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Biological Activity for L-755,507
L-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).
Compound Libraries for L-755,507
Technical Data for L-755,507
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for L-755,507
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for L-755,507
The following data is based on the product molecular weight 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.
|Concentration / Solvent Volume / Mass||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|
References for L-755,507
References are publications that support the biological activity of the product.
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.
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6 Citations for L-755,507
Citations are publications that use Tocris products. Selected citations for L-755,507 include:
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
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
Coan and Shoichet (2008) Stoichiometry and physical chemistry of promiscuous aggregate-based inhibitors. J Am Chem Soc 130 9606 PMID: 18588298
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
Do you know of a great paper that uses L-755,507 from Tocris? Please let us know.
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Literature in this Area
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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.