Islatravir triphosphate – CAS 950913-56-1

25006000

Islatravir triphosphate is synthesised by Santiago Lab (Prague, Czech Republic). We are providing Islatravir triphosphate in the form of Et3NH+ salt. All products are lyophilized and can easily sustain the shipment oversee.

Purity (LC-MS)

99%+ |Certificate of Analysis

Package contents

Islatravir triphosphate salt

This compound is for research use only. We do not sell to patients.

We are sending Islatravir triphosphate in the form of Et3NH+ salt.

SizeAvailabilityPriceQuantity
1 mg

In stock

2500
5 mg

In stock

6000
100mM/10μL

In stock

2500
10mM/100μL

In stock

2500

Islatravir triphosphate

Characterisation

CAS: 950913-56-1, 2736455-59-5 (Et3NH+ salt)

IUPAC Name: 2′-​deoxy-​4′-​C-​ethynyl-​2-​fluoro-adenosine 5′-​(tetrahydrogen triphosphate)

Other names: Islatravir triphosphate, Islatravir TP

Molecular weight: 533.19 g/mol, 

Molecular formula: C12 H15 F N5 O12 P3

Storage: -20 °C, protect from light, stored under argon

We are providing Islatravir triphosphate in the form of Et3NH+ salt.

Description

Islatravir triphosphate is synthesised by Santiago Lab (Prague, Czech Republic). Islatravir (EFdA, or MK-8591) is an investigational drug for the treatment of HIV infection developed by company Merck. It is classified as a nucleoside reverse transcriptase translocation inhibitor (NRTTI).  Islatravir has activity against HIV in animal models and is being studied clinically for HIV treatment and prophylaxis. Islatravir is a nucleoside analogue reverse transcriptase translocation inhibitor that, unlike other such inhibitors, inhibits HIV through multiple mechanisms, providing rapid suppression of the virus, when tested in macaques and mice.  Islatravir inhibits HIV reverse transcriptase but has a different mechanism of action with respect to all other approved NRTIs because of its unique structural features: a 3’-hydroxyl group makes this nucleotide a translocation inhibitor rather than a chain terminator. Introducing a 4’-ethynyl group enhances the selectivity towards the HIV reverse transcriptase. Similarly to other nucleoside antiviral drugs, Islatravir is first transformed to islatravir-5’-triphosphate (ISL-TP), which is the biologically active form of Islatravir. When ITP is incorporated into forming DNA strand by the reverse transcriptase, it acts as a chain terminator by preventing the translocation.

Based on its unique properties, Merck is currently developing a sub-dermal implant for the long-term release of Islatravir. This implant is now under clinical evaluation and is likely to cause a revolution in HIV treatment. You can find more information about Islatravir in our article.

Chemicals are distributed worldwide

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  • Shipping through DHL in 48 hours. We can also arrange shipping on dry ice.
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  • All compounds are safely and rigorously packed
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Payment
  • We are sending the invoice the same day as the shipment
  • We can modify the invoice for the academic institution so that the order can be paid from grants
References

References
1. Kawamoto, A; Kodama, E; Sarafianos, SG; Sakagami, Y; Kohgo, S; Kitano, K; Ashida, N; Iwai, Y; Hayakawa, H; Nakata, H; Mitsuya, H; Arnold, E; Matsuoka, M (2008). "2'-deoxy-4'-C-ethynyl-2-halo-adenosines active against drug-resistant human immunodeficiency virus type 1 variants". The International Journal of Biochemistry & Cell Biology. 40 (11): 2410–20. doi:10.1016/j.biocel.2008.04.007. PMID 18487070.
2. Roy M. Gulick (2018). "Investigational Antiretroviral Drugs: What is Coming Down the Pipeline". Top Antivir Med. 25 (4): 127–132. PMC 5935216. PMID 29689540.

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