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Submit ReviewL-755,507 is a potent β3-adrenergic receptor partial agonist > 1000-fold selective over β1- and β2-adrenoceptors (EC50 values are 0.43, 580 and > 10000 nM for activation of cloned human β3-, β1- and β2-adrenoceptors respectively). Stimulates lipolysis in rhesus adipocytes in vitro (EC50 = 3.9 nM). Enhances CRISPR-mediated homology-directed repair (HDR) efficiency 2-3-fold for large fragments and ~9-fold for point mutations, in human induced pluripotent stem cells (iPSCs).
L-755,507 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 | 584.73 |
公式 | C30H40N4O6S |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 159182-43-1 |
PubChem ID | 9829836 |
InChI Key | NYYJKMXNVNFOFQ-MHZLTWQESA-N |
Smiles | O=S(C1=CC=C(NC(NCCCCCC)=O)C=C1)(NC2=CC=C(CCNC[C@H](O)COC3=CC=C(O)C=C3)C=C2)=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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 58.47 | 100 | |
ethanol | 58.47 | 100 |
以下数据基于产品分子量 584.73。 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 | 1.71 mL | 8.55 mL | 17.1 mL |
5 mM | 0.34 mL | 1.71 mL | 3.42 mL |
10 mM | 0.17 mL | 0.86 mL | 1.71 mL |
50 mM | 0.03 mL | 0.17 mL | 0.34 mL |
参考文献是支持产品生物活性的出版物。
Parmee et al (1998) Discovery of L-755,507: a subnanomolar human β3 adrenergic receptor agonist. Bioorg.Med.Chem.Lett. 8 1107 PMID: 9871717
Fisher et al (1998) A selective human β3 adrenergic receptor agonist increases metabolic rate in rhesus monkeys. J.Clin.Invest. 101 2387 PMID: 9616210
Yu et al (2015) Small molecules enhance CRISPR genome editing in pluripotent stem cells. Cell Stem Cell 16 142 PMID: 25658371
If you know of a relevant reference for L-755,507, please let us know.
关键词: L-755,507, L-755,507 supplier, potent, selective, β3, beta3, partial, agonists, adrenergic, receptors, adrenoceptors, L755507, CRISPR, Cas9, HDR, NHEJ, homology, directed, repair, nonhomologous, end, joining, hematopoietic, haematopoietic, stem, cells, HSC, Adrenergic, Beta-3, Receptors, Reagents, Hematopoietic, Stem, Cells, 2197, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 L-755,507 的部分引用包括:
Riesenberg and Maricic (2018) Targeting repair pathways with small molecules increases precise genome editing in pluripotent stem cells. Nat Commun 9 2164 PMID: 29867139
Kornete et al (2018) Highly Efficient and Versatile Plasmid-Based Gene Editing in Primary T Cells. J Immunol 200 2489 PMID: 29445007
Pinder et al (2015) Nuclear domain 'knock-in' screen for the evaluation and identification of small molecule enhancers of CRISPR-based genome editing. Nucleic Acids Res 43 9379 PMID: 26429972
Afeli et al (2012) Do β3-adrenergic receptors play a role in guinea pig detrusor smooth muscle excitability and contractility?. Am J Physiol Renal Physiol 302 F251 PMID: 21993887
Coan et al (2009) Promiscuous aggregate-based inhibitors promote enzyme unfolding. J Med Chem 52 2067 PMID: 19281222
Coan and Shoichet (2008) Stoichiometry and physical chemistry of promiscuous aggregate-based inhibitors. J Am Chem Soc 130 9606 PMID: 18588298
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.