L-755,507

β3 adrenergic receptor agonist CAS# 159182-43-1

L-755,507

Catalog No. BCC7282----Order now to get a substantial discount!

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Chemical structure

L-755,507

3D structure

Chemical Properties of L-755,507

Cas No. 159182-43-1 SDF Download SDF
PubChem ID 9829836 Appearance Powder
Formula C30H40N4O6S M.Wt 584.73
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 100 mg/mL (171.02 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 1-hexyl-3-[4-[[4-[2-[[(2S)-2-hydroxy-3-(4-hydroxyphenoxy)propyl]amino]ethyl]phenyl]sulfamoyl]phenyl]urea
SMILES CCCCCCNC(=O)NC1=CC=C(C=C1)S(=O)(=O)NC2=CC=C(C=C2)CCNCC(COC3=CC=C(C=C3)O)O
Standard InChIKey NYYJKMXNVNFOFQ-MHZLTWQESA-N
Standard InChI InChI=1S/C30H40N4O6S/c1-2-3-4-5-19-32-30(37)33-24-10-16-29(17-11-24)41(38,39)34-25-8-6-23(7-9-25)18-20-31-21-27(36)22-40-28-14-12-26(35)13-15-28/h6-17,27,31,34-36H,2-5,18-22H2,1H3,(H2,32,33,37)/t27-/m0/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of L-755,507

DescriptionPotent 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 Dilution Calculator

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Preparing Stock Solutions of L-755,507

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.7102 mL 8.551 mL 17.1019 mL 34.2038 mL 42.7548 mL
5 mM 0.342 mL 1.7102 mL 3.4204 mL 6.8408 mL 8.551 mL
10 mM 0.171 mL 0.8551 mL 1.7102 mL 3.4204 mL 4.2755 mL
50 mM 0.0342 mL 0.171 mL 0.342 mL 0.6841 mL 0.8551 mL
100 mM 0.0171 mL 0.0855 mL 0.171 mL 0.342 mL 0.4275 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on L-755,507

IC50: 13 nM (binding at the human β3 adrenergic receptor) [1]

Benzenesulfonamide derivative L-755,507 is a partial agonist for the human β3 receptor, with maximal activation 52% of that evoked by isoproterenol [2]. β3 adrenergic receptor is a G protein-coupled receptors which can enhancement of lipolysis in adipose tissue.

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].

Clinical trial: So far, no clinical study has been conducted.

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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References on L-755,507

Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist.[Pubmed:9871717]

Bioorg Med Chem Lett. 1998 May 5;8(9):1107-12.

A study of 4-acylaminobenzenesulfonamides in a cloned human beta 3 adrenergic receptor assay resulted in the discovery of n-hexylurea, L-755,507 (22). This 0.43 nM beta 3 agonist, which is > 440-fold selective over both beta 1 and beta 2 binding, is among the most potent human beta 3 agonists reported to date.

Small molecules enhance CRISPR genome editing in pluripotent stem cells.[Pubmed:25658371]

Cell Stem Cell. 2015 Feb 5;16(2):142-7.

The bacterial CRISPR-Cas9 system has emerged as an effective tool for sequence-specific gene knockout through non-homologous end joining (NHEJ), but it remains inefficient for precise editing of genome sequences. Here we develop a reporter-based screening approach for high-throughput identification of chemical compounds that can modulate precise genome editing through homology-directed repair (HDR). Using our screening method, we have identified small molecules that can enhance CRISPR-mediated HDR efficiency, 3-fold for large fragment insertions and 9-fold for point mutations. Interestingly, we have also observed that a small molecule that inhibits HDR can enhance frame shift insertion and deletion (indel) mutations mediated by NHEJ. The identified small molecules function robustly in diverse cell types with minimal toxicity. The use of small molecules provides a simple and effective strategy to enhance precise genome engineering applications and facilitates the study of DNA repair mechanisms in mammalian cells.

A selective human beta3 adrenergic receptor agonist increases metabolic rate in rhesus monkeys.[Pubmed:9616210]

J Clin Invest. 1998 Jun 1;101(11):2387-93.

Activation of beta3 adrenergic receptors on the surface of adipocytes leads to increases in intracellular cAMP and stimulation of lipolysis. In brown adipose tissue, this serves to up-regulate and activate the mitochondrial uncoupling protein 1, which mediates a proton conductance pathway that uncouples oxidative phosphorylation, leading to a net increase in energy expenditure. While chronic treatment with beta3 agonists in nonprimate species leads to uncoupling protein 1 up-regulation and weight loss, the relevance of this mechanism to energy metabolism in primates, which have much lower levels of brown adipose tissue, has been questioned. With the discovery of L-755,507, a potent and selective partial agonist for both human and rhesus beta3 receptors, we now demonstrate that acute exposure of rhesus monkeys to a beta3 agonist elicits lipolysis and metabolic rate elevation, and that chronic exposure increases uncoupling protein 1 expression in rhesus brown adipose tissue. These data suggest a role for beta3 agonists in the treatment of human obesity.

Description

L755507 is a potent, selective agonist of β3-AR with an IC50 of 35 nM.

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