| Identification | Back Directory | [Name]
4-[[(HEXYLAMINO)CARBONYL]AMINO]-N-[4-[2-[[(2S)-2-HYDROXY-3-(4-HYDROXYPHENOXY)PROPYL]AMINO]ETHYL]PHENYL]-BENZENESULFONAMIDE | [CAS]
159182-43-1 | [Synonyms]
507
L755
L 755
CS-2258
L-755,507
L755;507;L-755507;L 755;507
(S)-4-(3-Hexylureido)-N-(4-(2-((2-hydroxy-3-(4-hydroxyphenoxy)propyl)amino)ethyl)phenyl)benzenesulfonamide
4-[[(HEXYLAMINO)CARBONYL]AMINO]-N-[4-[2-[[(2S)-2-HYDROXY-3-(4-HYDROXYPHENOXY)PROPYL]AMINO]ETHYL]PHENYL]-BENZENESULFONAMIDE
Benzenesulfonamide, 4-[[(hexylamino)carbonyl]amino]-N-[4-[2-[[(2S)-2-hydroxy-3-(4-hydroxyphenoxy)propyl]amino]ethyl]phenyl]- | [Molecular Formula]
C30H40N4O6S | [MDL Number]
MFCD08703099 | [MOL File]
159182-43-1.mol | [Molecular Weight]
584.73 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [Uses]
L755507 has been shown to enhance CRISPR genome editing efficiency. To see other small molecule CRISPR enhancers, visit sigma.com/CRISPR-enhancers. | [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. | [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] | [storage]
Store at +4°C | [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. |
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