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TMC353121 

Cat. No. M30709
TMC353121  Structure
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Biological Activity

TMC353121 is a potent respiratory syncytial virus (RSV) fusion inhibitor with pEC50 of 9.9.

Chemical Information
Molecular Weight 558.71
Formula C32H42N6O3
CAS Number 857066-90-1
Form Solid
Solubility (25°C) DMSO 50 mg/mL (ultrasonic)
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] Gemechu Churiso, et al. Infect Drug Resist. Immunity Cell Responses to RSV and the Role of Antiviral Inhibitors: A Systematic Review

[2] Gilberto González-Parra, et al. J Theor Biol. Modeling of fusion inhibitor treatment of RSV in African green monkeys

[3] Gabriela Ispas, et al. PLoS One. Antiviral Activity of TMC353121, a Respiratory Syncytial Virus (RSV) Fusion Inhibitor, in a Non-Human Primate Model

[4] Marie-Claude Rouan, et al. Antimicrob Agents Chemother. Pharmacokinetics-pharmacodynamics of a respiratory syncytial virus fusion inhibitor in the cotton rat model

[5] Jean-François Bonfanti, et al. J Med Chem. Selection of a respiratory syncytial virus fusion inhibitor clinical candidate. 2. Discovery of a morpholinopropylaminobenzimidazole derivative (TMC353121)

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Keywords: TMC353121  supplier, RSV, inhibitors, activators


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