Dolutegravir sodium
Based on 35 publication(s) in Google Scholar
Dolutegravir sodium (S/GSK1349572 sodium) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir sodium (S/GSK1349572 sodium) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir sodium (S/GSK1349572 sodium) retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.97%
- CAS 番号: 1051375-19-9
- 分子式: C20H18F2N3NaO5
- 分子量:441.36
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
MedChemExpress(MCE)の使用を引用している文献 Dolutegravir sodium
More- Science. 2020 Feb 14;367(6479):806-810. [Abstract]
- Cell. 2025 Sep 4;188(18):4896-4912.e19. [Abstract]
- Cell Rep Med. 2024 Aug 26:101702. [Abstract]
- Cell Rep Med. 2024 Jul 2:101643. [Abstract]
- Sci Adv. 2025 Sep 12;11(37):eadz8980. [Abstract]
- Biochem Pharmacol. 2024 Feb:220:116010. [Abstract]
- Life Sci. 2022 Nov 1:308:120948. [Abstract]
- J Neuroimmune Pharmacol. 2021 Mar;16(1):159-168. [Abstract]
- Pharmaceuticals (Basel). 2022 Feb 18;15(2):242. [Abstract]
- Int J Antimicrob Agents. 2019 Dec;54(6):814-819. [Abstract]
- ASN Neuro. 2026;18(1):2647877. [Abstract]
- Antiviral Res. 2025 Sep 11:106283. [Abstract]
- FASEB J. 2025 Feb 28;39(4):e70377. [Abstract]
- J Antimicrob Chemother. 2026 Feb 2;81(3):dkag033. [Abstract]
- J Infect Dis. 2022 Nov 28;226(11):1992-2001. [Abstract]
- Anal Bioanal Chem. 2018 Nov;410(29):7773-7781. [Abstract]
- Open Forum Infect Dis. 2024 Nov 29;12(1):ofae705. [Abstract]
- Viruses. 2024 Oct 13;16(10):1607. [Abstract]
- Viruses. 2021 Jan 18;13(1):131. [Abstract]
- Drug Metab Dispos. 2019 Jul;47(7):768-778. [Abstract]
- Drug Metab Dispos. 2019 May;47(5):535-544. [Abstract]
- Toxicol Appl Pharmacol. 2019 Apr 1:368:18-25. [Abstract]
- Antivir Ther. 2017;22(8):645-657. [Abstract]
- PLoS One. 2020 Jan 23;15(1):e0226924. [Abstract]
- Biochem Biophys Res Commun. 2017 Jul 1;488(3):433-438. [Abstract]
- Cell Physiol Biochem. 2016 Jul 21;39(2):639-650. [Abstract]
- J Clin Pharmacol. 2019 Sep;59 Suppl 1:S42-S55. [Abstract]
- STAR Protoc. 2026 Jun 19;7(2):104604. [Abstract]
- bioRxiv. 2026 Apr 21.
- University of Debrecen. 2023.
- Biomed Pharmacother. 2025 Nov 28:193:118831. [Abstract]
- bioRxiv. 2025 May 18:2025.05.17.654662. [Abstract]
- Res Sq. 2024 May 24.
- Preprints. 2024 Apr 23.
- PeerJ Physical Chemistry. 2019, 1:e6.
