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PD 123319

Cat. No. M3917

PD 123319 Structure
Size Price Availability Quantity
5mg USD 100 In stock
10mg USD 130 In stock
50mg USD 450 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

PD123319 shows inhibition potency in both rat adrenal and brain binding assay with IC50 values of 34nM and 210nM. At high concentrations PD123319 blocks the beneficial effects of the AT2-agonist LP2-3 on RVH. At low concentrations PD123319 attenuates cardiopulmonary injury by reducing pulmonary inflammation and fibrosis and preventing PAH-induced RVH but does not affect alveolar and vascular development in newborn rats with experimental BPD. Administration of PD123319 can suppress the generation of cyclic guanosine monophosphate and increase the production of prostaglandin E2. Besides that, administration of PD-123319 does not influence the effect of Ang II on protein tyrosine phosphorylation or thymidine incorporation.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models spontaneously hypertensive rats
Formulation saline
Dosages 0.36 and 1 mg/kg/min
Administration intravenous
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 508.61
Formula C31H32N4O3
CAS Number 130663-39-7
Purity >99%
Solubility DMSO 100 mg/mL
Water 100 mg/mL
Storage at -20°C
References

Angiotensin II type 2 receptor ligand PD123319 attenuates hyperoxia-induced lung and heart injury at a low dose in newborn rats.
Wagenaar GT, et al. Am J Physiol Lung Cell Mol Physiol. 2014 Aug 1;307(3):L261-72. PMID: 24951776.

Effects of acid challenges on type 2 angiotensin II receptor-sensitive ammonia production by the proximal tubule.
Nagami GT, et al. Am J Physiol Renal Physiol. 2014 Jul 1;307(1):F53-7. PMID: 24829505.

Angiotensin II receptor blockers: review of the binding characteristics.
Siragy H. Am J Cardiol. 1999 Nov 18;84(10A):3S-8S. PMID: 10588088.

Synthesis and structure-activity relationships of a novel series of non-peptide angiotensin II receptor binding inhibitors specific for the AT2 subtype.
Blankley CJ, et al. J Med Chem. 1991 Nov;34(11):3248-60. PMID: 1956044.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PD 123319 supplier, Angiotensin Receptor, inhibitors

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