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
- MDL Number:
- MFCD28502143
- MOL File:
- 865363-93-5.mol
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 |
FDA UNII | QPQ082R25D |
SAFETY
Risk and Safety Statements
Symbol(GHS) | GHS07 |
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Signal word | Warning | |||||||||
Hazard statements | H302-H315-H319-H335 | |||||||||
Precautionary statements | P261-P280-P301+P312-P302+P352-P305+P351+P338 | |||||||||
NFPA 704 |
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Islatravir price
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
ChemScene | CS-0023675 | Islatravir 99.94% | 865363-93-5 | 5mg | $500 | 2021-12-16 | Buy |
Axon Medchem | Axon3191 | Islatravir-EFdA|MK-8591 99% | 865363-93-5 | 2x5mg | $792 | 2021-12-16 | Buy |
ChemScene | CS-0023675 | Islatravir 99.94% | 865363-93-5 | 10mg | $850 | 2021-12-16 | Buy |
ChemScene | CS-0023675 | Islatravir 99.94% | 865363-93-5 | 25mg | $1800 | 2021-12-16 | Buy |
ChemScene | CS-0023675 | Islatravir 99.94% | 865363-93-5 | 50mg | $3000 | 2021-12-16 | Buy |
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
MK-?8591 is a carbocyclic nucleoside reverse transcriptase translocation inhibitor and is used as an antiviral with potential use towards the treatment of HIV.
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 | |
---|---|---|---|---|---|
Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131980 | 58 |
Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8474 | 58 |
NewCan Biotech Limited | +86-0571-86912261 +8613735419629 | sales@newcanbio.com | China | 9980 | 58 |
Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 | info@tianfuchem.com | China | 21667 | 55 |
Shenzhen Nexconn Pharmatechs Ltd | +86-755-89396905 +86-15013857715 | admin@nexconn.com | China | 10311 | 58 |
Beijing Ribio Biotech Co.,Ltd | 010-62664360 +8613328773880 | wucy@ribio.com.cn | China | 117 | 58 |
Yunbio Tech Co.,Ltd. | +86-010-60605551 +86-18046518538 | yunbiochem@126.com | China | 321 | 58 |
Shandong chuangyingchemical Co., Ltd. | 18853181302 | sale@chuangyingchem.com | CHINA | 5909 | 58 |
BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
View Lastest Price from Islatravir manufacturers
Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
---|---|---|---|---|---|---|---|---|
2024-09-18 | 4'-ethynyl-2-fluoro-2'-deoxyadenosine/EFDA
865363-93-5
|
US $0.00 / g | 1g | 95%min | 10G | WUHAN FORTUNA CHEMICAL CO., LTD | ||
2024-08-07 | 4'-ethynyl-2-fluoro-2'-deoxyadenosine EFDA E2FDA
865363-93-5
|
US $4000.00 / g | 1g | 95% | 10KGS | Yunbio Tech Co.,Ltd. | ||
2024-05-22 | Islatravir
865363-93-5
|
US $0.00-0.00 / mg | 100mg | 98% | 10g | NewCan Biotech Limited |
- 4'-ethynyl-2-fluoro-2'-deoxyadenosine/EFDA
865363-93-5
- US $0.00 / g
- 95%min
- WUHAN FORTUNA CHEMICAL CO., LTD
- 4'-ethynyl-2-fluoro-2'-deoxyadenosine EFDA E2FDA
865363-93-5
- US $4000.00 / g
- 95%
- Yunbio Tech Co.,Ltd.
- Islatravir
865363-93-5
- US $0.00-0.00 / mg
- 98%
- NewCan Biotech Limited
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