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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
Last updated:2024-05-23 09:46:09

Islatravir Properties

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)
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)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319-H335
Precautionary statements  P261-P280-P301+P312-P302+P352-P305+P351+P338
NFPA 704
0
2 0

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
Product number Packaging Price Buy
CS-0023675 5mg $500 Buy
Axon3191 2x5mg $792 Buy
CS-0023675 10mg $850 Buy
CS-0023675 25mg $1800 Buy
CS-0023675 50mg $3000 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

Global( 74)Suppliers
Supplier Tel Email Country ProdList Advantage
Amadis Chemical Company Limited
571-89925085 sales@amadischem.com China 131981 58
Wuhan Topule Biopharmaceutical Co., Ltd
+8618327326525 masar@topule.com China 8474 58
NewCan Biotech Limited
+86-0571-86912261 +8613735419629 sales@newcanbio.com China 9978 58
Henan Tianfu Chemical Co.,Ltd.
+86-0371-55170693 +86-19937530512 info@tianfuchem.com China 21689 55
Shenzhen Nexconn Pharmatechs Ltd
+86-755-89396905 +86-15013857715 admin@nexconn.com China 10247 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
Islatravir pictures 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 E2FDA pictures 2024-02-06 4'-ethynyl-2-fluoro-2'-deoxyadenosine EFDA E2FDA
865363-93-5
US $4000.00 / g 1g 95% 10KGS Yunbio Tech Co.,Ltd.
4'-ethynyl-2-fluoro-2'-deoxyadenosine/EFDA pictures 2021-09-29 4'-ethynyl-2-fluoro-2'-deoxyadenosine/EFDA
865363-93-5
US $0.00 / g 1g 95%min 10G WUHAN FORTUNA CHEMICAL CO., LTD
  • Islatravir pictures
  • Islatravir
    865363-93-5
  • US $0.00-0.00 / mg
  • 98%
  • NewCan Biotech Limited
4'-ethynyl-2-fluoro-2'-deoxyadenosine EFdA 2'-deoxy-4'-C-ethynyl-2-fluoro-Adenosine E2FDA 2'-Deoxy-4'-ethynyl-2-fluoroadenosine 4'-ethynyl-2-fluoro-2'-deoxyadenosine EFDA E2FDA Islatravir Adenosine Related Compound Adenosine Related Compound 6 (MK-8591) (2R,3S,5R)-5-(6-amino-2-fluoro-9H-purin-9-yl)-2-ethynyl-2-(hydroxymethyl)tetrahydrofuran-3-ol Adenosine, 2'-deoxy-4'-C-ethynyl-2-fluoro- Adenosine Impurity 22 4'-ethynyl-2-fluoro-2'-deoxyadenosine/EFDA Islatravir(MK-8591) (2R,3S,5R)-5-(6-amino-2-fluoro-4H-purin-9(5H)-yl)-2-ethynyl-2-(hydroxymethyl)-tetrahydrofuran-3-ol (2R,3S,5R)-5-(6-amino-2-fluoropurin-9-yl)-2-ethynyl-2-(hydroxymethyl)oxolan-3-ol Human immunodeficiency virus,Inhibitor,Islatravir,MK 8591,inhibit,MK8591,Reverse Transcriptase,HIV MK-8591 (Islatravir) 2-DEOXY-4-C-ETHYNYL-2-FLUORO- 4'-ethynyl-2-fluoro-2'-deoxyadenosine 865363-93-5 C12H12FN5O3