CGP-42112

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Chemical Structure| 127060-75-7 同义名 : CGP42112A
CAS号 : 127060-75-7
货号 : A635664
分子式 : C52H69N13O11
纯度 : 98%
分子量 : 1052.185
MDL号 : MFCD00133611
存储条件：

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(99.79 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Angiotensin II subtype 2 receptor (AT2R) is abundantly expressed in adrenal medullary chromaffin cells[2]. Recent data suggest that AT2R may modulate key processes linked to atherosclerosis[3]. CGP-42112 is a potent AT2R agonist. CGP-42112 (≥ 1 nM) significantly inhibited cGMP production, TH-mRNA, TH-protein and TH-enzyme activity from the basal value, and these inhibitory effects were abolished by PD123319 (AT2R antagonist). The [125I] CGP-42112 binding was of high affinity, saturable and specific in the rat brain (combined olfactory bulb, septum, thalamus and midbrain) and whole adrenal[4]. Intravenous infusions of CGP-42112 (0.1 and 1 mg/kg/min) shifted the upper limit of CBF (cerebral blood flow) autoregulation toward higher blood pressures without affecting baseline CBF[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

0.95mL

0.19mL

0.10mL

4.75mL

0.95mL

0.48mL

9.50mL

1.90mL

0.95mL
参考文献

[1]Takekoshi K, et al. Angiotensin-II subtype 2 receptor agonist (CGP-42112) inhibits catecholamine biosynthesis in cultured porcine adrenal medullary chromaffin cells. Biochem Biophys Res Commun. 2000 Jun 7;272(2):544-50.

[2]Takekoshi K, Ishii K, Isobe K, Nanmoku T, Kawakami Y, Nakai T. Angiotensin-II subtype 2 receptor agonist (CGP-42112) inhibits catecholamine biosynthesis in cultured porcine adrenal medullary chromaffin cells. Biochem Biophys Res Commun. 2000;272(2):544-550.

[3]Koïtka A, Cao Z, Koh P, et al. Angiotensin II subtype 2 receptor blockade and deficiency attenuate the development of atherosclerosis in an apolipoprotein E-deficient mouse model of diabetes. Diabetologia. 2010;53(3):584-592.

[4]Speth RC. [125I]CGP 42112 binding reveals differences between rat brain and adrenal AT2 receptor binding sites. Regul Pept. 1993;44(2):189-197. doi:10.1016/0167-0115(93)90242-z

[5]Näveri L, Strömberg C, Saavedra JM. Angiotensin II AT2 receptor stimulation extends the upper limit of cerebral blood flow autoregulation: agonist effects of CGP 42112 and PD 123319. J Cereb Blood Flow Metab. 1994;14(1):38-44.