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PD 123319 ditrifluoroacetate

Cat. No. M2164
PD 123319 ditrifluoroacetate Structure
Size Price Availability Quantity
5mg USD 120  USD120 In stock
10mg USD 150  USD150 In stock
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Biological Activity

PD 123319 ditrifluoroacetate is a potent, selective, non-peptide angiotensin AT2 receptor antagonist with IC50 values of 34 and 210 nM in rat adrenal tissue and brain respectively. PD 123319 ditrifluoroacetate prevents the binding of angiotensin II to the receptor, which blocks signal transduction and causes vasodilation. Intravenous administration of PD 123319 to conscious hypertensive rats elicited an immediate dose-dependent increase in MAP that was sustained for approximately 7.4 min with 3 mg/kg PD123319.

Chemical Information
Molecular Weight 736.67
Formula C31H32N4O3.2CF3CO2H
CAS Number 136676-91-0
Solubility (25°C) Water
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] Tamura M, et al. J Hypertens. Induction of angiotensin II subtype 2 receptor-mediated blood pressure regulation in synthetic diet-fed rats.

[2] Park PD, et al. Eur J Pharmacol. Receptor subtypes mediating spinal cardiovascular effects of angiotensin II in rat using losartan and PD 123319.

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