Eltrombopag 艾曲波帕; SB-497115|cas:496775-61-2|西域试剂

Eltrombopag 艾曲波帕; SB-497115,99.73%

产品编号：Bellancom-15306| CAS NO：496775-61-2| 分子式：C₂₅H₂₂N₄O₄| 分子量：442.47

Eltrombopag是一种血小板生成素 (TPO) 受体激动剂，治疗导致血小板减少的某些病症。

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-15306	￥780.00	杭州北京（现货）
Bellancom-15306	￥2350.00	杭州北京（现货）
Bellancom-15306	￥2800.00	杭州北京（现货）

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Eltrombopag 艾曲波帕; SB-497115

产品介绍

Eltrombopag (SB-497115) 是一种具有口服活性的 thrombopoietin-receptor 非肽激动剂。Eltrombopag 可促血小板的活性，用于研究血小板计数低的慢性免疫性血小板减少症。Eltrombopag 可用于心血管的研究。Eltrombopag 对多药耐药的金黄色葡萄球菌 (Staphylococcus aureus) 也有很强的抑制作用。Eltrombopag 还可诱导肝癌细胞凋亡 (apoptosis)。

生物活性

Eltrombopag (SB-497115) is an orally active thrombopoietin receptor nonpeptide agonist. Eltrombopag owns thrombopoietic activity, and has been used to research low blood platelet counts with chronic immune thrombocytopenia. Eltrombopag can be used for the research of cardiovascular. Eltrombopag also has highly inhibitory effects against multidrug resistant Staphylococcus aureus. Eltrombopag can induce apoptosis in hepatocellular carcinomab (HCC) as well^[4]^[5].

体外研究

Eltrombopag (0.002-50 μM; 4 h) possesses activity in murine BAF3 cells transfected with the luciferase reporter gene.
Eltrombopag (30 μM; 120 min) affects the activates of p-STAT5 in N2C-Tpo cells.
Eltrombopag (30 μM; 120 min) activates p-STAT5 in megakaryocytes.
Eltrombopag (0.1 nM-10 μM; 30 min) stimulates proliferation of BAF3/hTpoR cells.
Eltrombopag (0.03-3 μM; 10 days) increases the differentiation of bone marrow CD34⁺ cells into CD41⁺ megakaryocytes.
Eltrombopag (0-3 μM; 72 h) affects N2C-Tpo cell apoptosis.
Eltrombopag efficiently inhibits Pneumococcal growth with MIC₅₀ of 0.3 mg/L, but shows no activity against Gram-negative bacteria.
Eltrombopag (0-200 mg/L; 24 h; Caco-2 and HepG2 cells) inhibits Staphylococcus aureus growth with an MIC₅₀ of 1.5 mg/L, and exhibits higher potency when co-treats with Vancomycin (HY-B0671) with an MIC₅₀ of 1.2 mg/L.
Eltrombopag (0 or 10 μg/mL; 72 h) significantly induces G0/G1 phase arrest in Huh7 cells^[5].
Eltrombopag (0.1-100 μg/mL; 72 h) exhibits anti-proliferative activity against HCC cell lines^[5].

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

Cell Viability Assay

Cell Line:	Murine BAF3 cells
Concentration:	0.002-50 μM
Incubation Time:	4 h
Result:	Effectively inhibited murine BAF3 cells with human TpoR with an EC₅₀ value of 0.27 μM.

Cell Line:	N2C-Tpo cells and CD34⁺
Concentration:	30 μM for N2C-Tpo cells; 0, 1, 3 and 10 μM for CD34⁺
Incubation Time:	120 min for N2C-Tpo cells; 30 min for CD34⁺
Result:	Activated phospho-STAT5 and maximum signal intensity exhibited at 60 minutes after treatment in N2C-Tpo cells. Dose-dependently activated STAT5 phosphorylation at 30 minutes after treatment in CD34⁺.

Cell Proliferation Assay

Cell Line:	BAF3/hTpoR cells
Concentration:	0.1 nM-10 μM
Incubation Time:	2 days
Result:	Promoted BAF3/hTpoR cells proliferation after incubated for 2 days with an EC50 of 0.03 μM.

Cell Differentiation Assay

Cell Line:	CD34⁺
Concentration:	0.003, 0.01, 0.03, 0.1, 0.3, 1 and 3 μM
Incubation Time:	10 days
Result:	Dose-dependently stimulated the differentiation from bone marrow CD34⁺ cells to CD41⁺ megakaryocytes with an EC50 value of 0.1 μM.

