Islatravir
- CAS No.
- 865363-93-5
- Chemical Name:
- Islatravir
- Synonyms
- EFdA;E2FDA;Islatravir;Islatravir(MK-8591);MK-8591 (Islatravir);Adenosine Impurity 22;Adenosine Related Compound;2-DEOXY-4-C-ETHYNYL-2-FLUORO-;2'-Deoxy-4'-ethynyl-2-fluoroadenosine;4'-ethynyl-2-fluoro-2'-deoxyadenosine
- CBNumber:
- CB32657140
- Molecular Formula:
- C12H12FN5O3
- Molecular Weight:
- 293.25
- MOL File:
- 865363-93-5.mol
- Modify Date:
- 2024/7/2 8:55:06
| Melting point | 220.0-221.4 °C (decomp) |
|---|---|
| Boiling point | 669.2±65.0 °C(Predicted) |
| Density | 1.72±0.1 g/cm3(Predicted) |
| storage temp. | Store at -20°C |
| solubility |
DMSO:100.0(Max Conc. mg/mL);341.0(Max Conc. mM) Water:3.57(Max Conc. mg/mL);12.17(Max Conc. mM) |
| form | A solid |
| pka | 13.11±0.60(Predicted) |
| color | White to off-white |
| InChI | InChI=1S/C12H12FN5O3/c1-2-12(4-19)6(20)3-7(21-12)18-5-15-8-9(14)16-11(13)17-10(8)18/h1,5-7,19-20H,3-4H2,(H2,14,16,17)/t6-,7+,12+/m0/s1 |
| InChIKey | IKKXOSBHLYMWAE-QRPMWFLTSA-N |
| SMILES | OC[C@@]1(C#C)O[C@@H](N2C3C(=C(N=C(F)N=3)N)N=C2)C[C@@H]1O |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H315-H319-H335 | |||||||||
| Precautionary statements | P261-P280-P301+P312-P302+P352-P305+P351+P338 | |||||||||
| NFPA 704 |
|
Islatravir Chemical Properties,Uses,Production
Description
Islatravir belongs to a group of HIV drugs called nucleoside reverse transcriptase translocation inhibitors (NRTTIs). NRTTIs use several different methods to block an HIV enzyme called reverse transcriptase. By blocking reverse transcriptase, NRTTIs prevent HIV from multiplying and can reduce the amount of HIV in the body. This compound may be effective against certain HIV strains that are resistant to other HIV drugs.
Uses
4'-ethynyl-2-fluoro-2'-deoxyadenosine (Islatravir) is a heterocyclic organic compound and can be used as pharmaceutical intermediates.
Mechanism of action
Islatravir belongs to a group of HIV drugs called nucleoside reverse transcriptase translocation inhibitors (NRTTIs). NRTTIs use several different methods to block an HIV enzyme called reverse transcriptase. By blocking reverse transcriptase, NRTTIs prevent HIV from multiplying and can reduce the amount of HIV in the body. This compound may be effective against certain HIV strains that are resistant to other HIV drugs[1].
Pharmacokinetics
Islatravir is converted intracellularly by endogenous kinases to its active triphosphate (TP) form, islatravir-TP, which has a long intracellular half-life, allowing the potential for various dosing options and regimens. In participants without HIV, single oral doses of islatravir were rapidly absorbed, with peak plasma concentrations attained at ~ 0.5 h, with islatravir demonstrating a half-life of ~ 49–61 h. Peak intracellular islatravir-TP concentrations were attained 6–24 h after islatravir administration, with a half-life of 118–171 h; similar pharmacokinetics have been observed in people living with HIV-1. When administered once daily (QD), oral doses of islatravir resulted in steady-state plasma concentrations at approximately Day 14. At the same time, intracellular islatravir-TP reached a steady state by Day 28 and remained above the concentration threshold associated with antiviral efficacy (0.05 pmol/106 cells) for ~ 30 days following cessation of dosing. In addition, doses as low as 0.25 mg QD produced intracellular islatravir-TP concentrations exceeding the therapeutic concentration threshold on Day 1[1].
References
[1] Randolph P Matthews. “A Phase 1 Study to Evaluate the Drug Interaction Between Islatravir (MK-8591) and Doravirine in Adults Without HIV.” Clinical Drug Investigation (2021): 629–638.
Islatravir Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| Amadis Chemical Company Limited | 571-89925085 | China | 131980 | 58 | Inquiry |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | China | 8474 | 58 | Inquiry |
| NewCan Biotech Limited | +86-0571-86912261 +8613735419629 | China | 9980 | 58 | Inquiry |
| Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 | China | 21669 | 55 | Inquiry |
| Shenzhen Nexconn Pharmatechs Ltd | +86-755-89396905 +86-15013857715 | China | 10312 | 58 | Inquiry |
| Beijing Ribio Biotech Co.,Ltd | 010-62664360 +8613328773880 | China | 117 | 58 | Inquiry |
| Yunbio Tech Co.,Ltd. | +86-010-60605551 +86-18046518538 | China | 321 | 58 | Inquiry |
| BOC Sciences | +1-631-485-4226 | United States | 19553 | 58 | Inquiry |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | United States | 19892 | 58 | Inquiry |
| Finetech Industry Limited | +86-27-87465837 +8618971612321 | China | 9618 | 58 | Inquiry |
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