Islatravir
- Product Name
- 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-;4'-ethynyl-2-fluoro-2'-deoxyadenosine;2'-Deoxy-4'-ethynyl-2-fluoroadenosine
- CBNumber
- CB32657140
- Molecular Formula
- C12H12FN5O3
- Formula Weight
- 293.25
- MOL File
- 865363-93-5.mol
Islatravir Property
- 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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- CS-0023675
- Product name
- Islatravir
- Purity
- 99.94%
- Packaging
- 5mg
- Price
- $500
- Updated
- 2021/12/16
- Product number
- Axon3191
- Product name
- Islatravir-EFdA|MK-8591
- Purity
- 99%
- Packaging
- 2x5mg
- Price
- $792
- Updated
- 2021/12/16
- Product number
- CS-0023675
- Product name
- Islatravir
- Purity
- 99.94%
- Packaging
- 10mg
- Price
- $850
- Updated
- 2021/12/16
- Product number
- CS-0023675
- Product name
- Islatravir
- Purity
- 99.94%
- Packaging
- 25mg
- Price
- $1800
- Updated
- 2021/12/16
- Product number
- CS-0023675
- Product name
- Islatravir
- Purity
- 99.94%
- Packaging
- 50mg
- Price
- $3000
- Updated
- 2021/12/16
Islatravir Chemical Properties,Usage,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
Islatravir Suppliers
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- +1-781-999-5354 +1-00000000000
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- United States
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View Lastest Price from Islatravir manufacturers
- Product
- 4'-ethynyl-2-fluoro-2'-deoxyadenosine/EFDA 865363-93-5
- Price
- US $0.00/g
- Min. Order
- 1g
- Purity
- 95%min
- Supply Ability
- 10G
- Release date
- 2021-06-18
- Product
- 4'-ethynyl-2-fluoro-2'-deoxyadenosine EFDA E2FDA 865363-93-5
- Price
- US $4000.00/g
- Min. Order
- 1g
- Purity
- 95%
- Supply Ability
- 10KGS
- Release date
- 2019-11-28
- Product
- Islatravir 865363-93-5
- Price
- US $0.00-0.00/mg
- Min. Order
- 100mg
- Purity
- 98%
- Supply Ability
- 10g
- Release date
- 2024-05-22