Angiotensin Receptor Antagonists

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SML0245 Candesartan cilexetil ≥98% (HPLC) Candesartan cilexetil is the prodrug form of the potent angiotensin II receptor antagonist, candesartan. The prodrug is cleaved by esterases within the intestine to liberate the active molecule.
 
E2535 Eprosartan mesylate ≥98% (HPLC) Angiotensin II type 1 (AT1) receptor antagonist; anti-hypertensive.
 
I2286 Irbesartan ≥98% (HPLC), powder Irbesartan is an angiotensin II type 1 (AT1) receptor antagonist with anti-hypertensive activity.
 
M0821 Moexipril hydrochloride powder, ≥98% (HPLC) Moexipril is an ACE-Inhibitor; Antihypertensive; Unlike other ACE inhibitors, prolongs QT interval leading to torsades de pointes and cardiad arrhythmia;
 
N0415 Novokinin trifluoroacetate salt ≥95% (HPLC) Novokinin trifluoroacetate is a angiotensin II receptor 2 (AT2) agonist.
 
P5749 S-(+)-PD 123177 trifluoroacetate salt hydrate ≥98% (HPLC), solid S-(+)-PD 123177 is selective AT2 angiotensin receptor antagonist. The angiotensin AT2 receptor is an atypical seven transmembrane domain receptor that is coupled to activation of tyrosine phosphatase and inhibition of MAP kinase, and does not undergo agonist-induced internalization. An investigation of the occurrence and nature of AT2 receptor phosphorylation revealed that phorbol ester-induced activation of protein kinase C (PKC) in HA-AT2 receptor-expressing COS-7 cells caused rapid and specific phosphorylation of a single residue (Ser354) located in the cytoplasmic tail of the receptor. Agonist activation of AT2 receptors by angiotensin II (Ang II) also caused rapid PKC-dependent phosphorylation of Ser354 that was prevented by the AT2 antagonist, S-(+)-PD 123177, and by inhibitors of PKC. In cells coexpressing AT1 and AT2 receptors, Ang II-induced phosphorylation of the AT2 receptor was reduced by S-(+)-PD 123177 and abolished by treatment with both antagonists or with PKC inhibitors. These findings indicate that the AT2 receptor is rapidly phosphorylated via PKC during homologous activation by Ang II, and also undergoes heterologous PKC-dependent phosphorylation during activation of the AT1 receptor.
 
P186 PD 123,319 di(trifluoroacetate) salt hydrate powder, ≥98% (HPLC) PD123,319 di (trifluoroacetate) salt hydrate is a widely used angiotensin II subtype-2 receptor (AT2R) antagonist to study the role of AT2 receptor in vitro and in vivo. It increases the AngII-induced abdominal aortic aneurysms (AAAs) without interacting with AT2 receptor.
 
P0094 Perindopril erbumine Perindopril erbumine is an angiotensin converting enzyme (ACE) inhibitor; antihypertensive; becomes hydrolyzed in vivo to the active diacid metabolite; unlike the other ACE inhibitors, inhibits tumor growth in hepatocellular carcinoma cells due to suppression of VEGF levels; also suppresses angiotensin II production in vitro. Long-term therapy with this agent has a beneficial effect on the cerebral circulation by improving cerebral perfusion reserve in patients with previous minor stroke.
 
T8949 Telmisartan ≥98% (HPLC), solid Telmisartan is a non-peptide AT1 angiotensin receptor antagonist.
 
SML0142 Valsartan ≥98% (HPLC) Valsartan is an Angiotensin II type 1 (AT1) receptor antagonist and anti-hypertensive. Valsartan renders protection against heart attack and stroke resulting from abrupt increase in blood pressure. Valsartan reduces myocardial-infarction-related complications in heart attack survivors.