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L755507
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
L755507图片
CAS NO:159182-43-1
规格:≥98%

理化性质和储存条件
Molecular Weight (MW)584.73
FormulaC30H40N4O6S
CAS No.159182-43-1
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 100 mg/mL (171.0 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Other info

Chemical Name: 1-hexyl-3-[4-[[4-[2-[[(2S)-2-hydroxy-3-(4-hydroxyphenoxy)propyl]amino]ethyl]phenyl]sulfamoyl]phenyl]urea

InChi Key: NYYJKMXNVNFOFQ-MHZLTWQESA-N

InChi Code: 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

SMILES Code: O=C(NC1=CC=C(S(=O)(NC2=CC=C(CCNC[C@H](O)COC3=CC=C(O)C=C3)C=C2)=O)C=C1)NCCCCCC

Synonyms

L-755507; L 755507; L755507

实验参考方法
In Vitro

In vitro activity: 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. L755507 causes a robust concentration-dependent increase in cAMP accumulation in CHO-K1 cells expressing human β3-adrenoceptors(pEC50 values of 12.3). In a recent study employing a high-throughput screen to identify chemicals capable of modulating HR-mediated genome editing, L-755507 is identified that could enhance HR repair by up to ninefold.


Kinase Assay: L-755,507 is characterized as a potent and selective β3 adrenergic receptor partial agonist with EC50 of 0.43 nM. It is also recently identified to enhance CRISPR-mediated homology-directed repair (HDR) efficiency in human induced pluripotent stem cells (iPSCs) and other cell types.

In VivoAcute exposure of rhesus monkeys to L-755,507 elicits lipolysis and metabolic rate elevation, and that chronic exposure increases uncoupling protein 1 expression in rhesus brown adipose tissue.
Animal modelMale lean rhesus monkeys
Formulation & DosageFormulated in 25% ethanol, 25%polyethylene glycol 400, 50% saline; 3 mg/kg; i.v. injection
References

Bioorg Med Chem Lett. 1998 May 5;8(9):1107-12; J Clin Invest. 1998 Jun 1;101(11):2387-93; Cell Stem Cell. 2015 Feb 5;16(2):142-7.

 
 
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