Ulonivirine
Based on 1 Customer Validation
Ulonivirine is an orally active non-nucleoside HIV-1 reverse transcriptase inhibitor that binds to the classical non-nucleoside reverse transcriptase inhibitor hydrophobic binding pocket adjacent to the polymerase active site of HIV-1 reverse transcriptase. Ulonivirine can be used in studies related to HIV-1 infection.
For research use only. We do not sell to patients.
- Purity: 98.61%
- CAS No.: 1591823-76-5
- Formula: C18H8ClF6N5O3
- Molecular Weight:491.73
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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HIV-1 |
Ulonivirine (MK-8507) potently inhibits HIV-1 replication in vitro with an IC50 of 50 nM and retains activity against common NNRTI-resistant HIV-1 variants K103N and Y181C[1].
Ulonivirine exhibits in vitro antiviral activity against common HIV-1 NNRTI resistance-associated variants in an unspecified cell-based system[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1591823-76-5
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Appearance Solid
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Molecular Weight 491.73
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Formula C18H8ClF6N5O3
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Color White to light yellow
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SMILES
N#CC1=CC(Cl)=CC(OC2=C(C(F)(F)F)N=CN(CC3=NNC(C(C(F)(F)F)=C3)=O)C2=O)=C1
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Synonyms
MK-8507
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 250 mg/mL (508.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.08 mg/mL (4.23 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Schürmann D, et al. Single Oral Doses of MK-8507, a Novel Non-Nucleoside Reverse Transcriptase Inhibitor, Suppress HIV-1 RNA for a Week. J Acquir Immune Defic Syndr. 2022;89(2):191-198. [Content Brief]
[2]. Gillespie G, et al. Fluoride Pharmacokinetics in Urine and Plasma Following Multiple Doses of MK-8507, an Investigational, Oral, Once-Weekly Nonnucleoside Reverse Transcriptase Inhibitor. J Clin Pharmacol. 2022;62(2):199-205. [Content Brief]
[3]. Ankrom W, et al. Pharmacokinetic and Safety Profile of the Novel HIV Nonnucleoside Reverse Transcriptase Inhibitor MK-8507 in Adults without HIV. Antimicrob Agents Chemother. 2021;65(12):e0093521. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.0336 mL | 10.1682 mL | 20.3364 mL | 50.8409 mL |
| 5 mM | 0.4067 mL | 2.0336 mL | 4.0673 mL | 10.1682 mL | |
| 10 mM | 0.2034 mL | 1.0168 mL | 2.0336 mL | 5.0841 mL | |
| 15 mM | 0.1356 mL | 0.6779 mL | 1.3558 mL | 3.3894 mL | |
| 20 mM | 0.1017 mL | 0.5084 mL | 1.0168 mL | 2.5420 mL | |
| 25 mM | 0.0813 mL | 0.4067 mL | 0.8135 mL | 2.0336 mL | |
| 30 mM | 0.0678 mL | 0.3389 mL | 0.6779 mL | 1.6947 mL | |
| 40 mM | 0.0508 mL | 0.2542 mL | 0.5084 mL | 1.2710 mL | |
| 50 mM | 0.0407 mL | 0.2034 mL | 0.4067 mL | 1.0168 mL | |
| 60 mM | 0.0339 mL | 0.1695 mL | 0.3389 mL | 0.8473 mL | |
| 80 mM | 0.0254 mL | 0.1271 mL | 0.2542 mL | 0.6355 mL | |
| 100 mM | 0.0203 mL | 0.1017 mL | 0.2034 mL | 0.5084 mL |
- Ulonivirine
- 1591823-76-5
- MK-8507
- MK8507
- MK 8507
- Reverse Transcriptase
- HIV
- E138G
- HIV-1 reverse transcriptase
- non-nucleoside HIV-1 reverse transcriptase inhibitor
- HIV-1 infection
- Y181C
- nonnucleoside reverse transcriptase inhibitor resistance-associated variants
- cytochrome P450 3A4
- K103N
- V179D
- HIV-1 RNA
- Inhibitor
- inhibitor
- inhibit