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L-755,507

现货
Catalog No.
B6970
β3肾上腺素能受体激动剂
组合的产品项目
规格价格库存 数量
10mg
¥ 1,800.00
Ship with 10-15 days
50mg
¥ 6,340.00
Ship with 10-15 days

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Background

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.

Chemical Properties

Physical AppearanceA crystalline solid
StorageDesiccate at RT
M.Wt584.73
Cas No.159182-43-1
FormulaC30H40N4O6S
SolubilitySoluble in DMSO
Chemical Name(S,Z)-N'-hexyl-N-(4-(N-(4-(2-((2-hydroxy-3-(4-hydroxyphenoxy)propyl)amino)ethyl)phenyl)sulfamoyl)phenyl)carbamimidic acid
SDFDownload SDF
Canonical SMILESCCCCCC/N=C(O)/NC1=CC=C(S(NC2=CC=C(CCNC[C@@](O)([H])COC3=CC=C(O)C=C3)C=C2)(=O)=O)C=C1
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

质量控制

质量控制和MSDS

批次:

化学结构

L-755,507