Resorcinolnaphthalein
(Synonyms: NSC 354317) 目录号 : GC11560Activator of ACE2
Cas No.:41307-63-5
Sample solution is provided at 25 µL, 10mM.
Resorcinolnaphthalein is an Angiotensin-converting enzyme 2 (ACE2) activator [1].
Angiotensin-converting enzyme 2 (ACE2) has been involved in hydrolyzing angiotensin II and opposing its actions, and plays a protective role in the pathogenesis of pulmonary arterial hypertension (PAH) [2]. Targeted disruption of ACE2 in mice results in a severe cardiac contractility defect, increased angiotensin II levels, and upregulation of hypoxia-induced genes in the heart [2].
In vitro: Resorcinolnaphthalein enhanced ACE2 activity in a dose-dependent manner [1].
In vivo: Resorcinolnaphthalein caused significant activation of ACE2 in both normal and diseased rats in 7 days after treatment. Treatment with resorcinolnaphthalein prevented high PAP, right ventricular hypertrophy and neointimal formation. Resorcinolnaphthalein caused an improved endothelia-dependent vasorelaxation and decreased in proinflammatory cytokines, such as TNF-α, MCp-1, IL-6, and increased in anti-inflammatory cytokine IL-10 in the early stage of the pathogenesis [3]. Resorcinolnaphthalein can specifically and effectively enhanced ACE2 activity in rats [4]. ACE2 activation by resorcinolnaphthalein showed effects on pulmonary endothelial dysfunction and neointimal formation during the development of severe PAH in rats [4].
References:
[1] Prada J A H, Ferreira A J, Katovich M J, et al. Structure-based identification of small-molecule angiotensin-converting enzyme 2 activators as novel antihypertensive agents[J]. Hypertension, 2008, 51(5): 1312-1317.
[2] Crackower M A, Sarao R, Oudit G Y, et al. Angiotensin-converting enzyme 2 is an essential regulator of heart function[J]. Nature, 2002, 417(6891): 822-828.
[3] Haber P K, Ye M, Wysocki J, et al. Angiotensin-converting enzyme 2–independent action of presumed angiotensin-converting enzyme 2 activatorsNovelty and significance[J]. Hypertension, 2014, 63(4): 774-782.
[4] Li G, Liu Y, Zhu Y, et al. ACE2 activation confers endothelial protection and attenuates neointimal lesions in prevention of severe pulmonary arterial hypertension in rats[J]. Lung, 2013, 191(4): 327-336.
Cas No. | 41307-63-5 | SDF | |
别名 | NSC 354317 | ||
化学名 | 3',6'-dihydroxy-spiro[1H,3H-naphtho[1,8-cd]pyran-1,9'-[9H]xanthen-3-one | ||
Canonical SMILES | Oc1ccc2c(c1)Oc1cc(O)ccc1C12OC(=O)c2cccc3cccc1c23 | ||
分子式 | C24H14O5 | 分子量 | 382.4 |
溶解度 | ≤20mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 2.6151 mL | 13.0753 mL | 26.1506 mL |
5 mM | 0.523 mL | 2.6151 mL | 5.2301 mL |
10 mM | 0.2615 mL | 1.3075 mL | 2.6151 mL |
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2.
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