L-755,507
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50:13 nM(结合人β3肾上腺素受体)[1]
苯磺酰胺衍生物L-755,507是一种人β3受体的部分激动剂,最大激活是异丙肾上腺素诱发的52%[2]。β3肾上腺素受体是一种G蛋白偶联受体,可在脂肪组织中增强脂解。
体外:作为一种极其强效的人β3肾上腺素受体激动剂(β3 EC50 0.43 nM),L-755507显示优异的活性特征,选择性比β1和β2结合高440倍 [1]。在恒河猴中,通过测定其对克隆β肾上腺素受体的亲和力,L-755507也是一种强效的和选择性的β3部分激动剂,并刺激恒河猴脂肪细胞脂解,EC50 = 3.9 nM [2]。
体内:在恒河猴中,L-755,507给药引起脂肪分解和代谢率升高。对甘油血症的ED50为0.03 mg/kg,对心动过速的ED50为2.5 mg/kg,0.1 mg/kg急性单次静脉给药后刺激代谢率升高约30%[2]。
临床试验:目前尚未进行临床研究。
参考文献:
[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.
Physical Appearance | A crystalline solid |
Storage | Desiccate at RT |
M.Wt | 584.73 |
Cas No. | 159182-43-1 |
Formula | C30H40N4O6S |
Solubility | Soluble 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 |
SDF | Download SDF |
Canonical SMILES | CCCCCC/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 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |