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.
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Source | Br J Pharmacol (2013). Figure 2. YS-49 |
| Method | cell culture | |
| Cell Lines | RAW 264.7 cells | |
| Concentrations | - | |
| 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. |
| Molecular Weight | 386.28 |
| Formula | C20H20BrNO2 |
| CAS Number | 132836-42-1 |
| Solubility (25°C) | DMSO 80 mg/mL Water 10 mg/mL (ultrasonic and warming) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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