FG-4592 (ASP1517)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
FG-4592也被称为ASP1517，是2-(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carboxamido)acetic acid，是缺氧诱导因子脯氨酰羟化酶（HIF-PH）的强效小分子抑制剂，HIF-PH是一种酶，可以上调内源人红细胞生成素（EPO）的表达。FG-4592目前正在进行作为口服治疗慢性肾脏疾病（CKD）相关贫血的研究。不同于其它的贫血治疗剂红细胞生成刺激剂（ESAs），FG-4592通过稳定HIF，以不同的机制抑制HIF。以往的研究表明，在没有接受透析的CKD患者和接受透析但并不需要静脉补铁的末期肾病患者中，FG-4592能够纠正和维持血红蛋白水平。
参考文献：
1. Luis Borges. Different modalities of erythropoiesis stimulating agents. Port J Nephrol Hypert 2010; 24(2): 137-145
2. “FibroGen and Astellas announce initiation of phase 3 trial of FG-4592/ASP1517 for treatment of anemia of chronic kidney disease” Fibrogen Press Release. Dec 11 2012
3. “FibroGen announces initiation of phase 2b studies of FG-4592, an oral HIF prolyl hydroxylase inhibitor, for treatment of anemia”
- 1. Nicholson HE, Tariq Z, et al. "HIF-independent synthetic lethality between CDK4/6 inhibition and VHL loss across species." Sci Signal. 2019 Oct 1;12(601). pii: eaay0482. PMID:31575731
- 2. LUKE ERBER. "Functional Proteomics Analysis To Discover And Characterize Oxygen-Dependent Cellular Pathways." UNIVERSITY OF MINNESOTA. 2019.
- 3. Kiriakidis S, Hoer SS, et al. "Complement C1q is hydroxylated by collagen prolyl 4 hydroxylase and is sensitive to off-target inhibition by prolyl hydroxylase domain inhibitors that stabilize hypoxia-inducible factor." Kidney Int. 2017 May 12. pii: S0085-2538(17)30180-1. PMID:28506759
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 352.34 |
| Cas No. | 808118-40-3 |
| Formula | C19H16N2O5 |
| Solubility | insoluble in H2O; ≥17.62 mg/mL in DMSO; ≥2.9 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | 2-[(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carbonyl)amino]acetic acid |
| SDF | Download SDF |
| Canonical SMILES | CC1=NC(=C(C2=C1C=C(C=C2)OC3=CC=CC=C3)O)C(=O)NCC(=O)O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验 [1]: | |
|
细胞系 |
PC-12细胞 |
|
制备方法 |
在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液，一般步骤如下：请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。 |
|
反应条件 |
5、20或50 μM |
|
实验结果 |
FG-4592对TBHP诱导的细胞死亡具有显著的保护作用。 |
| 动物实验 [1]: | |
|
动物模型 |
脊髓损伤小鼠模型 |
|
给药剂量 |
50 mg/kg/day；腹腔注射；持续7天 |
|
实验结果 |
在脊髓损伤小鼠模型中，给予FG-4592促进损伤修复，同时增加脊髓病变部位神经元的存活率。 |
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其它注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同，但仍处于实验系统误差的允许范围内。 |
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References: [1]. Wu K, Zhou K, Wang Y, Zhou Y, Tian N, Wu Y, Chen D, Zhang D, Wang X, Xu H, Zhang X. Stabilization of HIF-1α by FG-4592 promotes functional recovery and neural protection in experimental spinal cord injury. Brain Res. 2016 Feb 1;1632:19-26. |
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| Description | FG-4592 is an inhibitor of HIF α prolyl hydroxylase. | |||||
| Targets | HIF α prolyl hydroxylase | |||||
| IC50 | ||||||
质量控制和MSDS
- 批次:
化学结构
相关生物数据
相关生物数据
