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Abarelix Acetate

Cat. No. M13983
Abarelix Acetate Structure
Synonym:

PPI 149 Acetate; R 3827 Acetate

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Biological Activity

Abarelix Acetate (PPI 149 Acetate; R 3827 Acetate) is a potent gonadotrophin-releasing hormone (GnRH) antagonist, used for prostate cancer research.

Chemical Information
Molecular Weight 1476.12
Formula C74H99ClN14O16
CAS Number 547741-72-0
Form Solid
Solubility (25°C) DMSO ≥ 90 mg/mL
Storage -20°C, dry, sealed
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] Judd W Moul. Utility of LHRH antagonists for advanced prostate cancer

[2] Jennifer Yannucci, et al. The effect of androgen deprivation therapy on fasting serum lipid and glucose parameters

[3] M Bayes, et al. Gateways to clinical trials

[4] John Trachtenberg, et al. A phase 3, multicenter, open label, randomized study of abarelix versus leuprolide plus daily antiandrogen in men with prostate cancer

[5] D McLeod, et al. A phase 3, multicenter, open-label, randomized study of abarelix versus leuprolide acetate in men with prostate cancer

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Keywords: Abarelix Acetate, PPI 149 Acetate; R 3827 Acetate supplier, LHRH/GnRH, inhibitors, activators


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