1. Metabolic Enzyme/Protease
    Anti-infection
  2. HIV Integrase
    HIV

Dolutegravir (Synonyms: S/GSK1349572; GSK1349572)

Cat. No.: HY-13238 Purity: 99.54%
Data Sheet SDS Handling Instructions

Dolutegravir is an inhibitor of HIV-1 integrase-catalyzed strand transfer with IC50 of 2.7 nM.

For research use only. We do not sell to patients.
Dolutegravir Chemical Structure

Dolutegravir Chemical Structure

CAS No. : 1051375-16-6

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10 mM * 1 mL in DMSO $99 In-stock
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10 mg $160 In-stock
50 mg $490 In-stock
100 mg $720 In-stock
200 mg $1100 In-stock
500 mg $1950 In-stock
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Other Forms of Dolutegravir:

    Dolutegravir purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2016 Jul 21;39(2):639-650.

    Arithmetic means±SEM (n=19) of erythrocyte annexin-V-binding following incubation for 48 hours to Ringer solution without (white bar) or with (black bars) Dolutegravir (4.77-19.08 µM). For comparison, the effect of the solvent DMSO is shown (grey bar).
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Dolutegravir is an inhibitor of HIV-1 integrase-catalyzed strand transfer with IC50 of 2.7 nM.

    IC50 & Target

    IC50: 2.7 nM (HIV-1 integrase)[1]

    In Vitro

    The EC50 of Dolutegravir (S/GSK1349572) against HIV-1 is 0.51 nM in PBMCs, 0.71 nM in MT-4 cells, and 2.2 nM in the PHIV assay, which uses a pseudotyped self-inactivating virus. The 50% cytotoxic concentrations (CC50) for Dolutegravir in proliferating IM-9, U-937, MT-4, and Molt-4 cells are 4.8, 7.0, 14, and 15 μM, respectively. In unstimulated and stimulated PBMCs, the CC50 are 189 μM and 52 μM, respectively. Based on the EC50 of Dolutegravir against HIV-1 in PBMCs (i.e., 0.51 nM), this translates to a cell-based therapeutic index of at least 9,400[1].

    In Vivo

    Following a single intravenous (IV) administration of Dolutegravir, the plasma clearance is low in rats (0.23 mL/min/kg) and monkeys (2.12 mL/min/kg). The half-lives in the rat and monkey are similar, approximately 6 h, and the steady-state volume of distribution (VSS) is low. Following oral administration, Dolutegravir is rapidly absorbed with a high oral bioavailability when administered as a solution to fasted male rats and a single monkey (75.6 and 87.0%, respectively). Dolutegravir exposure (Cmax and AUC) increased with increasing dose following oral administration of a suspension to non-fasted rats up to 250 mg/kg and non-fasted monkeys up to 50 mg/kg, although the increase is less than proportional[2].

    Clinical Trial
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    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.3845 mL 11.9224 mL 23.8447 mL
    5 mM 0.4769 mL 2.3845 mL 4.7689 mL
    10 mM 0.2384 mL 1.1922 mL 2.3845 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [1]

    Dolutegravir (S/GSK1349572) is dissolved in stock solutions, and then diluted with appropriate media before use[1].

    In vitro growth inhibition (cytotoxicity) studies are conducted with S/GSK1349572 (0.16, 0.8, 4, and 20 nM) in proliferating human leukemic and lymphomic cell lines (IM-9, U-937, MT-4, and Molt-4) as well as in stimulated and unstimulated human PBMCs. ATP levels are quantified by using the CellTiter-Glo luciferase reagent to measure the ability of a compound to inhibit cell growth as an indicator of the compound's potential for cytotoxicity[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    Dolutegravir (S/GSK1349572) is formulated as a solution in N,N-dimethylacetamide and diluted with 50 mM N-methylglucamine in 3% mannitol (intravenous)[2].
    Dolutegravir (S/GSK1349572) is formulated as a solution in D:Solutol:50 mM N-methylglucamine in 3% mannitol (1:1:8, v:w:v) (orally administered to fasted rats and monkeys)[2].
    Dolutegravir (S/GSK1349572) is formulated as a suspension in 0.5% hydroxypropyl methylcellulose (HPMC)/0.1% polyoxyethylene sorbitan monooleate (Tween 80) (orally administered to non-fasted rats and monkeys)[2].

    For rat and monkey PK studies, Dolutegravir is administered as the free acid or the sodium salt. All doses are presented in terms of the free acid. Dolutegravir is administered by intravenous (IV) short-term (within 2 min) bolus (1 mg/kg) to three male rats and two male monkeys. For single oral administration, Dolutegravir as a solution (5 mg/kg) is administered to three fasted male rats and two fasted male monkeys. Dolutegravir is administered as single oral doses of 5, 50, 100, and 250 mg/kg to non-fasted male rats (n=2/dose level) and 3, 10, and 50 mg/kg to non-fasted female monkeys. For intravenous administration, blood samples are collected from rats (0.2 mL via jugular vein cannula) and monkeys (approximately 0.2 or 0.5 mL via saphenous vein in a hindlimb) into Na2EDTA-treated syringes at 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, and 24 h. For oral administration, samples are collected at 0.25 (rats only), 0.5, 1, 2, 4, 6 [rats (solution and suspension) and monkey (solution only)], 8, and 24 h. Following collection, the blood is immediately put on wet ice and then centrifuged within an hour at 1740 g for 10 min at 4°C to obtain plasma. All samples are stored at approximately -20°C or colder prior to analysis by using a method based on protein precipitation and LC-MS/MS analysis. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    419.38

    Formula

    C₂₀H₁₉F₂N₃O₅

    CAS No.

    1051375-16-6

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: 10 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Product Name:
    Dolutegravir
    Cat. No.:
    HY-13238
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