| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
HIV; nucleoside reverse transcriptase translocation
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| ln Vitro |
MK-8527 inhibits HIV via same mechanism as that of Islatravir (ISL) may supersede Islatravir (ISL). Data on ISL inhibition of HBV are scarce, and preclinical data show dramatically lower ISL efficacy against HBV than currently preferred nucleos(t)ide drugs, indicating that ISL may not be a potent anti-HBV drug.[1]
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| Enzyme Assay |
Additionally, MK-8527 has a similar mechanism of inhibition to that of Islatravir (ISL), and is currently in Phase I clinical trials, suggesting that developers are finding ways to improve upon ISL. Therefore, MK-8527 May supersede and replace ISL.[1]
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| References | |
| Additional Infomation |
Introduction Islatravir (ISL) is a nucleoside reverse transcriptase translocation inhibitor (NRTTI) that inhibits HIV reverse transcriptase through multiple mechanisms. Unlike all approved NRTTIs, islatravir retains the 3'-hydroxyl group. In vitro and clinical data suggest that ISL is a highly tolerable and potent investigational drug. This article reviews the historical development of islatravir and its mechanisms of action against HIV and HBV and drug resistance. Furthermore, the results of Phase I and Phase II clinical trials are discussed. Expert Opinion Current first-line antiretroviral therapies, pre-exposure prophylaxis, and post-exposure prophylaxis interventions are highly effective in maintaining low or undetectable viral loads. Despite these measures, the exceptionally high annual rate of new infections continues to drive the development of novel antiretroviral drugs that can inhibit drug-resistant HIV and improve patient adherence. ISL was once considered a long-acting drug, but clinical trials have been suspended. The results of ongoing clinical trials of reduced-dose ISL will determine its future clinical application. In addition, MK-8527 inhibits HIV through the same mechanism as ISL and may replace ISL. There is little data on the inhibition of HBV by ISL, and preclinical data show that the efficacy of ISL against HBV is far lower than that of the currently preferred nucleoside (acid) analogues, suggesting that ISL may not be an effective anti-HBV drug. [1]
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| Molecular Formula |
C13H13CLN4O3
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|---|---|
| Molecular Weight |
308.72
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| CAS # |
1810869-23-8
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| Appearance |
White to off-white solid powder
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| Synonyms |
MK-8527; MK8527
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2392 mL | 16.1959 mL | 32.3918 mL | |
| 5 mM | 0.6478 mL | 3.2392 mL | 6.4784 mL | |
| 10 mM | 0.3239 mL | 1.6196 mL | 3.2392 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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