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TGR5 Receptor Agonist, Cpd23g-Calbiochem

产品编号:4083621
包装规格:10 MG
产品类别:进口试剂
品牌:Sigma-Aldrich
优惠价:立即咨询
产品价格
产品编号包装单位单价(元)国内现货国外库存询价单
408362110 MG2670
产品别名

TGR5 Receptor Agonist, Cpd23g-Calbiochem

(4-cyclopropyl-3,4-dihydroquinoxalin-1(2H)-yl)(4-(2,5-dimethylphenoxy)pyridin-3-yl)methanone, Bile Acid Receptor GPBAR-1 Agonist, Bile Acid Receptor Agonist, G protein-coupled bile acid receptor 1 Agonist

基本信息
Empirical Formula【经验(实验)分子式】
C25H25N3O2
Molecular weight
399.48
General description【一般描述】
A cell-permeable, orally available, phenoxypyrimidine carboxamide derivative that acts as a highly potent and selective agonist of Protein coupled receptor TGR5 (EC50 = 720 pM and 6.2 nM for human and mouse TGR5, respectively). Does not exhibit any significant affinity towards other related targets such as GPR40, GPR119, and GPR120. Shown to increase glucagon-like peptide-1 (GLP-1) secretion in a dose-dependent manner and significantly reduce blood glucose levels in db/db mice following a single oral dose (50 mg/kg). Exhibits desirable pharmacokinetic properties in rodent models (t½ = 1.5 h, Cmax = 56 ng/ml; and AUC = 147 ng.h/ml following an oral dose of 5 mg/kg).
A cell-permeable, orally available, phenoxypyrimidine carboxamide derivative that acts as a highly potent and selective agonist of Protein coupled receptor TGR5 (EC50 = 720 pM and 6.2 nM for human and mouse TGR5, respectively). Does not exhibit any significant affinity towards other related targets such as GPR40, GPR119, and GPR120. Shown to increase glucagon-like peptide-1 (GLP-1) secretion in a dose-dependent manner and significantly reduce blood glucose levels in db/db mice following a single oral dose (50 mg/kg). Exhibits desirable pharmacokinetic properties in rodent models (t1/2 = 1.5 h, Cmax = 56 ng/ml; and AUC = 147 ng.h/ml following an oral dose of 5 mg/kg).
Biochem/physiol Actions【生化/生理作用】
Reversible: yes
Primary Target
TGR5
Warning【警告】
Toxicity: Standard Handling (A)
Reconstitution【重悬】
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes【其他说明】
Duan, H., et al. 2012, J. Med. Chem.55, 10475.
Legal Information【法律信息】
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
产品性质
Quality Level【质量水平】
100
Assay【测定】
≥98% (HPLC)
form【形式】
powder
manufacturer/tradename
Calbiochem®
storage condition【储存条件】
OK to freeze
protect from light
color【颜色】
white
solubility【溶解性】
DMSO: 50 mg/mL
storage temp.【储存温度】
2-8℃
packaging【包装】
Packaged under inert gas
安全信息
Storage Class Code【储存分类代码】
11 - Combustible Solids
WGK
WGK 3
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