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Raltegravir

Cat. No. M2595
Raltegravir Structure
Synonym:

MK-0518

Size Price Availability Quantity
5mg USD 68  USD68 In stock
10mg USD 115  USD115 In stock
50mg USD 340  USD340 In stock
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Quality Control
Biological Activity

Raltegravir (MK-0518) is a novel HIV-1 integrase strand transfer inhibitor with potent in vitro activity against wild-type and multi-class resistant HIV-1 virus (in vitro IC95 for HIV-1 in 50% normal human serum = 33 nM). Raltegravir induces viro-immunological improvement of nonhuman primates with progressing SIVmac251 infection. Raltegravir is administered orally every 12h and does not require boosting with low-dose ritonavir (RTV) to achieve therapeutic concentrations.

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 444.42
Formula C20H21FN6O5
CAS Number 518048-05-0
Purity >99%
Solubility DMSO 80 mg/mL
Storage at -20°C
References

[1] Anton Pozniak, et al. Raltegravir in patients with tuberculosis

[2] Rosa de Miguel, et al. A safety evaluation of raltegravir for the treatment of HIV

[3] Emma D Deeks. Raltegravir Once-Daily Tablet: A Review in HIV-1 Infection

[4] Francois Clavel. HIV resistance to raltegravir

[5] F Cossarini, et al. Raltegravir in treatment naive patients

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Keywords: Raltegravir, MK-0518 supplier, Integrase, inhibitors

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