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Dolutegravir sodium

Cat. No. M4824
Dolutegravir sodium Structure

GSK-1349572A, DTG

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 81  USD90 In stock
2mg USD 45  USD50 In stock
5mg USD 81  USD90 In stock
10mg USD 135  USD150 In stock
50mg USD 531  USD590 In stock
100mg USD 810  USD900 In stock
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Quality Control
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 441.36
Formula C20H18F2N3NaO5
CAS Number 1051375-19-9
Purity 98.36%
Solubility DMSO >4 mg/ml
Storage at -20°C

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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