| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
GS-6207 targets the HIV-1 capsid protein, a structural protein that forms the conical core of the viral particle. The capsid protein is essential for multiple stages of the viral life cycle, including reverse transcription, nuclear import, and viral assembly. GS-6207 binds to the capsid protein and disrupts its function, inhibiting HIV-1 replication. By targeting a highly conserved viral protein, the compound has the potential to be effective against multiple HIV-1 strains.
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| ln Vitro |
In vitro, GS-6207 potently inhibits HIV-1 replication in cell culture. The compound demonstrates activity against a broad range of HIV-1 isolates, including strains resistant to other classes of antiretroviral drugs. GS-6207 inhibits viral capsid function, blocking uncoating and nuclear import of the viral genome, which are critical steps for HIV-1 replication.
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| ln Vivo |
In vivo, GS-6207 has been evaluated in preclinical models and clinical trials for HIV treatment. As a capsid inhibitor, it demonstrates potent antiviral activity and has shown promise in clinical studies. The compound's unique mechanism of action and potency against resistant strains make it a valuable addition to the HIV treatment armamentarium.
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| Enzyme Assay |
In vitro antiviral assays for HIV-1 inhibition are performed using HIV-1-infected cell lines such as MT-4 cells or primary human CD4+ T cells. Cells are infected with HIV-1 in the presence of varying concentrations of GS-6207. Viral replication is assessed by measuring p24 antigen production by ELISA or by quantifying viral RNA by qPCR. IC₅₀ values are calculated from dose-response curves.
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| Cell Assay |
Cellular assays are performed using HIV-1-susceptible cell lines. Cells are treated with GS-6207 at various concentrations and infected with HIV-1. The compound's ability to inhibit viral replication is assessed by measuring p24 antigen levels in culture supernatants. Cytotoxicity is evaluated using MTT or CellTiter-Glo assays to determine the selectivity index.
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| Animal Protocol |
In vivo studies are conducted in humanized mouse models of HIV-1 infection or in clinical trials. GS-6207 is administered subcutaneously or intravenously at various doses. Viral load is measured in plasma by qPCR, and CD4+ T cell counts are monitored. The compound's pharmacokinetic profile and antiviral efficacy are assessed in these studies.
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| ADME/Pharmacokinetics |
GS-6207 (molecular weight 958.34, formula C₄₁H₃₆ClF₈N₇O₅S₂) is a small-molecule compound. It has a LogP of 6.4, indicating high lipophilicity. The compound is typically administered subcutaneously or intravenously in clinical settings. Its physicochemical properties support long-acting parenteral administration.
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| Toxicity/Toxicokinetics |
Preclinical and clinical toxicity studies have evaluated GS-6207 in animals and humans. As an HIV capsid inhibitor, its toxicity profile is related to its antiviral mechanism. Clinical studies have demonstrated a favorable safety profile, with the compound being generally well-tolerated. No significant toxicity has been reported at therapeutic doses.
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| References | |
| Additional Infomation |
GS-6207 (GS-CA1) is a first-in-class HIV-1 capsid inhibitor developed by Gilead Sciences. Its mechanism involves targeting the HIV-1 capsid protein, disrupting viral uncoating and nuclear import. The compound represents a new class of antiretroviral agents with a unique mechanism of action and potency against resistant strains. GS-6207 has been evaluated in clinical trials for HIV treatment and has shown promising results. It has not received regulatory approval for clinical use at this time.
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| Molecular Formula |
C41H36CLF8N7O5S2
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|---|---|
| Molecular Weight |
958.3387
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| Exact Mass |
957.178
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| CAS # |
2189684-45-3
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| PubChem CID |
134262970
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| Appearance |
White to light yellow solid powder
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| LogP |
6.4
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
17
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
64
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| Complexity |
2030
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| Defined Atom Stereocenter Count |
3
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| SMILES |
ClC1C([H])=C([H])C(=C2C=1C(=NN2C([H])([H])C([H])(F)F)N([H])S(C1([H])C([H])([H])C1([H])[H])(=O)=O)C1C([H])=C([H])C(C#CC(C([H])([H])[H])(C([H])([H])[H])S(C([H])([H])[H])(=O)=O)=NC=1[C@@]([H])(C([H])([H])C1C([H])=C(C([H])=C(C=1[H])F)F)N([H])C(C([H])([H])N1C2=C(C(C([H])(F)F)=N1)[C@]1([H])C([H])([H])[C@]1([H])C2(F)F)=O
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| InChi Key |
CPCUUUACFKQOHY-GKRYNVPLSA-N
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| InChi Code |
InChI=1S/C41H36ClF8N7O5S2/c1-40(2,63(3,59)60)11-10-22-4-7-24(25-8-9-28(42)33-36(25)56(17-30(45)46)54-39(33)55-64(61,62)23-5-6-23)34(51-22)29(14-19-12-20(43)15-21(44)13-19)52-31(58)18-57-37-32(35(53-57)38(47)48)26-16-27(26)41(37,49)50/h4,7-9,12-13,15,23,26-27,29-30,38H,5-6,14,16-18H2,1-3H3,(H,52,58)(H,54,55)/t26-,27+,29-/m0/s1
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| Chemical Name |
N-[(1S)-1-[3-[4-chloro-3-(cyclopropylsulfonylamino)-1-(2,2-difluoroethyl)indazol-7-yl]-6-(3-methyl-3-methylsulfonylbut-1-ynyl)pyridin-2-yl]-2-(3,5-difluorophenyl)ethyl]-2-[(2S,4R)-9-(difluoromethyl)-5,5-difluoro-7,8-diazatricyclo[4.3.0.02,4]nona-1(6),8-dien-7-yl]acetamide
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| Synonyms |
GS-6207; GS6207; GS 6207
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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 (~52.17 mM)
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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 | 1.0435 mL | 5.2174 mL | 10.4347 mL | |
| 5 mM | 0.2087 mL | 1.0435 mL | 2.0869 mL | |
| 10 mM | 0.1043 mL | 0.5217 mL | 1.0435 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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