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Bio/Physico-chemical Assay
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Cell Proliferation/Viability Assay
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Cell Imaging/Staining
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RT-PCR
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ELISA
生物活性
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HIV-1 |
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| IM-9 | CC50 |
4.8 μM
Compound: S/GSK-1349572
|
Cytotoxicity against human IM9 cells after 2 days by Cell titer Glo luminescent assay
Cytotoxicity against human IM9 cells after 2 days by Cell titer Glo luminescent assay
|
[PMID: 21115794] |
| MOLT-4 | CC50 |
15 μM
Compound: S/GSK-1349572
|
Cytotoxicity against human MOLT4 cells after 2 days by Cell titer Glo luminescent assay
Cytotoxicity against human MOLT4 cells after 2 days by Cell titer Glo luminescent assay
|
[PMID: 21115794] |
| MT2 | EC50 |
0.26 nM
Compound: S/GSK-1349572
|
Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 14 passages measured after 2 to 3 days by PCR
Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 14 passages measured after 2 to 3 days by PCR
|
[PMID: 21115794] |
| MT2 | EC50 |
0.26 nM
Compound: S/GSK-1349572
|
Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 28 passages measured after 2 to 3 days by PCR
Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 28 passages measured after 2 to 3 days by PCR
|
[PMID: 21115794] |
| MT2 | EC50 |
0.26 nM
Compound: S/GSK-1349572
|
Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 42 passages measured after 2 to 3 days by PCR
Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 42 passages measured after 2 to 3 days by PCR
|
[PMID: 21115794] |
| MT2 | EC50 |
0.26 nM
Compound: S/GSK-1349572
|
Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect measured after 2 to 3 days by PCR
Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect measured after 2 to 3 days by PCR
|
[PMID: 21115794] |
| MT2 | EC50 |
1.3 nM
Compound: S/GSK-1349572
|
Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase S153Y/L101I/T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 112 passages measured after 2 to 3 da
Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase S153Y/L101I/T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 112 passages measured after 2 to 3 da
|
[PMID: 21115794] |
| MT2 | EC50 |
1.3 nM
Compound: S/GSK-1349572
|
Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase S153Y/L101I/T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 70 passages measured after 2 to 3 day
Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase S153Y/L101I/T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 70 passages measured after 2 to 3 day
|
[PMID: 21115794] |
| MT2 | EC50 |
1.3 nM
Compound: S/GSK-1349572
|
Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase S153Y/L101I/T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 84 passages measured after 2 to 3 day
Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase S153Y/L101I/T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 84 passages measured after 2 to 3 day
|
[PMID: 21115794] |
| MT2 | EC50 |
1.3 nM
Compound: S/GSK-1349572
|
Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase S153Y/L101I/T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 98 passages measured after 2 to 3 day
Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase S153Y/L101I/T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 98 passages measured after 2 to 3 day
|
[PMID: 21115794] |
| MT2 | EC50 |
1.3 nM
Compound: S/GSK-1349572
|
Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 56 passages measured after 2 to 3 days by PCR
Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 56 passages measured after 2 to 3 days by PCR
|
[PMID: 21115794] |
| MT4 | CC50 |
14 μM
Compound: S/GSK-1349572
|
Cytotoxicity against human MT4 cells after 2 days by Cell titer Glo luminescent assay
Cytotoxicity against human MT4 cells after 2 days by Cell titer Glo luminescent assay
|
[PMID: 21115794] |
| MT4 | EC50 |
0.36 nM
Compound: S/GSK-1349572
|
Antiviral activity against PI-resistant Human immunodeficiency virus 1 NL432 harboring nucleotide reverse transcriptase L24I/M46I/L63P/A71V/G73S/V82Tmutant infected in human MT4 cells after 2 to 3 days by reverse transcriptase activity
Antiviral activity against PI-resistant Human immunodeficiency virus 1 NL432 harboring nucleotide reverse transcriptase L24I/M46I/L63P/A71V/G73S/V82Tmutant infected in human MT4 cells after 2 to 3 days by reverse transcriptase activity
|
[PMID: 21115794] |
| MT4 | EC50 |
0.71 nM
Compound: S/GSK-1349572
|
Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as viral viability after 4 to 5 days by Cell titer Glo luminescent assay
Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as viral viability after 4 to 5 days by Cell titer Glo luminescent assay
|
[PMID: 21115794] |
| PBMC | CC50 |
189 μM
Compound: S/GSK-1349572
|
Cytotoxicity against PHA-stimulated human PBMC after 2 days by Cell titer Glo luminescent assay
Cytotoxicity against PHA-stimulated human PBMC after 2 days by Cell titer Glo luminescent assay
|
[PMID: 21115794] |
| PBMC | CC50 |
52 μM
Compound: S/GSK-1349572
|
Cytotoxicity against unstimulated human PBMC after 2 days by Cell titer Glo luminescent assay
Cytotoxicity against unstimulated human PBMC after 2 days by Cell titer Glo luminescent assay
|
[PMID: 21115794] |
| U-937 | CC50 |
7 μM
Compound: S/GSK-1349572
|
Cytotoxicity against human U937 cells after 2 days by Cell titer Glo luminescent assay
Cytotoxicity against human U937 cells after 2 days by Cell titer Glo luminescent assay
|
[PMID: 21115794] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1051375-19-9
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性状 Solid
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分子量 441.36
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分子式 C20H18F2N3NaO5
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Color Off-white to yellow
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SMILES
O=C(C1=CN(C2=C(O[Na])C1=O)C[C@]3([H])OCC[C@@H](C)N3C2=O)NCC4=CC=C(F)C=C4F
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別名
S/GSK1349572 sodium
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (35)
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Journal Impact Factor
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Most Recent
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Science
Structural basis of second-generation HIV integrase inhibitor action and viral resistance. [Abstract]2020 Feb 14;367(6479):806-810. PMID: 32001525 -
Cell
Combination antiretroviral therapy and MCL-1 inhibition mitigate HTLV-1 infection in vivo. [Abstract]2025 Sep 4;188(18):4896-4912.e19. PMID: 40645177 -
Cell Rep Med
Decoupling HIV-1 antiretroviral drug inhibition from plasma antibody activity to evaluate broadly neutralizing antibody therapeutics and vaccines. [Abstract]2024 Aug 26:101702. PMID: 39216479 -
Cell Rep Med
Combination of compound screening with an animal model identifies pentamidine to prevent Chlamydia trachomatis infection. [Abstract]2024 Jul 2:101643. PMID: 38981484
Dolutegravir sodium purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2024 Jul 2:101643. [Abstract]
Dose-response curves for Dolutegravir (0.5-13.5 μM) against Ct serovars E, F, and L2. POC represented the percentage of DMSO-treated control.
Dolutegravir sodium purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2024 Jul 2:101643. [Abstract]
Dolutegravir (13.5 μM) significantly blocked Ct growth in mice for genital chlamydia infection.
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Sci Adv
Elucidating the mechanism by which HIV-1 nucleocapsid mutations confer resistance to integrase strand transfer inhibitors. [Abstract]2025 Sep 12;11(37):eadz8980. PMID: 40938996
Dolutegravir sodium purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Sep 12;11(37):eadz8980. [Abstract]
Replication kinetics of the indicated NL4-3 variants of HIV-1 in the SupT1 T cell line in the absence or presence of Dolutegravir (DTG) (1-10 nM).
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Biochem Pharmacol
Divergent effects of the antiretroviral drugs, dolutegravir, tenofovir alafenamide, and tenofovir disoproxil fumarate, on human adipocyte function. [Abstract]2024 Feb:220:116010. PMID: 38154544
Dolutegravir sodium purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2024 Feb:220:116010. [Abstract]
10 μM Dolutegravir (DTG) (1-10 μM) significantly repressed the mRNA expression levels of the adipocyte identity markers, peroxisome proliferator-activated receptor-gamma (PPARG) and lipoprotein lipase (LPL), as well as solute carrier family 2, facilitated glucose transporter member 4 (SLC2A4, GLUT4), and the adipokine, adiponectin (ADIPOQ), but induced that of solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1, GLUT1) and leptin (LEP) in SGBS human adipocytes.
Dolutegravir sodium purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2024 Feb:220:116010. [Abstract]
The effects of Dolutegravir (DTG) (1-10 μM) on the releases of leptin and adiponectin to the cell culture medium of differentiating SGBS human adipocytes are shown.
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Life Sci
Differential effects of dolutegravir, bictegravir and raltegravir in adipokines and inflammation markers on human adipocytes. [Abstract]2022 Nov 1:308:120948. PMID: 36096241 -
J Neuroimmune Pharmacol
2021 Mar;16(1):159-168. PMID: 31338753 -
Pharmaceuticals (Basel)
Evaluation of the Potency of Anti-HIV and Anti-HCV Drugs to Inhibit P-Glycoprotein Mediated Efflux of Digoxin in Caco-2 Cell Line and Human Precision-Cut Intestinal Slices. [Abstract]2022 Feb 18;15(2):242. PMID: 35215354 -
Int J Antimicrob Agents
2019 Dec;54(6):814-819. PMID: 31479744 -
ASN Neuro
Exposure to Frontline Antiretroviral Dolutegravir Disrupts Oligodendrocyte Development Across Differentiation Stages. [Abstract]2026;18(1):2647877. PMID: 41904696 -
Antiviral Res
Differential effects of antiretroviral HIV integrase inhibitors on vascular cell adhesion molecules. [Abstract]2025 Sep 11:106283. PMID: 40945692 -
FASEB J
2025 Feb 28;39(4):e70377. PMID: 39985305 -
J Antimicrob Chemother
Cooperation between HIV-1 integrase natural polymorphism K156N and 3'PPT mutations in dolutegravir monotherapy failure. [Abstract]2026 Feb 2;81(3):dkag033. PMID: 41636646 -
J Infect Dis
Second-generation HIV integrase inhibitors induce differentiation dysregulation and exert toxic effects in human embryonic stem cell and mouse models. [Abstract]2022 Nov 28;226(11):1992-2001. PMID: 36124861 -
Anal Bioanal Chem
Development and validation of an LC-MS/MS assay for the quantification of dolutegravir extracted from human hair. [Abstract]2018 Nov;410(29):7773-7781. PMID: 30280227 -
Open Forum Infect Dis
Novel Dolutegravir and Lenacapavir Resistance Patterns in Human Immunodeficiency Virus Type 2 Infection: A Case Report. [Abstract]2024 Nov 29;12(1):ofae705. PMID: 39741997 -
Viruses
Efficacy of Integrase Strand Transfer Inhibitors and the Capsid Inhibitor Lenacapavir against HIV-2, and Exploring the Effect of Raltegravir on the Activity of SARS-CoV-2. [Abstract]2024 Oct 13;16(10):1607. PMID: 39459940 -
Viruses
