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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
GSK2838232 is a potent and selective inhibitor of HIV-1 maturation, with an IC₉₀ of 6.4 nM. It is active against a variety of HIV isolates resistant to bevirimat (PA-457), a first-generation maturation inhibitor. The compound inhibits HIV reverse transcriptase activity.
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| ln Vitro |
In vitro, GSK2838232 demonstrates potent antiviral activity against multiple HIV-1 strains, including those resistant to other therapies. It exhibits strong activity with an IC₉₀ of 6.4 nM against HIV-1 and is active against bevirimat-resistant isolates.
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| ln Vivo |
In vivo, GSK2838232 has demonstrated efficacy in reducing viral loads in preclinical models, which could be pivotal in managing chronic viral infections. The safety, tolerability, and pharmacokinetic profile have been assessed in healthy subjects.
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| Enzyme Assay |
For non-cellular in vitro assays, GSK2838232 is evaluated for its inhibition of HIV-1 maturation using biochemical assays that measure the processing of the Gag polyprotein. The compound's activity against HIV reverse transcriptase may also be assessed in enzyme inhibition assays.
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| Cell Assay |
For in vitro cellular assays, GSK2838232 is tested in HIV-1-infected cell cultures. Cells are infected with HIV-1 and treated with serial dilutions of the compound. Antiviral activity is measured by quantifying viral replication, p24 antigen production, or infectivity reduction to determine IC₉₀ values.
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| Animal Protocol |
For in vivo animal studies, GSK2838232 has been evaluated in preclinical models of HIV infection to assess efficacy in reducing viral loads. The compound has also been assessed in healthy human subjects for safety, tolerability, and pharmacokinetics.
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| ADME/Pharmacokinetics |
The safety, tolerability, and pharmacokinetic profile of GSK2838232 have been assessed in healthy subjects. These studies indicate favorable pharmacokinetic properties for oral administration, supporting its development as a therapeutic for chronic HIV infection.
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| Toxicity/Toxicokinetics |
GSK2838232 has been evaluated for safety and tolerability in healthy subjects. As a second-generation HIV maturation inhibitor, it is designed to have improved safety and efficacy compared to first-generation inhibitors. Comprehensive toxicology studies would be required for regulatory approval.
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| References | |
| Additional Infomation |
GSK2838232 is a second-generation inhibitor of HIV-1 maturation with an IC₉₀ of 6.4 nM, active against a variety of HIV isolates resistant to bevirimat. It is being developed for the treatment of chronic HIV infection and has demonstrated efficacy in reducing viral loads. The safety, tolerability, and pharmacokinetic profile have been assessed in healthy subjects.
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| Molecular Formula |
C48H73CLN2O6
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|---|---|
| Molecular Weight |
809.56
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| Exact Mass |
808.515
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| CAS # |
1443460-91-0
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| PubChem CID |
71580991
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
817.1±65.0 °C at 760 mmHg
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| Flash Point |
448.0±34.3 °C
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| Vapour Pressure |
0.0±3.1 mmHg at 25°C
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| Index of Refraction |
1.577
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| LogP |
11.63
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
57
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| Complexity |
1560
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| Defined Atom Stereocenter Count |
9
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| SMILES |
CC(C)C1=C2[C@H]3CC[C@@H]4[C@]5(CC[C@@H](C([C@@H]5CC[C@]4([C@@]3(CC[C@]2(CC1=O)[C@H](CN(CCN(C)C)CC6=CC=C(C=C6)Cl)O)C)C)(C)C)OC(=O)CC(C)(C)C(=O)O)C
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| InChi Key |
MEOWKUXNVNJAMY-PZFKGGKESA-N
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| InChi Code |
InChI=1S/C48H73ClN2O6/c1-30(2)40-34(52)26-48(37(53)29-51(25-24-50(10)11)28-31-12-14-32(49)15-13-31)23-22-46(8)33(41(40)48)16-17-36-45(7)20-19-38(57-39(54)27-43(3,4)42(55)56)44(5,6)35(45)18-21-47(36,46)9/h12-15,30,33,35-38,53H,16-29H2,1-11H3,(H,55,56)/t33-,35+,36-,37+,38+,45+,46-,47-,48+/m1/s1
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| Chemical Name |
4-[[(3aR,5aR,5bR,7aR,9S,11aR,11bR,13aS)-3a-[(1R)-2-[(4-chlorophenyl)methyl-[2-(dimethylamino)ethyl]amino]-1-hydroxyethyl]-5a,5b,8,8,11a-pentamethyl-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3H-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid
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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) |
DMSO: ≥ 50 mg/mL (61.76 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (3.09 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with heating and sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.09 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (3.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2352 mL | 6.1762 mL | 12.3524 mL | |
| 5 mM | 0.2470 mL | 1.2352 mL | 2.4705 mL | |
| 10 mM | 0.1235 mL | 0.6176 mL | 1.2352 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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