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.
|Source||Br J Pharmacol (2015). Figure 3. PD 123319|
|Cell Lines||male Sprague Dawley rats|
|Incubation Time||2 weeks|
|Results||Remarkably, C21 treatment of MCT rats reversed both interstitial and perivascular fibrosis, an effect that was blocked by PD-123319|
|Animal models||spontaneously hypertensive rats|
|Dosages||0.36 and 1 mg/kg/min|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO 90 mg/mL
Water 90 mg/mL
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.
|Related Angiotensin Receptor Products|
A-779 is a specific antagonist of G-protein coupled receptor (Mas receptor).
Angiotensin (1-7) is a synthetic heptapeptide identical to endogenous angiotensin-(1-7), inhibits purified canine angiotensin converting enzyme (ACE) activity with an IC50 of 0.65 μM.
Losartan is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.
EMA401 (also known as Olodanrigan and PD-126055) is a highly selective angiotensin AT2 antagonist.
|Angiotensin II human
Angiotensin II human is converted by Angiotensin I through removal of two C-terminal residues by the enzyme angiotensin-converting enzyme (ACE). Angiotensin II is mediated by AT1 and AT2 receptors, which are seven transmembrane glycoproteins with 30% sequence similarity.
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