RAAS
Renin-angiotensin-aldosterone axis, or renin-angiotensin aldosterone system (RAAS) is a vital one, for survival. This system maintains vascular tonicity by regulating extracellular fluid volume and arterial pressure. By this system, water, blood, plasma, lymph and interstitial fluid are controlled tightly for functioning of the pulsating organ heart and filtration organ kidney, without the onslaught of either extremes. Perturbation of this system can disturb blood pressure, leading to chronic or acute diseases, or even sudden death. Renin and angiotensin are two critical components forming the system. Renin (or angiotensinogenase), is secreted by the kidney granular cells.
Angiotensinogen is a member of the serpin family (SERPINA8), so a potential enzyme inhibitor. The decapeptide angiotensin I further undergoes cleavage in the lungs capillaries, endothelial cells, and kidney epithelial cells by the endothelial-bound angiotensin-converting enzyme (ACE). This enzyme, a carboxypeptidase, also known as kininase II, peptidyl-dipeptidase A, or CD143, converts angiotensin I into the peptide angiotensin II. ACE is a common component of the RAAS, as well as kinin- kallikrein system (KKS). ACE interacts with Gprotein-coupled receptor (GPCR) AT1 by stimulating the Gq protein in vascular smooth muscle cells to activate phospholipase C, for increasing intracellular calcium. So, angiotensin II is a critical regulator of blood volume, pressure, and pH. Renin induced increment in TGF-b1 (transforming Growth Factor-b1) stimulates increment in PAI-1, fibronectin (FN) and collagen I, which indicates that renin plays part in renal fibrotic disease. A large number of factors can influence RAAS, some prominent of which include birth control pills, pregnancy, other hormones (estrogen, testosterone, thyroid, cortisol), diuretics, vasodilators, blood pressure drugs, also other medications.
References
1.Patel S, et al. Biomed Pharmacother. 2017;94:317–325.
Angiotensinogen is a member of the serpin family (SERPINA8), so a potential enzyme inhibitor. The decapeptide angiotensin I further undergoes cleavage in the lungs capillaries, endothelial cells, and kidney epithelial cells by the endothelial-bound angiotensin-converting enzyme (ACE). This enzyme, a carboxypeptidase, also known as kininase II, peptidyl-dipeptidase A, or CD143, converts angiotensin I into the peptide angiotensin II. ACE is a common component of the RAAS, as well as kinin- kallikrein system (KKS). ACE interacts with Gprotein-coupled receptor (GPCR) AT1 by stimulating the Gq protein in vascular smooth muscle cells to activate phospholipase C, for increasing intracellular calcium. So, angiotensin II is a critical regulator of blood volume, pressure, and pH. Renin induced increment in TGF-b1 (transforming Growth Factor-b1) stimulates increment in PAI-1, fibronectin (FN) and collagen I, which indicates that renin plays part in renal fibrotic disease. A large number of factors can influence RAAS, some prominent of which include birth control pills, pregnancy, other hormones (estrogen, testosterone, thyroid, cortisol), diuretics, vasodilators, blood pressure drugs, also other medications.
References
1.Patel S, et al. Biomed Pharmacother. 2017;94:317–325.
Endocrinology/Hormones
RAAS
-
Theasinensin C
产品货号 : M37863
cas no: 89013-69-4
Theasinensin C is a compound extracted from black tea water with an IC50 value of 40.21 μM for renin activity. -
Alunacedase alfa
产品货号 : M37266
cas no: 2416824-55-8
Alunacedase alfa (APN-01) is a soluble angiotensin-converting enzyme 2 (hrsACE2) with antiviral activity that reduces the competitive entry of SARS-CoV-2 into cell membranes bound to ACE2. alunacedase alfa mimics ACE2 in vivo and can be used to study novel coronavirus infections, pulmonary hypertension and acute lung injury. Alunacedase alfa mimics ACE2 in vivo and can be used to study novel coronavirus infections, pulmonary hypertension and acute lung injury. -
Zabicipril
产品货号 : M36247
cas no: 83059-56-7
Zabicipril is a novel orally available angiotensin-converting enzyme inhibitor, a prodrug with antihypertensive activity following in vivo de-esterification. -
Valsartan Methyl Ester
产品货号 : M36024
cas no: 137863-17-3
Valsartan Methyl Ester is a potent angiotensin II receptor antagonist, IC50= 0.06uM. -
Azilsartan Methyl Ester
产品货号 : M35894
cas no: 147403-52-9
Azilsartanmethylester 是 Azilsartan (HY-14914) 的衍生物,是一种血管紧张素 II 受体拮抗剂,在高血压中发挥重要作用。