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| 4-[[(HEXYLAMINO)CARBONYL]AMINO]-N-[4-[2-[[(2S)-2-HYDROXY-3-(4-HYDROXYPHENOXY)PROPYL]AMINO]ETHYL]PHENYL]-BENZENESULFONAMIDE Basic information |
| 4-[[(HEXYLAMINO)CARBONYL]AMINO]-N-[4-[2-[[(2S)-2-HYDROXY-3-(4-HYDROXYPHENOXY)PROPYL]AMINO]ETHYL]PHENYL]-BENZENESULFONAMIDE Chemical Properties |
| density | 1.274±0.06 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | Soluble in DMSO | | form | powder | | pka | 8.85±0.10(Predicted) | | color | white to beige |
| 4-[[(HEXYLAMINO)CARBONYL]AMINO]-N-[4-[2-[[(2S)-2-HYDROXY-3-(4-HYDROXYPHENOXY)PROPYL]AMINO]ETHYL]PHENYL]-BENZENESULFONAMIDE Usage And Synthesis |
| Uses | L755507 is a novel, potent, and selective β3 adrenergic receptor (β3-AR) that can enhance CRISPR genome editing in pluripotent stem cells. It may also serve as a potential therapeutic target for the treatment of type II diabetes and obesity. | | Uses | L755507 has been shown to enhance CRISPR genome editing efficiency. To see other small molecule CRISPR enhancers, visit sigma.com/CRISPR-enhancers. | | General Description | L755507 is a derivative of 4-acylaminobenzenesulfonamide. | | Biological Activity | Subnanomolar potent β 3 -adrenergic receptor partial agonist that is > 1000-fold selective over β 1 - and β 2 -adrenoceptors (EC 50 values are 0.43, 580 and > 10000 nM for activation of cloned human β 3 -, β 1 - and β 2 -adrenoceptors respectively). In vitro, stimulates lipolysis in rhesus adipocytes with an EC 50 of 3.9 nM. | | Biochem/physiol Actions | L755507 is a potent β3-adrenergic receptor partial agonist with an EC50 value of 0.43 nM for β3 receptors with over 440-fold selectivity for β3 compared to β1 and β2-adrenergic receptor binding. L755507 has been shown to enhance CRISPR-mediated homology-directed repair (HDR) efficiency in human induced pluripotent stem cells (iPSCs), increasing the efficiency of GFP insertion by 3-fold compared to control cells. | | in vitro | l-755,507 displays an excellent activity profile as an extremely potent human β3 adrenergic receptor agonist (β3 ec50 0.43 nm), with >440-fold selectivity over β1 and β2 binding [1]. l-755,507 is also a potent and selective b3 partial agonist in rhesus monkeys as assessed by its affinity for the cloned b adrenergic receptors, and stimulates lipolysis in rhesus adipocytes with an ec50 = 3.9 nm [2]. | | in vivo | dose rhesus monkeys with l-755,507 elicits lipolysis and metabolic rate elevation. the ed50 for glycerolemia was 0.03 mg/kg and the ed50 for tachycardia was 2.5 mg/kg, and stimulates metabolic rate by ~ 30% after acute bolus intravenous administration of 0.1 mg/kg [2]. | | IC 50 | 13 nm (binding at the human β3 adrenergic receptor) [1] | | references | [1] parmee er, ok ho, candelore mr, tota l, deng l, strader cd, wyvratt mj, fisher mh, weber ae. discovery of l-755,507: a subnanomolar human beta 3 adrenergic receptor agonist. bioorg med chem lett. 1998 may 5;8(9):1107-12.[2] fisher mh, amend am, bach tj, barker jm, brady ej, candelore mr, carroll d, cascieri ma, chiu sh, deng l, forrest mj, hegarty-friscino b, guan xm, hom gj, hutchins je, kelly lj, mathvink rj, metzger jm, miller rr, ok ho, parmee er, saperstein r, strader cd, stearns ra, macintyre de, et al. a selective human beta3 adrenergic receptor agonist increases metabolic rate in rhesus monkeys. j clin invest. 1998 jun 1;101(11):2387-93. |
| 4-[[(HEXYLAMINO)CARBONYL]AMINO]-N-[4-[2-[[(2S)-2-HYDROXY-3-(4-HYDROXYPHENOXY)PROPYL]AMINO]ETHYL]PHENYL]-BENZENESULFONAMIDE Preparation Products And Raw materials |
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![4-[[(HEXYLAMINO)CARBONYL]AMINO]-N-[4-[2-[[(2S)-2-HYDROXY-3-(4-HYDROXYPHENOXY)PROPYL]AMINO]ETHYL]PHENYL]-BENZENESULFONAMIDE](/img/159182-43-1.jpg "4-[[(HEXYLAMINO)CARBONYL]AMINO]-N-[4-[2-[[(2S)-2-HYDROXY-3-(4-HYDROXYPHENOXY)PROPYL]AMINO]ETHYL]PHENYL]-BENZENESULFONAMIDE")
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