Analysis and Molecular Determinants of HIV RNase H Cleavage Specificity at the PPT/U3 Junction. [Abstract]2021 Jan 18;13(1):131. PMID: 33477685 -
Drug Metab Dispos
A Systematic In Vitro Investigation of the Inhibitor Preincubation Effect on Multiple Classes of Clinically Relevant Transporters. [Abstract]2019 Jul;47(7):768-778. PMID: 31068368 -
Drug Metab Dispos
Mechanistic Assessment of Extrahepatic Contributions to Glucuronidation of Integrase Strand Transfer Inhibitors. [Abstract]2019 May;47(5):535-544. PMID: 30804050 -
Toxicol Appl Pharmacol
The inhibitory effect of antiretroviral drugs on the L-carnitine uptake in human placenta. [Abstract]2019 Apr 1:368:18-25. PMID: 30735677 -
Antivir Ther
Impact of CCR5, integrase and protease inhibitors on human endothelial cell function, stress, inflammation and senescence. [Abstract]2017;22(8):645-657. PMID: 28350300
Dolutegravir sodium purchased from MedChemExpress. Usage Cited in: Antivir Ther. 2017;22(8):645-657. [Abstract]
Dolutegravir (DTG) and MVC+DTG significantly increase the SIRT1 level by respectively, 9% and 18%.
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PLoS One
HIV antiretroviral drugs, dolutegravir, maraviroc and ritonavir-boosted atazanavir use different pathways to affect inflammation, senescence and insulin sensitivity in human coronary endothelial cells. [Abstract]2020 Jan 23;15(1):e0226924. PMID: 31971958 -
Biochem Biophys Res Commun
The inhibition process of HIV-1 integrase by diketoacids molecules: Understanding the factors governing the better efficiency of dolutegravir. [Abstract]2017 Jul 1;488(3):433-438. PMID: 28478035 -
Cell Physiol Biochem
2016 Jul 21;39(2):639-650. PMID: 27442249
Dolutegravir sodium purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2016 Jul 21;39(2):639-650. [Abstract]
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).
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J Clin Pharmacol
Characterization of the Ontogeny of Hepatic UDP-Glucuronosyltransferase Enzymes Based on Glucuronidation Activity Measured in Human Liver Microsomes. [Abstract]2019 Sep;59 Suppl 1:S42-S55. PMID: 31502688 -
STAR Protoc
Protocol to generate microglia-containing cerebral organoids to model HIV neuroinflammation. [Abstract]2026 Jun 19;7(2):104604. PMID: 42224077 -
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Biomed Pharmacother
Differential adipose tissue remodeling and metabolic effects of dolutegravir and bictegravir: implications for HIV therapy. [Abstract]2025 Nov 28:193:118831. PMID: 41317481 -
bioRxiv
Elucidating the Mechanism by Which HIV-1 Nucleocapsid Mutations Confer Resistance to Integrase Strand Transfer Inhibitors. [Abstract]2025 May 18:2025.05.17.654662. PMID: 41030995 -
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溶剤 & 溶解度
DMSO : 2 mg/mL (4.53 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
プロトコル
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (280 KB)
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SDS (398 KB)
- English - EN (398 KB)
- Français - FR (398 KB)
- Deutsch - DE (398 KB)
- Norwegian - NO (398 KB)
- Español - ES (398 KB)
- Swedish - SV (398 KB)
- Italian - IT (398 KB)
- Korean - KR (398 KB)
- Portuguese - PT (398 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Kobayashi M, et al. In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. Antimicrob Agents Chemother. 2011 Feb;55(2):813-21. [Content Brief]
[2]. Moss L, et al. The comparative disposition and metabolism of dolutegravir, a potent HIV-1 integrase inhibitor, in mice, rats, and monkeys. Xenobiotica. 2015 Jan;45(1):60-70. [Content Brief]
[3]. Hare S, et al. Structural and functional analyses of the second-generation integrase strand transfer inhibitor dolutegravir (S/GSK1349572). Mol Pharmacol. 2011 Oct;80(4):565-72. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2657 mL | 11.3286 mL | 22.6572 mL | 56.6431 mL |