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ABBV-4083

Cat. No. M21659
ABBV-4083 Structure
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Biological Activity

ABBV-4083 is a novel analog of Tylosin A that has potent anti-Wolbachia and anti-filarial activity.

Protocol (for reference only)
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models microfilariae-positive jirds
Formulation dissolved in 0.5% HPMC/0.02% Tween-80
Dosages 150 mg/kg QD using a volume of 5ml/kg
Administration PO
Chemical Information
Molecular Weight 1024.21
Formula C53H82FNO17
CAS Number 1809266-03-2
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] Alexandra Ehrens, et al. GMS Infect Dis. Current perspective of new anti-Wolbachial and direct-acting macrofilaricidal drugs as treatment strategies for human filariasis

[2] Kelly L Johnston, et al. Trends Parasitol. Anti-Wolbachia drugs for filariasis

[3] Marc P Hbner, et al. PLoS Negl Trop Dis. In vivo kinetics of Wolbachia depletion by ABBV-4083 in L. sigmodontis adult worms and microfilariae

[4] Mark J Taylor, et al. Sci Transl Med. Preclinical development of an oral anti- Wolbachia macrolide drug for the treatment of lymphatic filariasis and onchocerciasis

[5] Thomas W von Geldern, et al. PLoS Negl Trop Dis. Discovery of ABBV-4083, a novel analog of Tylosin A that has potent anti-Wolbachia and anti-filarial activity

[6] Thomas W von Geldern, et al. PLoS Negl Trop Dis. Discovery of ABBV-4083, a novel analog of Tylosin A that has potent anti-Wolbachia and anti-filarial activity

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