当荧光素酶报告基因转染小鼠 BAF3 细胞时，艾曲波帕（0.002-50 μM；4 小时）表现出活性 [1]。艾曲波帕（30 μM；120 分钟）对细胞中 p-N2C-Tpo STAT5 的激活方式有影响 [1]。在巨核细胞中，艾曲波帕（30 μM；120 分钟）刺激 p-STAT5[1]。艾曲波帕（0.1 nM-10 μM；30 分钟）刺激 BAF3/hTpoR 细胞增殖 [1]。艾曲波帕（0.03-3 μM；10 天）促进骨髓中的 CD34+ 细胞分化为 CD41+ 巨核细胞 [1]。 N2C-Tpo 细胞凋亡受艾曲波帕（0-3 μM；72 小时）影响[1]。艾曲波帕的 MIC50 为 0.3 mg/L，可有效防止肺炎球菌的生长，但对革兰氏阴性菌无效 [3]。艾曲波帕（0 -200 mg/L；24 小时；HepG2 和 Caco-2 细胞）的 MIC50 为 1.5 mg/L，联合使用时效果低于万古霉素（MIC50 为 1.2 mg/L）。 L[3]。在 Huh7 细胞中，艾曲波帕（0 或 10 μg/mL；72 小时）强烈促进 G0/G1 期阻滞 [5]。对于 HCC 细胞系，艾曲波帕（0.1-100 μg/mL；72 小时）表现出抗增殖作用 [5]。

黑猩猩可以耐受艾曲波帕乙醇胺（10 mg/kg），每天口服一次，持续五天[1]。埃洛曲波帕奥拉明（17.6 mg/kg；腹膜内注射；每天一次，持续两天）使平均 S 大大降低。小鼠鼻腔感染与金黄色葡萄球菌数量有关[3]。

细胞活力测定[1]
细胞类型： 鼠 BAF3 细胞
测试浓度： 0.002-50 μM
孵育时间： 4 h
实验结果：用人TpoR有效抑制小鼠BAF3细胞，EC50值为0.27 μM。 [1][1]
细胞类型： N2C-Tpo 细胞和 CD34+
测试浓度： N2C-Tpo 细胞为 30 μM； CD34+ 为 0、1、3 和 10 μM
孵育时间：N2C-Tpo 细胞为 120 分钟； CD34+ 30 分钟
实验结果：在 N2C-Tpo 细胞中处理后 60 分钟显示出激活的磷酸-STAT5 和最大信号强度。 CD34+ 治疗后 30 分钟，剂量依赖性激活 STAT5 磷酸化。

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细胞增殖检测[1]
细胞类型： BAF3/hTpoR 细胞
测试浓度： 0.1 nM-10 μM
孵育时间： 2 天
实验结果： 孵育 2 天后，EC50 为 0.03 μM，促进 BAF3/hTpoR 细胞增殖。

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细胞分化测定[1]
细胞类型： CD34+
测试浓度： 0.003, 0.01, 0.03, 0.1, 0.3, 1和 3 μM
孵育时间： 10 天
实验结果：剂量依赖性刺激骨髓 CD34+ 细胞向 CD 的分化

Animal/Disease Models: Female chimpanzees[1]
Doses: 10 mg/kg
Route of Administration: po (oral gavage); 10 mg/kg one time/day; for 5 days
Experimental Results: Appeared a goes up and then goes back tendency of platelet counts after treatment, and demonstrated no bad effects of hematology, coagulation, or clinical chemistry parameters on animal.

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Animal/Disease Models: C57BL/6 male mice (7 weeks, 20-22 g; injected S. aureus (5 × 108 CFU suspended in 40 µL PBS) into the nasal cavities )[3]
Doses: 17.6 mg/kg
Route of Administration: IP; one time/day for 2 days
Experimental Results: Dramatically decreased mean bacterial counts (5.0 × 106 CFU/lung) in the nasal infection model compared with control PBS (5.2 × 107 CFU/lung) lung) mice.

Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
Minimal information is available on the use of eltrombopag during breastfeeding. One breastfed infant with thrombocytosis at birth that was possibly prolonged by eltrombopag in milk. Until more data become available, romiplostim should be used with careful infant monitoring of infant blood parameters during breastfeeding, especially while nursing a newborn or preterm infant. The manufacturer recommends avoiding breastfeeding during the use of eltrombopag. Based on the drug’s half-life, the drug should be eliminated by the mother 8 days after the last dose.
◉ Effects in Breastfed Infants
An infant was born to a mother taking eltrombopag in a maximum dose of 100 mg during pregnancy. At birth, the infant had thrombocytosis, which persisted for a few weeks while the mother was breastfeeding. The extent of breastfeeding and the maternal dose were not stated. The authors felt that the persistence of thrombocytosis in the infant was possibly caused by eltrombopag in milk.
◉ Effects on Lactation and Breastmilk
Relevant published information was not found as of the revision date.

