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Darunavir

Cat. No. M6094
Darunavir Structure
Synonym:

TMC114; TMC-114; TMC 114

Size Price Availability Quantity
5mg USD 90  USD100 In stock
10mg USD 144  USD160 In stock
50mg USD 297  USD330 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Darunavir displays potent activity against HIV strains resistant to other available protease inhibitor. Darunavir inhibits P-glycoprotein-mediated efflux of calcein-acetoxymethyl ester in L-MDR1 cells with the inhibitory potency of 121 mM. Darunavir is a protein inhibits that mimics the phenylalanine sequences at positions 167 and 168 of the gag-pol polypeptide and binds to the active sites of the HIV protease, thereby inhibiting its activity. Darunavir blocks the infectivity and replication of each of the HIV-1 variants at concentrations up to 5 μM. Darunavir shows strong ARV activity against a selected panel of 19 recombinant clinical isolates carrying multiple protease mutations conferring resistance to an average of five other protien inhibitors. Darunavir inhibits 75% of 1501 PI-resistant viruses tested with a half maximal effective concentration (EC50) of < 10 nM.

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 547.66
Formula C27H37N3O7S
CAS Number 206361-99-1
Purity >98%
Solubility 10 mM in DMSO
Storage at -20°C
References

Once-daily dolutegravir versus darunavir plus ritonavir for treatment-naive adults with HIV-1 infection (FLAMINGO): 96 week results from a randomised, open-label, phase 3b study.
Molina JM, et al. Lancet HIV. 2015 Apr;2(4):e127-36. PMID: 26424673.

Darunavir: A Review in Pediatric HIV-1 Infection.
Keating GM Paediatr Drugs. 2015 Oct;17(5):411-21. PMID: 26323490.

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Keywords: Darunavir, TMC114; TMC-114; TMC 114 supplier, HIV Protease, inhibitors

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