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Dolutegravir sodium

Cat. No. M4824

Dolutegravir sodium Structure

Synonym: GSK-1349572A, DTG

Size Price Availability Quantity
2mg USD 170 In stock
5mg USD 250 In stock
10mg USD 350 In stock
50mg USD 900 In stock
100mg USD 1400 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Dolutegravir (DTG) is a second-generation integrase strand transfer inhibitor (INSTI) and INSTIs are the latest class of potent anti-HIV drugs.Compared to the first generation INSTIs, raltegravir, and elvitegravir, Dolutegravir shows a limited cross-resistance profile.More interestingly, clinical resistance mutations to Dolutegravir in treatment-naive patents have not been observed to this date.Dolutegravir is a dominant strategy in the management of TN and TE patients when compared to recommended comparators.Dolutegravir had no effect on NGM/EE PK or PD. NGM/EE can be administered with DTG without dose adjustment.Dolutegravir is the integrase inhibitor of choice for rescue therapy in multiresistant HIV infection, both in integrase inhibitor-naïve patients and in those previously treated with raltegravir or elvitegravir.Treatment with DTG led to less HIV-1 genetic and amino-acid diversification over time, as compared to treatment with RAL or the absence of drug.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 441.36
Formula C20H18F2N3NaO5
CAS Number 1051375-19-9
Purity >99%
Solubility DMSO >80 mg/ml
Storage at -20°C
References

Cost-Effectiveness of Dolutegravir in HIV-1 Treatment-Naive and Treatment-Experienced Patients in Canada.
Despiégel N, et al. Infect Dis Ther. 2015 Jun 23. PMID: 26099626.

Will drug resistance against dolutegravir in initial therapy ever occur?
Wainberg MA, et al. Front Pharmacol. 2015 Apr 29;6:90. PMID: 25972810.

Dolutegravir Has No Effect on the Pharmacokinetics of Oral Contraceptives With Norgestimate and Ethinyl Estradiol.
Song IH, et al. Ann Pharmacother. 2015 Jul;49(7):784-9. PMID: 25862012.

[Efficacy of dolutegravir in treatment-experienced patients: the SAILING and VIKING trials].
Moreno S, et al. Enferm Infecc Microbiol Clin. 2015 Mar;33 Suppl 1:26-30. PMID: 25858609.

Dolutegravir inhibits HIV-1 Env evolution in primary human cells.
Mesplède T, et al. AIDS. 2015 Mar 27;29(6):659-65. PMID: 25849829.

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Keywords: Dolutegravir sodium, GSK-1349572A, DTG supplier, HIV Protease, inhibitors

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