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

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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

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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.

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0023675
Product name: Islatravir
Purity: 99.94%
Packaging: 5mg
Price: $500
Updated: 2021/12/16

Axon Medchem

Product number: Axon3191
Product name: Islatravir-EFdA|MK-8591
Purity: 99%
Packaging: 2x5mg
Price: $792
Updated: 2021/12/16

ChemScene

Product number: CS-0023675
Product name: Islatravir
Purity: 99.94%
Packaging: 10mg
Price: $850
Updated: 2021/12/16

ChemScene

Product number: CS-0023675
Product name: Islatravir
Purity: 99.94%
Packaging: 25mg
Price: $1800
Updated: 2021/12/16

ChemScene

Product number: CS-0023675
Product name: Islatravir
Purity: 99.94%
Packaging: 50mg
Price: $3000
Updated: 2021/12/16

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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

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Islatravir Suppliers

China 69 United States 6 Global 75

NewCan Biotech Limited

Tel: +86-0571-86912261 +86-15658003402
Email: sales@newcanbio.com
Country: China
ProdList: 344
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InvivoChem

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Wuhan Biocar Pharmacy Co.，Ltd

Tel: 18665676617
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Shanghai jerryxing Biomedical Technology Co., Ltd

Tel: 17721492509
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Country: China
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Changsha Fuzhen Biotechnology Co.，LTD

Tel: 13823398779 18670069958
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Bayee Biotech (Anqing) Co., Ltd.

Tel: 0556-5032306 18917961636
Fax: +86-556-5032307
Email: wtx@bayeebio.com
Country: China
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ShangHai Caerulum Pharma Discovery Co., Ltd.

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Finetech Industry Limited

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Fax: 027-8777-2287
Email: sales@finetechnology-ind.com
Country: China
ProdList: 9649
Advantage: 58

NINGBO INNO PHARMCHEM CO.,LTD.

Tel: 86-574-27787657
Fax: 86-574-27912196
Email: info@dearchem.com
Country: China
ProdList: 4613
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Cool Pharm, Ltd

Tel: 021-60455363 18019463053
Fax: 50966098
Email: sales@coolpharm.com
Country: China
ProdList: 12346
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View Lastest Price from Islatravir manufacturers

WUHAN FORTUNA CHEMICAL CO., LTD

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

Yunbio Tech Co.,Ltd.

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

NewCan Biotech Limited

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

865363-93-5, IslatravirRelated Search:

(R, S)-Adenosyl-L-Methionine ADENOSINE 5'-TRIPHOSPHATE DISODIUM SAL& Adenosine-5'-diphosphate disodium salt ADENOSINE5'-MONOPHOSPHATESODIUMSALT 8-AMino[1”-(N”-dansyl)-4”-aMinobutyl]-5'-(1-aziridinyl)-5'-deoxy Adenosine Ademetionine 1,4-butanedisulfonate (S, S)-Adenosyl-L-Methionine Ademetionine disulfate tosylate Adenosine 5'-monophosphate Decarboxy-S-adenosylmethionine 5'-DEOXY-5'-METHYLTHIOADENOSINE 2,3,5-TRI-O-ACETYL-6-CHLOROPURINE-9-?-D-RIBOFURANOSIDE S-Adenosyl-L-methionine 2-methylthio-N-6-isopentenyladenosine Adenosine-13C5 2'-O-MB-CAMP SODIUM SALT Adenosine Related Compound 1 Adenosyl Methionine Impurity 2

4'-ethynyl-2-fluoro-2'-deoxyadenosine

E2FDA

EFdA

2'-deoxy-4'-C-ethynyl-2-fluoro-Adenosine

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