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Submit ReviewAZD 3988 is a potent and selective diacylglycerol acyltransferase (DGAT-1) inhibitor (IC50 = 0.6 nM). Exhibits selectivity for DGAT-1 over DGAT-2, Kv11.1 (hERG) and cytochrome P450 enzymes. Suppresses triacylglyceride (TAG) plasma excursion and adipose tissue TAG synthesis in rats. Reduces body weight of diet-induced obese rats. Cell permeable and orally bioavailable.
Sold with the permission of AstraZeneca UK Ltd.
AZD 3988 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 456.44 |
公式 | C23H22F2N4O4 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 892489-52-0 |
PubChem ID | 23648867 |
InChI Key | NGEBYTLALFOQKI-UHFFFAOYSA-N |
Smiles | O=C(NC3=CC=[C@@]([C@H]4CC[C@H](CC(O)=O)CC4)C=C3)C1=NN=C(NC2=CC(F)=C(F)C=C2)O1 |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 45.64 | 100 | |
1eq. NaOH | 4.56 | 10 温和加热 |
以下数据基于产品分子量 456.44。 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.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.19 mL | 10.95 mL | 21.91 mL |
5 mM | 0.44 mL | 2.19 mL | 4.38 mL |
10 mM | 0.22 mL | 1.1 mL | 2.19 mL |
50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
参考文献是支持产品生物活性的出版物。
McCoull et al (2012) Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes. Bioorg.Med.Chem.Lett. 22 3873 PMID: 22608962
If you know of a relevant reference for AZD 3988, please let us know.
关键词: AZD 3988, AZD 3988 supplier, AZD3988, potent, selective, diacylglycerol, transferases, DGAT1, inhibitors, inhibits, obesity, orally, bioavailable, cell, permeable, Diacylglycerol, O-Acyltransferase, 4837, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 AZD 3988 的部分引用包括:
Mahoney et al (2019) A chemical biology screen identifies a vulnerability of neuroendocrine cancer cells to SQLE inhibition. Nat Commun 10 96 PMID: 30626880
Andris et al (2022) Oxidative stress from DGAT1 oncoprotein inhibition in melanoma suppresses tumor growth when ROS defenses are also breached. Cell Rep 39 110995 PMID: 35732120
Benedikt M et al (2019) A Novel Role for Triglyceride Metabolism in Foxp3 Expression. Front Immunol 10 1860 PMID: 31456800
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