| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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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. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation No published information is available on the use of cabotegravir during breastfeeding. Achieving and maintaining viral suppression with antiretroviral therapy decreases breastfeeding transmission risk to less than 1%, but not zero. Individuals with HIV who are on antiretroviral therapy with a sustained undetectable viral load and who choose to breastfeed should be supported in this decision. If a viral load is not suppressed, banked pasteurized donor milk or formula is recommended. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
| References |
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| Additional Infomation |
Cabotegravir sodium is an organic sodium salt that is the monosodium salt of cabotegravir. Used for treatment of HIV-1. It has a role as a HIV-1 integrase inhibitor. It contains a cabotegravir(1-).
Cabotegravir is a prescription medicine approved by the U.S. Food and Drug Administration (FDA). It is approved as two different dosage forms under two different brand names for the following uses: Cabotegravir oral tablet (brand name: Vocabria) For the short-term treatment of HIV infection in adults and adolescents 12 years of age and older who weigh at least 77 lb (35 kg) and who meet certain requirements, as determined by a health care provider. When used for HIV treatment, cabotegravir is always used with the HIV medicine rilpivirine (brand name: Edurant). For short-term PrEP to reduce the risk of HIV infection in adults and adolescents who weigh at least 77 lb (35 kg), are HIV negative, and are at risk of getting HIV. Oral cabotegravir for PrEP should always be used in combination with safer sex practices, such as using condoms, to reduce the risk of getting other sexually transmitted infections. Long-acting injectable cabotegravir (brand name: Apretude) For HIV PrEP to reduce the risk of HIV infection in adults and adolescents who weigh at least 77 lb (35 kg), are HIV negative, and are at risk of getting HIV. Long-acting injectable cabotegravir for PrEP should always be used in combination with safer sex practices, such as using condoms, to reduce the risk of getting other sexually transmitted infections. Drug Indication Vocabria tablets are indicated in combination with rilpivirine tablets for the short-term treatment of Human Immunodeficiency Virus type 1 (HIV-1) infection in adults who are virologically suppressed (HIV-1 RNA |
| Molecular Formula |
C19H16N3O5F2-.NA+
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|---|---|
| Molecular Weight |
427.33404
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| Exact Mass |
427.095
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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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| PubChem CID |
46215800
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
30
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| Complexity |
820
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C[C@H]1CO[C@H]2N1C(=O)C3=C(C(=O)C(=CN3C2)C(=O)NCC4=C(C=C(C=C4)F)F)[O-].[Na+]
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| InChi Key |
AEZBWGMXBKPGFP-KIUAEZIZSA-M
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| InChi Code |
InChI=1S/C19H17F2N3O5.Na/c1-9-8-29-14-7-23-6-12(16(25)17(26)15(23)19(28)24(9)14)18(27)22-5-10-2-3-11(20)4-13(10)21;/h2-4,6,9,14,26H,5,7-8H2,1H3,(H,22,27);/q;+1/p-1/t9-,14+;/m0./s1
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| Chemical Name |
sodium;(3R,6S)-12-[(2,4-difluorophenyl)methylcarbamoyl]-6-methyl-8,11-dioxo-4-oxa-1,7-diazatricyclo[7.4.0.03,7]trideca-9,12-dien-10-olate
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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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