Apoptosis Analysis

Cell Line:	N2C-Tpo cells
Concentration:	0, 0.003, 0.01, 0.03, 0.1, 0.3, 1 and 3 μM
Incubation Time:	72 hours
Result:	Exhibited dose-dependently antiapoptotic effects N2C-Tpo cells with a concentration over 0.03 μM.

Cell Proliferation Assay^[5]

Cell Line:	Huh7, HepG2 and Hep3B cells (preloaded with iron (500 μg/ml FAC) for 24 h)
Concentration:	0.1-100 μg/mL
Incubation Time:	72 h
Result:	Exhibited anti-proliferative activity against HCC cell lines with IC₅₀s of 5.7 μg/ml for Huh7, 5.4 μg/ml for HepG2, and 4.7 μg/ml for Hep3B.

Cell Cycle Analysis^[5]

Cell Line:	Huh7 cells
Concentration:	0 or 10 μg/mL
Incubation Time:	72 h
Result:	Significantly induced G0/G1 phase arrest.

体内研究
(In Vivo)

Eltrombopag Olamine (10 mg/kg; p.o. once a day for 5 days) shows good tolerance in chimpanzees.
Eltrombopag Olamine (17.6 mg/kg; i.p.; once a day for 2 days) significantly reduces mean S. aureus counts in mice nasal infection.

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

Animal Model:	Female chimpanzees
Dosage:	10 mg/kg
Administration:	Oral gavage; 10 mg/kg once a day; for 5 days
Result:	Appeared a goes up and then goes back tendency of platelet counts after treatment, and showed no bad effects of hematology, coagulation, or clinical chemistry parameters on animal.

Animal Model:	C57BL/6 male mice (7 weeks, 20-22 g; injected S. aureus (5 × 10⁸ CFU suspended in 40 µL PBS) into the nasal cavities)
Dosage:	17.6 mg/kg
Administration:	IP; once a day for 2 days
Result:	Significantly reduced mean bacterial counts (5.0 × 10⁶ CFU/lung) in the nasal infection model compared with control PBS (5.2 × 10⁷ CFU/lung) mice.

体内研究

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

Animal Model:	Female chimpanzees
Dosage:	10 mg/kg
Administration:	Oral gavage; 10 mg/kg once a day; for 5 days
Result:	Appeared a goes up and then goes back tendency of platelet counts after treatment, and showed no bad effects of hematology, coagulation, or clinical chemistry parameters on animal.

Animal Model:	C57BL/6 male mice (7 weeks, 20-22 g; injected S. aureus (5 × 10⁸ CFU suspended in 40 µL PBS) into the nasal cavities)
Dosage:	17.6 mg/kg
Administration:	IP; once a day for 2 days
Result:	Significantly reduced mean bacterial counts (5.0 × 10⁶ CFU/lung) in the nasal infection model compared with control PBS (5.2 × 10⁷ CFU/lung) mice.

体内研究

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

Animal Model:	Female chimpanzees
Dosage:	10 mg/kg
Administration:	Oral gavage; 10 mg/kg once a day; for 5 days
Result:	Appeared a goes up and then goes back tendency of platelet counts after treatment, and showed no bad effects of hematology, coagulation, or clinical chemistry parameters on animal.

Animal Model:	C57BL/6 male mice (7 weeks, 20-22 g; injected S. aureus (5 × 10⁸ CFU suspended in 40 µL PBS) into the nasal cavities)
Dosage:	17.6 mg/kg
Administration:	IP; once a day for 2 days
Result:	Significantly reduced mean bacterial counts (5.0 × 10⁶ CFU/lung) in the nasal infection model compared with control PBS (5.2 × 10⁷ CFU/lung) mice.

性状

Solid

溶解性数据

In Vitro:

DMSO : 8.33 mg/mL (18.83 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2600 mL	11.3002 mL	22.6004 mL
5 mM	0.4520 mL	2.2600 mL	4.5201 mL
10 mM	0.2260 mL	1.1300 mL	2.2600 mL

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1 mg/mL (2.26 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (2.26 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在西域网站选购。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

. Erickson-Miller CL, et al. Preclinical activity of eltrombopag (SB-497115), an oral, nonpeptide thrombopoietin receptor agonist. Stem Cells. 2009 Feb;27(2):424-30. [Content Brief]

. Erickson-Miller CL, et al. Discovery and characterization of a selective, nonpeptidyl thrombopoietin receptor agonist. Exp Hematol. 2005 Jan;33(1):85-93. [Content Brief]

. Lee H, et al. Repurposing Eltrombopag for Multidrug Resistant Staphylococcus aureus Infections. Antibiotics (Basel). 2021 Nov 9;10(11):1372. [Content Brief]

