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R 59-022

产品编号 T16709 CAS 93076-89-2

别名: Diacylglycerol kinase inhibitor I, DKGI-I

R 59-022 is a 5-HTR antagonist and activates protein kinase C (PKC). R 59-022 is a diacylglycerol kinase inhibitor (IC50=2.8 μM). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.

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R 59-022, CAS 93076-89-2

规格	价格/CNY	货期
1 mg	￥ 647	35日内发货
5 mg	￥ 1,570	35日内发货
10 mg	￥ 2,740	35日内发货
50 mg	￥ 11,700	35日内发货

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	R 59-022 is a 5-HTR antagonist and activates protein kinase C (PKC). R 59-022 is a diacylglycerol kinase inhibitor (IC50=2.8 μM). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.
靶点活性	DGK:2.8 μM
体外活性	R 59-022 is able to interrupt thrombin-induced inositol lipid cycling at the level of diacylglycerol and leads to an elevation of protein kinase C activity, in the intact platelet. R 59-022 blocks entry of EBOV pseudotypes in a concentration-dependent manner (IC50: ~5 μM). R 59-022, an inhibitor of filovirus entry, prevents the macropinocytic uptake of filoviral particles, inhibits entry mediated by multiple filovirus GPs, and blocks replicative EBOV growth. R 59-022 dose-dependent decreases in entry by the VLPs harboring the EBOV GP (IC50: ~2 μM). R 59-022 (10 μM) potentiates aggregation, but not shape change induced by sub-maximal concentrations of thrombin. R59022 (10 μM) had no significant effect on the dose-response curve for the mobilization of intracellular Ca2+ by thrombin in either the presence or the absence of extracellular Ca2+. R 59-022 (2-12 μM; 1 hour) can inhibit EBOV GP-mediated entry in multiple cell types. R 59-022 (5 μM; 30 minutes) blocks macropinocytosis in vero cells[1][2][5].

别名	Diacylglycerol kinase inhibitor I, DKGI-I
分子量	459.58
分子式	C27H26FN3OS
CAS No.	93076-89-2

存储

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

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参考文献

1. de Chaffoy de Courcelles DC, et al. R 59 022, a diacylglycerol kinase inhibitor. Its effect on diacylglycerol and thrombin-induced C kinase activation in the intact platelet. J Biol Chem. 1985 Dec 15;260(29):15762-70. 2. Nunn DL, et al. A diacylglycerol kinase inhibitor, R59022, potentiates secretion by and aggregation of thrombin-stimulated human platelets. Biochem J. 1987 May 1;243(3):809-13. 3. Jones JA, et al. Influence of phorbol esters, and diacylglycerol kinase and lipase inhibitors on noradrenalinerelease and phosphoinositide hydrolysis in chromaffin cells. Br J Pharmacol. 1990 Nov;101(3):521-6. 4. Boroda S, et al. Dual activities of ritanserin and R59022 as DGKα inhibitors and serotonin receptor antagonists. Biochem Pharmacol. 2017 Jan 1;123:29-39. 5. Stewart CM, et al. A Diacylglycerol Kinase Inhibitor, R-59-022, Blocks Filovirus Internalization in Host Cells. Viruses. 2019 Mar 1;11(3). pii: E206.

剂量换算

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体内实验配液计算器

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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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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