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AC 265347

Cat. No. M6392
AC 265347 Structure
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Biological Activity

AC 265347 is a caSR biased allosteric modulator (pEC50 = 7.8-8.1). Calcimimetic. Displays ability to bias signalling towards the accumulation of PERK1/2 and IP1. Reduces parathyroid hormone (PTH) levels in rat serum without inducing the release of calcitonin. Exhibits no significant activation of human GABAB or type I PTH receptors. Orally active.

Chemical Information
Molecular Weight 283.39
Formula C17H17NOS
CAS Number 1253901-26-6
Solubility (25°C) DMSO 28.34 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] Patel, et al. J Biol Chem. Calcium/calmodulin-dependent phosphorylation and activation of human Cdc25-C at the G2/M phase transition in HeLa cells.

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