| Size | Price | Stock | Qty |
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| 5mg |
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| 50mg |
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Cabotegravir Sodium is an HIV integrase inhibitor (IC50 = 2.5 nM for HIVADA) with anti-HIV activity. Cabotegravir sodium is mainly metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1, and exhibits low potential to interact with other antiretroviral drugs (ARVs).
| ln Vitro |
In vitro, cabotegravir (GSK-1265744) blocks the strand transfer reaction that HIV-1 integrase catalyzes at an IC50 of 3.0 nM. The antiviral EC50 for NL432 and HIV-1 Ba-L in PBMCs was 0.34 nM and 0.22 nM, respectively. With an EC50 of 0.5 nM in a PHIV experiment employing type A self-inactivating virus, the EC50 in MT-4 cells was determined to be 0.57 nM using CellTiter-Glo and 1.3 nM using MTT [3].
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| ln Vivo |
The half-phase drop of Cabotegravir in mice is as long as 54 days [1]. Cabotegravir (25 or 50 mg/kg; iv; single or twice dosage) protects against SIVmac251 infection in macaques (Macaques) [4].
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| Cell Assay |
Viability assay[3]
Cell Types: MT-4 Cell Tested Concentrations: 0-32 nM Incubation Duration: 4 or 5 days Experimental Results: Displayed antiviral activity with EC50 of 1.3 nM. |
| References |
[1]. Zhou T, et al. Creation of a nanoformulated cabotegravir prodrug with improved antiretroviral profiles. Biomaterials. 2018 Jan;151:53-65.
[2]. Reese MJ, et al. Drug interaction profile of the HIV integrase inhibitor cabotegravir: assessment from in vitro studies and a clinical investigation with midazolam. Xenobiotica. 2016;46(5):445-56. [3]. Yoshinaga T, et al. Antiviral characteristics of GSK1265744, an HIV integrase inhibitor dosed orally or by long-acting injection. Antimicrob Agents Chemother. 2015 Jan;59(1):397-406. [4]. Andrews CD, et al. Cabotegravir long acting injection protects macaques against intravenous challenge with SIVmac251. AIDS. 2017 Feb 20;31(4):461-467. |
| Molecular Formula |
C19H16N3O5F2-.NA+
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|---|---|
| Molecular Weight |
427.33404
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| CAS # |
1051375-13-3
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| Related CAS # |
Cabotegravir;1051375-10-0;Cabotegravir-d3 sodium
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| SMILES |
C[C@H]1CO[C@@H]2CN3C=C(C(NCC4=C(F)C=C(F)C=C4)=O)C(C([O-])=C3C(N12)=O)=O.[Na+]
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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 : ~6.25 mg/mL (~14.63 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 | 2.3401 mL | 11.7006 mL | 23.4011 mL | |
| 5 mM | 0.4680 mL | 2.3401 mL | 4.6802 mL | |
| 10 mM | 0.2340 mL | 1.1701 mL | 2.3401 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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