Eltrombopag (Synonyms: SB 497115) |
カタログ番号GC12513
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Eltrombopagは非ペプチドトロンボポエチン受容体（TPO-R）特異性の作動剤であり、TPO-Rに対するEC₅₀値は0.19µMである。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 496775-61-2
Sample solution is provided at 25 µL, 10mM.
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Eltrombopagは非ペプチドトロンボポエチン受容体（TPO-R）特異性の作動剤であり、TPO-Rに対するEC₅₀値は0.19µMである[1]。Eltrombopagは、TPO-Rシグナル伝達経路を活性化することで、天然のトロンボポエチンの生物機能を模擬し、主に免疫性血小板減少症と化学療法誘発性血小板減少症の処理に使われる。更に、Eltrombopagは、hERGカリウムチャネルに対する阻害作用をも持っている[2]。
正常なCD34+細胞の体外培養物で、Eltrombopag（3µg/mL；4時間）はヒト造血幹細胞で、TPO細胞内シグナル伝達に対するIFN-γの阻害作用を回避できる[3]。MEF細胞で、Eltrombopag（10μM；6.5時間）はBAXのみを発見するMEF細胞でSTS誘発の、caspase-3/7活性が媒介したアポトーシスを阻害したものの、BAKのみを発見するMEF細胞では作用を発揮しなかった[4]。マウス胚性線維芽細胞で、Eltrombopag（0–30μM；24時間）はBAK α4/α6/α7溝と結合でき、BAKの活性化を始め、BAKに依存し、BAXに依存せぬアポトーシスを誘発する[5]。
白血病のマウス移植モデルで、Eltrombopag（0.4-1.0mg/mL；経口投与；50日間）はこれらのマウスで生存率を著しく改善し、Eltrombopag処理のマウスで、移植の白血病細胞はCD11bとCD14の発見を増やした[6]。免疫媒介の骨髄不全のマウスモデルで、Eltrombopag（20μg/g/d；腹腔内；10日間）は、Th1免疫反応と関連するサイトカインを著しく下方制御し、Th2免疫反応と関連するサイトカインを著しく上方制御した[7]。
References:
[1]. Subbarayan R, Srinivasan D, Sadullah Usmani S, et al. Molecular insights on Eltrombopag: potential mitogen stimulants, angiogenesis, and therapeutic radioprotectant through TPO-R activation[J]. Platelets, 2024, 35(1): 2359028.
[2]. Pathak S, Roth M, Verma A, et al. Eltrombopag for the treatment of thrombocytopenia in patients with malignant and non-malignant hematologic disorders[J]. Expert opinion on drug metabolism & toxicology, 2013, 9(12): 1667-1675.
[3]. Alvarado L J, Huntsman H D, Cheng H, et al. Eltrombopag maintains human hematopoietic stem and progenitor cells under inflammatory conditions mediated by IFN-γ[J]. Blood, The Journal of the American Society of Hematology, 2019, 133(19): 2043-2055.
[4]. Spitz A Z, Zacharioudakis E, Reyna D E, et al. Eltrombopag directly inhibits BAX and prevents cell death[J]. Nature communications, 2021, 12(1): 1134.
[5]. Chen M, Hu L, Bao X, et al. Eltrombopag directly activates BAK and induces apoptosis[J]. Cell Death & Disease, 2023, 14(7): 394.
[6]. Roth M, Will B, Simkin G, et al. Eltrombopag inhibits the proliferation of leukemia cells via reduction of intracellular iron and induction of differentiation[J]. Blood, The Journal of the American Society of Hematology, 2012, 120(2): 386-394.
[]. Ding S, Liang X, Zhang T, et al. The effectiveness of rapamycin combined with Eltrombopag in murine models of immune‐mediated bone marrow failure[J]. Journal of Immunology Research, 2020, 2020(1): 1798795.
| 細胞実験[1]: | |
細胞株 | HL60細胞とURE細胞 |
準備方法 | 濃度が増加するEltrombopagでHL60細胞とURE細胞を72時間インキュベートした。 |
反応条件 | 0.1-20μM；72時間 |
アプリケーション | ヒトとマウス白血病細胞で、Eltrombopagは、細胞の分裂率を減らし、細胞周期のG1期を遮断した。 |
| 動物実験 [1]: | |
動物モデル | 白血病のマウス移植モデル |
準備方法 | 尾静脈を通じて、1000万個のHL60細胞をNSGマウスに静脈内注射し、+3日目から、飲用水の中の1.0mg/mLのEltrombopag、または未処理の飲用水でマウスを処理した。 |
投与形態 | 0.4-1.0mg/mL；経口投与；50日間 |
アプリケーション | Eltrombopagの処理は、これらのマウスで生存率を著しく改善し、Eltrombopag処理のマウスで、移植の白血病細胞はCD11bとCD14の発見を増やした。 |
References: | |
| Cas No. | 496775-61-2 | SDF | |
| 同義語 | SB 497115 | ||
| Chemical Name | 3-[(5E)-5-[[2-(3,4-dimethylphenyl)-5-methyl-3-oxo-1H-pyrazol-4-yl]hydrazinylidene]-6-oxocyclohexa-1,3-dien-1-yl]benzoic acid | ||
| Canonical SMILES | CC1=C(C=C(C=C1)N2C(=O)C(=C(N2)C)NN=C3C=CC=C(C3=O)C4=CC(=CC=C4)C(=O)O)C | ||
| Formula | C25H22N4O4 | M.Wt | 442.47 |
| 溶解度 | ≥ 13.2mg/mL in DMSO | Storage | Store at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.26 mL | 11.3002 mL | 22.6004 mL |
| 5 mM | 452 μL | 2.26 mL | 4.5201 mL |
| 10 mM | 226 μL | 1.13 mL | 2.26 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)