CAS NO: | 132836-42-1 |
包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
10mg | 电议 |
50mg | 电议 |
YS-49 是一种具有正性肌力作用的异喹啉化合物生物碱,能通过诱导 HO-1,抑制血管紧张素II刺激的血管平滑肌细胞 (VSMC) 增殖。
Cas No. | 132836-42-1 |
别名 | 1,2,3,4-四氢-1-(1-萘基甲基)-6,7-异喹啉二醇氢溴酸盐 |
Canonical SMILES | OC1=CC2=C(C(CC3=C4C=CC=CC4=CC=C3)NCC2)C=C1O.[H]Br |
分子式 | C20H20BrNO2 |
分子量 | 386.28 |
溶解度 | DMSO : ≥ 100 mg/mL (258.88 mM) |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | YS-49 inhibits Ang II-stimulated proliferation of VSMCs via induction of HO-1.IC50 value:Target: HO-1YS-49 is a novel positive inotropic isoquinoline compound. YS-49 has potential as a therapeutic strategy for the pathogenesis of Ang II-related vascular diseases such as hypertension and atherosclerosis, via the induction of HO-1 gene activity. YS-49 induced HO-1 protein production in a dose-and time-dependent manner in VSMCs. Treatment with YS-49 significantly and dose-dependently inhibited Ang II-induced VSMC proliferation, ROS production, and phosphorylation of JNK, but not P38 MAP kinase or ERK1/2.YS-49(32.8 microM) exhibited much stronger inhibitory effects on TXA(2) formation. The higher inhibitory potencies of YS-49 (IC(50): 3.3microM) than higenamine (IC(50): 140 microM) on AA induced rat platelet aggregation was presumed to be the result of low inhibitory effect of higenamine than YS-49 on TXA(2) production from AA. The oral administration of YS-49 (50 mg/kg) increased the recovery rates from the acute thrombotic challenge in mice and lowered the weight of thrombus formed inside the AV shunt tube in rats. [1]. Lee YS, Kim CH, Yun-Choi HS,et al. Cardiovascular effect of a naphthylmethyl substituted tetrahydroisoquinoline, YS 49, in rat and rabbit. Life Sci. 1994;55(21):PL415-20. [2]. Kang YJ, Koo EB, Lee YS,et al. Prevention of the expression of inducible nitric oxide synthase by a novel positive inotropic agent, YS 49, in rat vascular smooth muscle and RAW 264.7 macrophages. Br J Pharmacol. 1999;128(2):357-64. [3]. Yun-Choi HS, Pyo MK, Park KM, et al. Antithrombotic effects of YS-49 and YS-51--1-naphthylmethyl analogs of higenamine . Thromb Res. 2001;104(4):249-55. [4]. Pyo MK, Yun-Choi HS, Chang KC, et al. Effects of two tetrahydroisoquinolines (YS-49 and YS-51) on experimental disseminated intravascular coagulation induced by lipopolysaccharide in rats. Arzneimittelforschung. 2004;54(11):705-10. [5]. Pyo MK, Kim JM, Jin JL,et al. Effects of higenamine and its 1-naphthyl analogs, YS-49 and YS-51, on platelet TXA2 synthesis and aggregation. Thromb Res. 2007;120(1):81-6. [6]. Sun JJ, Kim HJ, Seo HG, et al. YS49,1-(alpha-naphtylmethyl)-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline,regulates angiotensin II-stimulated ROS production, JNK phosphorylation and vascular smooth muscle cell proliferation via the induction of heme oxygenase-1. Life Sci. 2008;82(11-12):600-7. |