CGP 42112
(Synonyms: CGP42112A) 目录号 : GC15406
CGP 42112是一种有效的血管紧张素II亚型2受体(AT2R)激动剂。
Cas No.:127060-75-7
Sample solution is provided at 25 µL, 10mM.
CGP 42112 is an effective angiotensin II subtype 2 receptor (AT2R) agonist [1]. AT2R plays a crucial role in the development of the kidney and exerts anti-proliferative, anti-fibrotic and pro-apoptotic effects in vivo [2]. CGP 42112 can be used for studies on isolated rat hearts and vascular endothelial function [3].
In vitro, treatment of NR8383 cells with CGP 42112 (2nM) for 6-24 hours can weaken the effect of lipopolysaccharide (LPS) on the cells, significantly reduce the expression of M1 polarization markers (including iNOS and TNF-α), and inhibit the expression of p-p65, p50, p-ERK1/2 and p-IκBα [4]. CGP 42112 (0.1-100μM) treated the renal proximal tubule suspension (1mg/ml) at 37°C for 30 minutes can inhibit NKA activity in a dose-dependent manner and increase the accumulation of cGMP in the proximal tubules [5].
In vivo, CGP 42112 (5, 10 and 20μg/kg, once every 3 days, total three times) administered by intra-articular injection to rats can significantly reduce the arthritis index of a single left hind paw. CGP 42112 can improve the histological signs of arthritis rats [6]. CGP 42112 (1mg/kg; once; i.p.) administered to ATla-deficient mice has no effect on the plasma aldosterone and corticosterone levels of the mice [7].
References:
[1] Takekoshi K, Ishii K, Isobe K, et al. Angiotensin-II subtype 2 receptor agonist (CGP-42112) inhibits catecholamine biosynthesis in cultured porcine adrenal medullary chromaffin cells[J]. Biochemical and Biophysical Research Communications, 2000, 272(2): 544-550.
[2] Elbaz N, Bedecs K, Masson M, et al. Functional trans-inactivation of insulin receptor kinase by growth-inhibitory angiotensin II AT2 receptor[J]. Molecular Endocrinology, 2000, 14(6): 795-804.
[3] Raffai G, Durand M J, Lombard J H. Acute and chronic angiotensin-(1–7) restores vasodilation and reduces oxidative stress in mesenteric arteries of salt-fed rats[J]. American Journal of Physiology-Heart and Circulatory Physiology, 2011, 301(4): H1341-H1352.
[4] Zheng X, Xu Z, Xu L, et al. Angiotensin II Type 2 receptor inhibits M1 polarization and apoptosis of alveolar macrophage and protects against mechanical ventilation-induced lung injury[J]. Inflammation, 2025, 48(1): 165-180.
[5] Hakam A C, Hussain T. Angiotensin II AT2 receptors inhibit proximal tubular Na+-K+-ATPase activity via a NO/cGMP-dependent pathway[J]. American Journal of Physiology-Renal Physiology, 2006, 290(6): F1430-F1436.
[6] Wang D, Hu S, Zhu J, et al. Angiotensin II type 2 receptor correlates with therapeutic effects of losartan in rats with adjuvant‐induced arthritis[J]. Journal of cellular and molecular medicine, 2013, 17(12): 1577-1587.
[7] Naruse M, Tanabe A, Sugaya T, et al. Deferential roles of angiotensin receptor subtypes in adrenocortical function in mice[J]. Life sciences, 1998, 63(18): 1593-1598.
CGP 42112是一种有效的血管紧张素II亚型2受体(AT2R)激动剂 [1]。AT2R在肾脏的发育过程中起着关键作用,并在体内发挥着抗增殖、抗纤维化和促凋亡的作用 [2]。CGP 42112可用于对大鼠离体心脏以及血管内皮功能的研究 [3]。
在体外,CGP 42112(2nM)处理NR8383细胞6-24h,能够减弱脂多糖(LPS )对细胞的作用,显著降低了M1极化标志物(包括iNOS和TNF-α)的表达,同时抑制p-p65、p50、p-ERK1/2和p-IκBα的表达 [4]。CGP 42112(0.1-100M)在37℃下处理肾近端小管悬液(1mg/ml)30min,能够以剂量依赖性方式抑制NKA活性,增加近端小管中cGMP的蓄积[5]。
在体内, CGP 42112(5, 10和20μg/kg,每三天一次,总共三次)通过关节内注射治疗大鼠,能够显著降低单个左后爪的关节炎指数。CGP 42112可改善关节炎大鼠的组织学体征[6]。CGP 42112(1mg/kg; once; i.p.)注射ATla缺陷型小鼠后,对小鼠的血浆醛固酮和皮质酮水平没有影响[7]。
Cell experiment [1]: | |
Cell lines | NR8383 cells |
Preparation Method | Rat alveolar macrophages (NR8383) were cultured in F12K medium supplemented with 10% fetal bovine serum (FBS) and 1% penicillin/streptomycin. Cells were seeded on 6-well plates at a density of 4 × 106 cells/ml for Western blot, PCR and flow cytometry experiments. After 24h incubation, the cells were stimulated with DMSO medium, LPS (100ng/mL) 、AT2R activator CGP 42112 (2nM) 、AT2R inhibitor PD123319 (70nM) and AT1R inhibitor valsartan (100μM, CGP 48933) for 6h or 24h. In addition, the cells were mounted onto slides for fluorescent immunohistochemistry. |
Reaction Conditions | 2nM; 6h, 24h |
Applications | The AT2R agonist CGP 42112 can weaken the effect of LPS, significantly reducing the expression of M1 polarization markers (including iNOS and TNF-α), and simultaneously inhibiting the expressions of p-p65, p50, p-ERK1/2 and p-IκBα. |
Animal experiment [2]: | |
Animal models | Sprague-Dawley rats |
Preparation Method | Adjuvant-induced arthritis (AIA) rats were randomly assigned to the following treatments: losartan (5, 10 and 15mg/kg/day, orally, once daily), MTX (0.5mg/kg, intraperitoneally, per 3 days), and vehicle (NS). Sham-operated rats received the vehicle (NS). The treatment started on day 14 after immunization and continued until day 28. After 15 days of treatment, on day 28, all rats were anesthetized with the chloral hydrate and killed (n = 6 per group). The serum, paw and spleen were collected for further study. To study the effects of AT2R agonist on rats with AIA, CGP 42112 (5, 10 and 20μg/kg, once every 3 days, total three times) and triamcinolone acetonide (1mg/kg, once every 3 days, total three times) were administered by intra-articular injection into the left hind (non-injected) paws following the onset of the secondary arthritis (n = 7 per group). Normal and model rats received NS instead. |
Dosage form | 5, 10 and 20μg/kg, once every 3 days, total three times; intra-articular injection |
Applications | Intra-articular injection of AIA rats with CGP 42112 (10 and 20μg/kg) significantly decreased the arthritis index of single left hind (non-injected) paw on days 22 and 26. |
References: |
Cas No. | 127060-75-7 | SDF | |
别名 | CGP42112A | ||
分子式 | C52H69N13O11 | 分子量 | 1052.2 |
溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,PBS (pH 7.2): 10 mg/ml | 储存条件 | Desiccate at -20°C |
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1 mg | 5 mg | 10 mg |
1 mM | 0.9504 mL | 4.7519 mL | 9.5039 mL |
5 mM | 0.1901 mL | 0.9504 mL | 1.9008 mL |
10 mM | 0.095 mL | 0.4752 mL | 0.9504 mL |
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2.
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