Emetine dihydrochloride hydrate
(Synonyms: 吐根碱盐酸盐水合物) 目录号 : GC32048
Emetine dihydrochloride hydrate是一种抗原虫药物，能够用于肠和组织阿米巴病的治疗。
Cas No.:7083-71-8
Sample solution is provided at 25 µL, 10mM.
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Emetine dihydrochloride hydrate is an antigen parasite drug that can be used for the treatment of intestinal and tissue amoebic diseases[1].
Emetine dihydrochloride is reported to have an IC50 value of 1nM on the drug sensitive 3D7 P. falciparum parasite strains. Dose response curves are determined for both drugs using K1 resistant isolates and IC50 values of 47nM and 2.6nM established for Emetine dihydrochloride hydrate and DHA, respectively[1]. After the lymphoblasts are treated with Emetine dihydrochloride hydrate, the expression level of the mutant allele is elevated almost equally to the wild-type alleles by direct sequencing of the corresponding cDNA[2]. Emetine dihydrochloride hydrate is identified as a lead compound with significant concentration dependent suppression of PEDF-induced TNF secretion and an IC50 of 146nM. Emetine dihydrochloride hydrate inhibits PEDF-mediated TNF release without affecting cell viability and binds to PEDF receptor ATGL with high-binding affinity (Kd=14.3nM)[3]. Emetine dihydrochloride hydrate reduces cell viability, induces apoptosis, promptes AML cells towards differentiation and downregulates HIF-1α[4].
Emetine dihydrochloride hydrate (0.002, 0.02, 0.2 and 2mg/kg) not only attenuates blood glucose levels in dose-dependent way but also induces a persistent attenuation of blood glucose levels. Daily administration of Emetine dihydrochloride hydrate dose-dependently attenuates hyperglycemic response by D21. Consistent with this observation, administration of Emetine dihydrochloride hydrate, but not the vehicle control, results in a sustained attenuation of blood glucose levels. Emetine dihydrochloride hydrate improves disease severity in a spontaneous model of NOD T1D[3]. Emetine dihydrochloride hydrate (1mg/kg) reduces both leukemia burden in an in vivo xenotransplantation mouse model and the clonogenic capacity of leukemic cells upon treatment[4].
References:
[1]. Matthews H, et al. Drug repositioning as a route to anti-malarial drug discovery: preliminary investigation of the in vitro anti-malarial efficacy of emetine dihydrochloride hydrate. Malar J. 2013 Oct 9;12:359.
[2]. Wu L, et al. PRRT2 truncated mutations lead to nonsense-mediated mRNA decay in Paroxysmal Kinesigenic Dyskinesia. Parkinsonism Relat Disord. 2014 Dec;20(12):1399-404.
[3]. Hudson LK, et al. Emetine Di-HCl attenuates Type 1 diabetes mellitus in mice. Mol Med. 2016 Jun 10;22.
[4]. Cornet-Masana JM, et al. Emetine induces chemosensitivity and reduces clonogenicity of acute myeloid leukemia cells. Oncotarget. 2016 Apr 26;7(17):23239-50.
