R 59-022 hydrochloride DKGI-I hydrochloride; Diacylglycerol kinase inhibitor I hydrochloride,98.88%

产品编号:Bellancom-107613A| CAS NO:93076-98-3| 分子式:C27H27ClFN3OS| 分子量:496.04

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货号 包装 价格 库存与货期 购买量 操作
Bellancom-107613A
1100.00 杭州 北京(现货)
Bellancom-107613A
1800.00 杭州 北京(现货)
Bellancom-107613A
3600.00 杭州 北京(现货)
Bellancom-107613A
5800.00 杭州 北京(现货)

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R 59-022 hydrochloride DKGI-I hydrochloride; Diacylglycerol kinase inhibitor I hydrochloride

产品介绍 R 59-022 (DKGI-I) hydrochloride 是一种 DGK 抑制剂 (IC50: 2.8 µM)。R 59-022 hydrochloride 抑制 OAG 磷酸化为 OAPA。R 59-022 hydrochloride 是一种 5-HT Receptor 拮抗剂,可激活蛋白激酶 C (PKC)。R 59-022 增强血小板中凝血酶诱导的甘油二酯的产生,并抑制嗜中性粒细胞中磷脂酸的产生。
生物活性

R 59-022 (DKGI-I) hydrochloride is a DGK inhibitor (IC50: 2.8 µM). R 59-022 hydrochloride inhibits the phosphorylation of OAG to OAPA. R 59-022 hydrochloride is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 hydrochloride potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils[4].

体外研究

R 59-022 (10 μM,1 分钟) hydrochloride 增强血小板聚集
R 59-022 (30 μM,0-60 分钟) hydrochloride 增加嗜铬细胞中去甲肾上腺素的释放
R 59-022 (40 μM,30 分钟) hydrochloride 激活 HeLa 和 U87 细胞中的 PKC[4]
R 59-022 (0-10 μM,4 小时) hydrochloride 阻断 EBOV GP 进入 Vero 细胞[5]

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[4]

Cell Line: HeLa cells
Concentration: 40 uM
Incubation Time: 30 min
Result: Increased the phosphorylation of PKC downstream targets by about 2.5-fold.
体内研究
(In Vivo)

R 59-022 (2 mg/kg,腹腔注射,12 天) hydrochloride 显着增加植入 U87 GBM 细胞的 SCID 小鼠的中位生存期[6]

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SCID mice implanted with U87 GBM cells[6]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Increased median survival and decreased tumor volume.
体内研究

R 59-022 (2 mg/kg,腹腔注射,12 天) hydrochloride 显着增加植入 U87 GBM 细胞的 SCID 小鼠的中位生存期[6]

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SCID mice implanted with U87 GBM cells[6]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Increased median survival and decreased tumor volume.
体内研究

R 59-022 (2 mg/kg,腹腔注射,12 天) hydrochloride 显着增加植入 U87 GBM 细胞的 SCID 小鼠的中位生存期[6]

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SCID mice implanted with U87 GBM cells[6]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Increased median survival and decreased tumor volume.
性状Solid
溶解性数据
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

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