[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]. Lee H, et al. Repurposing Eltrombopag for Multidrug Resistant Staphylococcus aureus Infections. Antibiotics (Basel). 2021 Nov 9;10(11):1372.
[4]. Juan Zhu, et al. Identification of Eltrombopag as a Repurposing Drug Against Staphylococcus epidermidis and its Biofilms. Curr Microbiol. 2021 Feb 21.
[5]. Kurokawa T, et al. The Eltrombopag antitumor effect on hepatocellular carcinoma. Int J Oncol. 2015 Nov;47(5):1696-702.

Eltrombopag is a hydrazine in which each nitrogen atom is substituted, one by a 3'-carboxy-2-hydroxy[1,1'-biphenyl]-3-yl group and the other by a 1-(3,4-dimethylphenyl)-3-methyl-5-oxo-1,5-dihydro-4H-pyrazol-4-ylidene group. A small molecule agonist of the c-mpl (TpoR) receptor (the physiological target of the hormone thrombopoietin), it has been developed as a medication for conditions that lead to thrombocytopenia (abnormally low platelet counts). It has a role as a thrombopoietin receptor agonist and a xenobiotic. It is a member of hydrazines, a member of pyrazoles and a member of benzoic acids.
Eltrombopag is a Thrombopoietin Receptor Agonist. The mechanism of action of eltrombopag is as a Thrombopoietin Receptor Agonist, and Organic Anion Transporting Polypeptide 1B1 Inhibitor, and Breast Cancer Resistance Protein Inhibitor, and UGT1A1 Inhibitor, and UGT1A3 Inhibitor, and UGT1A4 Inhibitor, and UGT1A6 Inhibitor, and UGT1A9 Inhibitor, and UGT2B7 Inhibitor, and UGT2B15 Inhibitor. The physiologic effect of eltrombopag is by means of Increased Megakaryocyte Maturation, and Increased Platelet Production.
See also: Romiplostim (annotation moved to); Eltrombopag (annotation moved to).

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Drug Indication
Revolade is indicated for the treatment of adult patients with primary immune thrombocytopenia (ITP) who are refractory to other treatments (e. g. corticosteroids, immunoglobulins) (see sections 4. 2 and 5. 1). Revolade is indicated for the treatment of paediatric patients aged 1 year and above with primary immune thrombocytopenia (ITP) lasting 6 months or longer from diagnosis and who are refractory to other treatments (e. g. corticosteroids, immunoglobulins) (see sections 4. 2 and 5. 1). Revolade is indicated in adult patients with chronic hepatitis C virus (HCV) infection for the treatment of thrombocytopenia, where the degree of thrombocytopenia is the main factor preventing the initiation or limiting the ability to maintain optimal interferon-based therapy (see sections 4. 4 and 5. 1). Revolade is indicated in adult patients with acquired severe aplastic anaemia (SAA) who were either refractory to prior immunosuppressive therapy or heavily pretreated and are unsuitable for haematopoietic stem cell transplantation (see section 5. 1).

C25H22N4O4

442.47

442.164

496775-61-2

Eltrombopag Olamine;496775-62-3;(E/Z)-Eltrombopag-13C4;1217230-31-3

135449332

Typically exists as solid at room temperature

1.3±0.1 g/cm3

656.8±65.0 °C at 760 mmHg

242-244ºC

351.0±34.3 °C

0.0±2.1 mmHg at 25°C

1.667

3.7

114.59

3

7

5

33

812

0

O=C1C(=C(C([H])([H])[H])N([H])N1C1C([H])=C([H])C(C([H])([H])[H])=C(C([H])([H])[H])C=1[H])/N=N/C1=C([H])C([H])=C([H])C(=C1O[H])C1C([H])=C([H])C([H])=C(C(=O)O[H])C=1[H]

SVOQIEJWJCQGDQ-UHFFFAOYSA-N

InChI=1S/C25H22N4O4/c1-14-10-11-19(12-15(14)2)29-24(31)22(16(3)28-29)27-26-21-9-5-8-20(23(21)30)17-6-4-7-18(13-17)25(32)33/h4-13,28,30H,1-3H3,(H,32,33)

3-[2-[(2Z)-1-(3,4-Dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazinyl]-2-hydroxy-[1,1-biphenyl]-3-carboxylic acid

Eltrombopag; SB497115; SB-497115; SB 497115; SB497115GR; trade name: PROMACTA

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

配方 1 中的溶解度: ≥ 1 mg/mL (2.26 mM) (饱和度未知) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 10.0 mg/mL澄清的DMSO储备液加入到400 μL PEG300中，混匀；再将50 μL Tween-80+加入到上述溶液中，混匀；然后加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。