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K134

产品编号 T15640 CAS 189362-06-9

别名: OPC33509

K134 is an inhibitor of phosphodiesterase 3. The IC50s of K134 for PDE3A, PDE3B, PDE5, PDE2 and PDE4 are 0.1, 0.28, 12.1, <300 and <300 μM, respectively.

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K134, CAS 189362-06-9

规格	价格/CNY	货期
2 mg	￥ 3,190	5日内发货
25 mg	￥ 11,700	6-8周
50 mg	￥ 15,300	6-8周
100 mg	￥ 19,500	6-8周

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生物活性

化学信息

存储 & 溶解度

参考文献

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产品描述	K134 is an inhibitor of phosphodiesterase 3. The IC50s of K134 for PDE3A, PDE3B, PDE5, PDE2 and PDE4 are 0.1, 0.28, 12.1, >300 and >300 μM, respectively.
靶点活性	PDE3A:0.1 μM, PDE3B:0.28 μM, PDE5:12.1 μM
体外活性	K134 (K-134) inhibits rat platelet aggregation caused by collagen and ADP in a dose-dependent manner in vitro. K134 also inhibits mouse platelet aggregation induced by collagen and ADP in a dose-dependent manner (IC50s: 5.5 μM and 6.7 μM, respectively), in vitro experiments. The half-maximal (50%) inhibitory concentration (IC50) values of K134 are 2.5 μM and 3.2 μM, respectively [1].
体内活性	K134 obviously decreases the incidence of occlusive shunt thrombi at doses above 10 mg/kg (half-maximal effective dose: ED50=11 mg/kg). The effects of PDE3 inhibitors on thrombus formation are also investigated in an arteriovenous shunt model in rats. The plasma concentration of K134 is 0.43±0.08 μM (Cmax) at a dose of 10 mg/kg. K134 obviously prolongs middle cerebral artery (MCA) occlusion time at doses >10 mg/kg and decreases cerebral infarct size at 30 mg/kg in the stroke model (n?=?12, 87.5±5.6 vs. 126.8±7.5 mm3, P<0.01), indicating its potent antithrombotic effect. The overall bleeding risk of K134 is assessed in general in mice. K134 (30 mg/kg; Single oral administration) does not prolong bleeding time at a dose of compared to control (106±5 vs. 110±5 s, not significant). A sufficiently high enough plasma concentration of K134 (13.6±2.3 μM) is detected to inhibit platelet aggregation at 10 min after single administration in mice at a dose of 30 mg/kg, which is the same time point as the above test of bleeding time [1].

别名	OPC33509
分子量	399.48
分子式	C22H29N3O4
CAS No.	189362-06-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

1. Yoshida H, et al. K-134, a phosphodiesterase 3 inhibitor, prevents brain damage by inhibiting thrombus formation in a rat cerebral infarction model. PLoS One. 2012;7(10):e46432.

剂量换算

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请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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