[4]. Juan Zhu, et al. Identification of Eltrombopag as a Repurposing Drug Against Staphylococcus epidermidis and its Biofilms. Curr Microbiol. 2021 Feb 21. [Content Brief]

[5]. Kurokawa T, et al. The Eltrombopag antitumor effect on hepatocellular carcinoma. Int J Oncol. 2015 Nov;47(5):1696-702. [Content Brief]

化学品安全说明书(MSDS)

下载MSDS

质检证书(COA)

产品编号(Item Number)

批号(Lot Number)

海关编码	2933990090

1. 物质的识别

产品名：	Eltrombopag
CAS号：	496775-61-2
制造商/供应商：	西域试剂网站：www.hzbp.cn 邮件：13911702513@139.com

2. 合成/成分数据

产品名：	Eltrombopag
别名：	SB-497115-GR, SB497115
分子式：	C25H22N4O4
分子量：	442.47

3. 急救措施

吸入后：	如果吸入，移至空气新鲜处，如果呼吸困难，给输氧，如呼吸停止，给予人工呼吸。
皮肤接触后：	用大量的水冲洗，移除污染的衣服和鞋子。
眼睛接触后：	检查并取下隐形眼镜，并用大量的水冲洗；呼叫医生。
吞食后：	如果吞食，用大量纯净水漱口；呼叫医生。

4. 消防措施

适当的灭火剂：	雾状水，二氧化碳，干粉或泡沫。
防护设备：	穿戴自给式呼吸器和防护服，以防止与皮肤和眼睛接触。

5. 泄漏应急处理

安全防范措施：	封锁泄漏区域；穿戴自给式呼吸器，防护服和厚橡胶手套。
清洁/收集措施：	使用液体粘合原料（硅藻土，通用粘合剂）吸取精细粉末；使用酒精擦洗表面和设备除去污渍；根据第11条处理被污染的材料。

6. 处理和储存

安全处理说明：	避免吸入和接触皮肤，眼睛及衣物；材料可能略微具有刺激性。
储存：	粉末型式 -20°C 3年；4°C 2年溶于溶剂 -80°C 6个月；-20°C 1个月

7. 接触控制和个人防护

呼吸设备：	NIOSH / MSHA认可的呼吸器。
双手保护：	耐化学腐蚀的橡胶手套。
眼睛防护：	化学安全护目镜。

8. 稳定性和反应活性

稳定性：	按照说明存储是稳定的；避免强氧化剂。
热分解/其他要避免的情况：	避免光和热。

9. 毒性资料

急性毒性：	无可用资料。
主要刺激性影响：	无可用资料。
在皮肤上：	无可用资料。
对眼睛：	无可用资料；可能具有刺激性。

10. 生态资料

一般注意事项：

无可用资料。

11. 废弃处置

按照所在国家，省份，县市和地方的法规处置。

12. 运输信息

正确的运输名称：	无
非危险品运输：	这种物质被视为非危险品运输。

13. 法规信息

尚未有针对此产品作出的化学安全性评估。

14. 其他信息

[1]. Erickson-Miller CL, et al. Preclinical activity of eltrombopag (SB-497115), an oral, nonpeptide thrombopoietin receptor agonist. Stem Cells. 2009 Feb;27(2):424-30.

[2]. Erickson-Miller CL, et al. Discovery and characterization of a selective, nonpeptidyl thrombopoietin receptor agonist. Exp Hematol. 2005 Jan;33(1):85-93.

[3]. McHutchison JG, et al. Eltrombopag for thrombocytopenia in patients with cirrhosis associated with hepatitis C. N Engl J Med. 2007 Nov 29;357(22):2227-36.

[4]. Jenkins JM, et al. Phase 1 clinical study of eltrombopag, an oral, nonpeptide thrombopoietin receptor agonist. Blood. 2007 Jun 1;109(11):4739-41.

[5]. Saleh MN, et al. Safety and efficacy of eltrombopag for treatment of chronic immune thrombocytopenia: results of the long-term, open-label EXTEND study. Blood. 2013 Jan 17;121(3):537-45.

Eltrombopag 艾曲波帕; SB-497115,99.73%

Eltrombopag 艾曲波帕; SB-497115

化学品安全说明书(MSDS)

质检证书(COA)

1. 物质的识别

2. 合成/成分数据

3. 急救措施

4. 消防措施

5. 泄漏应急处理

6. 处理和储存

7. 接触控制和个人防护

8. 稳定性和反应活性

9. 毒性资料

10. 生态资料

11. 废弃处置

12. 运输信息

13. 法规信息

14. 其他信息

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