicted) | | density | 1.42±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | form | Solid | | pka | 7.22±0.30(Predicted) | | color | Light yellow to yellow |
| | Reverse transcriptase-IN-1 Usage And Synthesis |
| 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 |
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