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Rilpivirine (R278474)

Cat. No. M2980
Rilpivirine (R278474) Structure
Synonym:

R278474, TMC278

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 60  USD60 In stock
5mg USD 50  USD50 In stock
10mg USD 90  USD90 In stock
50mg USD 270  USD270 In stock
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Quality Control & Documentation
Biological Activity

Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine (R278474) inhibits 81% of clinical isolates (about 1200 recombinant clinical isolates) at a 50% inhibitory concentration (EC50) less than 1 nM, and inhibits 94% at EC50 less than 10 nM.

Chemical Information
Molecular Weight 366.42
Formula C22H18N6
CAS Number 500287-72-9
Solubility (25°C) DMSO 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] A Markham. Cabotegravir Plus Rilpivirine: First Approval

[2] Susan Swindells, et al. Long-Acting Cabotegravir and Rilpivirine for Maintenance of HIV-1 Suppression

[3] Chloe Orkin, et al. Long-Acting Cabotegravir and Rilpivirine after Oral Induction for HIV-1 Infection

[4] No authors listed. Rilpivirine

[5] No authors listed. Rilpivirine

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Keywords: Rilpivirine (R278474), R278474, TMC278 supplier, Reverse Transcriptase, inhibitors, activators


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