YS-49 protects cells from oxidant injury.YS-49 is an anti-inflammatory agent. YS-49 is a activator of PI3K/Akt signaling. YS-49, an analog of higenamine, induces heme oxygenase (HO-1) in endothelial cells and protects cells from oxidant injury. The compound was reported to inhibit Ang II-stimulated VSMC proliferation through HO-1 production, which inhibits both the JNK pathway and ROS production. A study (JPET) reported that CKD712 (S-YS-49) confer cardiac protection and anti-inflammatory via activation of the PI3K signal pathway. YS-49 and YS-51 showed inhibitory activities to both human and rat platelet aggregation induced by ADP, collagen and epinephrine. YS-49 and YS-51 have therapeutic potential for DIC and/or accompanying multiple organ failure.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||Water >10 mg/mL|
|Source||Br J Pharmacol (2013). Figure 2. YS-49|
|Cell Lines||RAW 264.7 cells|
|Incubation Time||1 h|
|Results||As shown in Fig. 2, 1 μg/ml LPS significantly induced the morphological change at 2 h, which was subsequently inhibited by CKD712 in a concentration-dependent manner.|
YS 49, 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.
Sun JJ, et al. Life Sci. 2008 Mar 12;82(11-12):600-7. PMID: 18262205.
Effects of two tetrahydroisoquinolines (YS-49 and YS-51) on experimental disseminated intravascular coagulation induced by lipopolysaccharide in rats.
Pyo MK, et al. Arzneimittelforschung. 2004;54(11):705-10. PMID: 15612611.
Antithrombotic effects of YS-49 and YS-51--1-naphthylmethyl analogs of higenamine.
Yun-Choi HS, et al. Thromb Res. 2001 Nov 15;104(4):249-55. PMID: 11728526.
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