Emetine dihydrochloride hydrate是一种抗原虫药物，能够用于肠和组织阿米巴病的治疗[1]。
据报道，Emetine dihydrochloride对3D7型恶性疟原虫药敏株的IC50值为1nM。采用K1耐药菌株确定了两种药物的剂量反应曲线，并分别建立了Emetine dihydrochloride hydrate和DHA的IC50值为47nM和2.6nM。用Emetine dihydrochloride hydrate处理淋巴母细胞后，通过对相应cDNA的直接测序，突变等位基因的表达水平几乎与野生型等位基因相同[2]。Emetine dihydrochloride hydrate是一种先导化合物，对PEDF诱导的TNF分泌具有明显的浓度依赖性抑制作用，IC50为146nM。Emetine dihydrochloride hydrate抑制PEDF介导的TNF释放而不影响细胞活力，并以高结合亲和力（Kd=14.3nM）与PEDF受体ATGL结合[3]。Emetine dihydrochloride hydrate降低细胞活力，诱导细胞凋亡，促进AML细胞分化，下调HIF-1α[4]。
Emetine dihydrochloride hydrate（0.002、0.02、0.2和2mg/kg）不仅呈剂量依赖性地降低血糖水平，而且能诱导血糖水平持续降低。每日给予Emetine dihydrochloride hydrate剂量依赖性降低高血糖反应至21d。与这一观察结果一致，给予Emetine dihydrochloride hydrate，而不是对照，导致血糖水平持续下降。Emetine dihydrochloride hydrate改善NOD T1D自发性模型的疾病严重程度[3]。Emetine dihydrochloride hydrate（1mg/kg）可降低体内异种移植小鼠模型的白血病负担和治疗后白血病细胞的克隆生成能力[4]。
| Cell experiment [1]: | |
Cell lines | AML cell lines HL-60 (ACC-3), KG-1 (ACC-14), MonoMac-1 (ACC-252), Kasumi-1 (ACC-220) and THP-1 (ACC-16). |
Preparation Method | 7.5×105 cells per mL were cultured in 96-well plates in complete medium. Emetine dihydrochloride hydrate and Ara-C were added at indicated concentrations. Cell viability was measured by 7-AAD (eBioscience) exclusion and Hoechst33342 positivity staining by flow cytometry; and cell count was obtained by volume in a FACSCantoII cytometer (BD). Statistical analysis and EC50 determination were calculated in GraphPad (Prism software). FlowJo software (TriStar) was used for flow cytometry analysis. |
Reaction Conditions | 0-2μM; 24h |
Applications | The IC50 range of Emetine dihydrochloride hydrate in these cell lines is 40-320nM. |
| Animal experiment [2]: | |
Animal models | 6 to 8 weeks old C57Bl/6 mice, Type 1 diabetes mellitus model. |
Preparation Method | T1D is induced by administration of streptozotocin (50mg/kg dissolved in sodium citrate buffer, pH 4.5) to 6 to 8 weeks old C57Bl/6 mice intraperitoneally (i.p.) once each day for 5 consecutive days. Mice are given water supplemented with 10% sucrose for six days to prevent sudden hypoglycemia during streptozotocin administration. For time course studies, body weight and blood glucose are measured every other day. Blood glucose is measured with a FreeStyle Lite blood glucose meter. For studies with emetine, mice receive daily administration of Emetine dihydrochloride hydrate (0.002, 0.02, 0.2 and 2mg/kg) or saline. Blood glucose with either FreeStyle Lite blood glucose meter or Bayer Contour blood glucose meter and body weight are measured once weekly. At the end of each study, mice are euthanized by CO2 asphyxiation. Blood and pancreas are collected for cytokine analysis. |
Dosage form | 0.002, 0.02, 0.2 and 2mg/kg; i.p. |
Applications | Emetine dihydrochloride hydrate (0.002, 0.02, 0.2 and 2 mg/kg) not only attenuates blood glucose levels in dose-dependent way but also induces a persistent attenuation of blood glucose levels. Emetine dihydrochloride hydrate Administration Attenuates Hyperglycemia and Reduces Pancreatic TNF Levels in T1D. |
References: | |
| Cas No. | 7083-71-8 | SDF | |
| 别名 | 吐根碱盐酸盐水合物 | ||
| Canonical SMILES | CC[C@@H]1[C@H](C[C@@]2([H])C3=CC(OC)=C(OC)C=C3CCN2C1)C[C@]4([H])C5=CC(OC)=C(OC)C=C5CCN4.[H]Cl.[H]Cl.O | ||
| 分子式 | C29H40N2O4 . 2 HCl . H2O | 分子量 | 571.58 |
| 溶解度 | 100mg/mL in water; 1mg/mL in chloroform. | 储存条件 | Store at 2-8°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7495 mL | 8.7477 mL | 17.4954 mL |
| 5 mM | 0.3499 mL | 1.7495 mL | 3.4991 mL |
| 10 mM | 0.175 mL | 0.8748 mL | 1.7495 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
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