Molidustat (BAY85-3934)
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.
IC50: 对PHD1\PHD2和PHD3的IC50分别为480 nM\280 nM和450 nM.
通过低氧诱导因子脯氨酰羟化酶(HIF-PHs)诱导的氧感应是促红细胞生成素(EPO)表达的主要调节机制.在慢性肾脏疾病(CKD)中,受损的EPO表达导致贫血,这可以通过补充重组人EPO(rhEPO)进行治疗.Molidustat(BAY85-3934)是一种新型的HIF-PH抑制剂.
体外实验:IC50值依赖于反应缓冲液中2-酮戊二酸的浓度.将2-酮戊二酸的浓度从20 μM降低到0.3 μM,测试的化合物效力增加至10倍.反应缓冲液中Fe2+和抗坏血酸的浓度变化分别为30和200时,对抑制剂效力的改变不超过2倍[1].
在体实验:与对照组动物相比,重复剂量的BAY85-3934引起血红蛋白水平升高,而内源性EPO维持在正常生理范围内.在肾功能受损的大鼠中,BAY85-3934可以有效的治疗肾性贫血.不同于rhEPO的治疗,在CKD大鼠模型中,BAY85-3934引起高血压的血压正常化[1].
临床试验:在肾性贫血的患者中,BAY85-3934的临床研究仍在进行.
参考文献：
[1] Flamme I, Oehme F, Ellinghaus P, Jeske M, Keldenich J, Thuss U. Mimicking hypoxia to treat anemia: HIF-stabilizer BAY 85-3934 (Molidustat) stimulates erythropoietin production without hypertensive effects. PLoS One. 2014 Nov 13;9(11):e111838.
- 1. Shaojun Wu, Ying Zhang, et al. "Septin4 promotes cardiomyocytes apoptosis by enhancing the VHL-mediated degradation of HIF-1α." Cell Death Discov. 2021 Jul 6;7(1):172. PMID: 34230460
- 2. Shaojun Wu, Ying Zhang, et al. "Septin4 Aggravates Hypoxia-Induced Cardiomyocytes Injury by Promoting HIF-1α Ubiquitination and Degradation through VHL." Research Square. October 21st, 2020.
- 3. Vijesh J. Bhute, James Harte, et al. "Mannose binding lectin is hydroxylated by collagen prolyl-4-hydroxylase and inhibited by some PHD inhibitors." Kidney360. April 3, 2020.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 314.3 |
| Cas No. | 1154028-82-6 |
| Formula | C13H14N8O2 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥5.68 mg/mL in DMF |
| Chemical Name | 2-(6-morpholinopyrimidin-4-yl)-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-3(2H)-one |
| SDF | Download SDF |
| Canonical SMILES | O=C1C(N2C=CN=N2)=CNN1C3=NC=NC(N4CCOCC4)=C3 |
| 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。 |
质量控制和MSDS
- 批次:
化学结构
相关生物数据
