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ML 221

Cat. No. 4748 3 篇引用文献 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Apelin antagonist
化学名： 5-[(4-Nitrobenzoyl)oxy]-2-[(2-pyrimidinylthio)methyl]-4H-pyran-4-one
纯度： ≥99% (HPLC)
说明书
引用文献 (3)
评论
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for ML 221

ML 221 is an apelin receptor (APJ) antagonist (IC50 values are 0.70 and 1.75 μM in a cAMP assay and β-arrestin assay, respectively). Displays >37-fold selectivity over the closely related angiotensin II type 1 (AT1) receptor. Exhibits no toxicity towards human hepatocytes at concentrations >50 μM.

技术数据 for ML 221

分子量 385.35
公式 C17H11N3O6S
储存 Store at +4°C
纯度 ≥99% (HPLC)
CAS Number 877636-42-5
PubChem ID 7217941
InChI Key UASIRTUMPRQVFY-UHFFFAOYSA-N
Smiles O=C(C3=CC=C([N+]([O-])=O)C=C3)OC1=COC(CSC2=NC=CC=N2)=CC1=O

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for ML 221

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 3.85 10

制备储备液 for ML 221

以下数据基于产品分子量 385.35。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
0.1 mM 25.95 mL 129.75 mL 259.5 mL
0.5 mM 5.19 mL 25.95 mL 51.9 mL
1 mM 2.6 mL 12.98 mL 25.95 mL
5 mM 0.52 mL 2.6 mL 5.19 mL

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参考文献 for ML 221

参考文献是支持产品生物活性的出版物。

Maloney et al (2012) Discovery of 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate (ML221) as a functional antagonist of the apelin (APJ) receptor. Bioorg.Med.Chem.Lett. 22 6656 PMID: 23010269

If you know of a relevant reference for ML 221, please let us know.

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关键词: ML 221, ML 221 supplier, ML221, apelin, receptors, APJ, antagonists, Apelin, Receptors, 4748, Tocris Bioscience

3 篇 ML 221 的引用文献

引用文献是使用了 Tocris 产品的出版物。 ML 221 的部分引用包括：

Yang et al (2017) Elabela/Toddler is an endogenous agonist of the apelin APJ receptor in the adult cardiovascular system, and exogenous administration of the peptide compensates for the downregulation of its expression in pulmonary arterial hypertension. Circulation 135 1160 PMID: 28137936

Pawel et al (2021) Anti-Apoptotic Effect of Apelin in Human Placenta: Studies on BeWo Cells and Villous Explants from Third-Trimester Human Pregnancy. Int J Mol Sci 22 PMID: 33803239

Hall et al (2017) Inhibition of the apelin/apelin receptor axis decreases cholangiocarcinoma growth. Cancer Lett 386 179 PMID: 27894959

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