GSK 2833503A is a potent and selective TRPC6 and TRPC3 antagonist (IC50 = 3-16 nM and 21-100 nM, respectively). GSK 2833503A exhibits >63-fold selectivity over other ion channels, including other TRP channels, CaV1.2, hERG and NaV1.5. GSK 2833503A suppresses angiotensin II or endothelin-1-induced cardiachypertrophy signaling in HEK293 cellsin vitroand in cardiomyocytes.
MDL-100240 is a dual inhibitor of angiotensin-converting enzyme (ACE) and neprilysin with a balanced activity. MDL 100240 shows an impressive effectiveness both in preventing and in regressing hypertension-induced vascular remodeling and cardiac hypertrop
AAA is an antagonist of G protein-coupled receptor 75 (GPR75).1It increases basal GPR75 protein levels and inhibits 20-HETE-induced reductions in GPR75 protein levels in PC3 cells. AAA (5 and 10 μM) also reduces 20-HETE-induced phosphorylation of EGFR, NF-κB, and Akt in, and cell migration of, PC3 cells.In vivo, AAA (10 mg/kg per day) reduces systolic blood pressure, albuminuria, renal angiotensin II levels, and cardiachypertrophy in a Cyp1a1-Ren-2 transgenic rat model of malignant hypertension when administered prior to induction or after establishment of hypertension.2 1.Cárdenas, S., Colombero, C., Panelo, L., et al.GPR75 receptor mediates 20-HETE-signaling and metastatic features of androgen-insensitive prostate cancer cellsBiochim. Biophys. Acta Mol. Cell Biol. Lipids1865(2)158573(2020) 2.Sedláková, L., Kikerlová, S., Husková, Z., et al.20-Hydroxyeicosatetraenoic acid antagonist attenuates the development of malignant hypertension and reverses it once established: a study in Cyp1a1-Ren-2 transgenic ratsBiosci. Rep.38(5)BSR20171496(2018)
Chlorthalidone impurity G is a potential impurity found in commercial preparations of chlorthalidone that has moderate antihypertensive effects. Chlorthalidone is a thiazide-like diuretic that inhibits the Na+/Cl- cotransporter in the distal convoluted tubule of the kidney, which prevents reabsorption of sodium and chloride leading to a reduction in plasma volume and cardiac output. It also inhibits carbonic anhydrase (CA), including the isoforms CAVB, VII, IX, XII, and XIII (Kis = 2.8-23 nM) and, to a lesser extent, CAI, CAII, IV, VA, and VI (Kis = 138-1,347 nM), which may mediate its sustained vasodilatory activity. Dietary administration of chlorthalidone (8 mg per animal per day) reduces arterial hypertension and prevents or reduces ventricular hypertrophy induced by deoxycorticosterone acetate (DOCA) in salt-hypertensive rats. Formulations containing chlorthalidone have been used alone or in combination with other antihypertensive agents to lower arterial blood pressure and as adjuvants to address edema caused by cardiac or renal disorders.
Angiotensin II 是一种主要的生物活性血管收缩肽,通过与AT1R和AT2R受体结合,调节血压,刺激交感神经,促进醛固酮合成和肾脏功能。它还能诱导血管平滑肌细胞增生、胶原合成增加,导致血管和心肌增厚及纤维化,同时促进细胞凋亡和内皮细胞毛细血管形成。Angiotensin II常用于诱导高血压和心脏肥大动物模型。
VCP-746 is a potent adenosine A2B receptor agonist that stimulates anti-fibrotic signalling. VCP746 reduces hypertrophy in a rat neonatal cardiac myocyte model. VCP746 is a hybrid molecule consisting of an adenosine moiety linked to an adenosine A1 receptor (A1AR) allosteric modulator moiety. At the A1AR, VCP746 mediated cardioprotection in the absence of haemodynamic side effects such as bradycardia.
Angiotensin II human TFA 是肾素-血管紧张素系统中的强效血管收缩剂,通过与 AT1R 和 AT2R 受体作用调节血压,可激活交感神经、促进醛固酮合成和肾功能,诱导血管平滑肌细胞增殖及成纤维细胞中 I 型和 III 型胶原合成,导致血管和心肌增厚、纤维化,并诱导凋亡及促进毛细血管生成,可用于构建心脏肥大、高血压和腹主动脉瘤模型。
Angiotensin II human acetate 是肾素-血管紧张素系统中的主要血管收缩肽,通过与AT1R和AT2R受体结合调节血压,刺激交感神经,促进醛固酮合成和肾脏功能,诱导血管平滑肌细胞增生和胶原合成,导致血管及心肌增厚和纤维化,同时促进细胞凋亡和内皮毛细血管形成。常用于诱导高血压和心脏肥大模型。