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PD-156707

Cat. No. M8058
PD-156707 Structure
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Biological Activity

PD-156707 is a selective endothelin receptor (ETA) antagonist.

Chemical Information
Molecular Weight 528.48
Formula C28H25O9·Na
CAS Number 162412-70-6
Solubility (25°C) DMSO: ≥20 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] Carsten Hltke, et al. Synthesis, in vitro pharmacology and biodistribution studies of new PD 156707-derived ET(A) receptor radioligands

[2] Yashu Coe, et al. The endothelin A receptor antagonists PD 156707 (CI-1020) and PD 180988 (CI-1034) reverse the hypoxic pulmonary vasoconstriction in the perinatal lamb

[3] A M Doherty, et al. Discovery and development of an endothelin A receptor-selective antagonist PD 156707

[4] D P Ignasiak, et al. Effects of endothelin ETA receptor antagonism with PD 156707 on hemodynamics and renal vascular resistance in rabbits

[5] E E Reynolds, et al. Pharmacological characterization of PD 156707, an orally active ETA receptor antagonist

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