5.05854
TGR5 Receptor Agonist, Cpd23g
동의어(들):
TGR5 Receptor Agonist, Cpd23g, (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
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크기 선택
제품정보 (DICE 배송 시 비용 별도)
실험식(Hill 표기법):
C25H25N3O2
CAS 번호:
Molecular Weight:
399.48
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
Storage condition:
OK to freeze, protect from light
InChI key
JQULIQJSYPZQMA-UHFFFAOYSA-N
SMILES string
N2(CCN(c5c2cccc5)C(=O)c3cnccc3Oc4c(ccc(c4)C)C)C1CC1
assay
≥98% (HPLC)
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
DMSO: 50 mg/mL
storage temp.
2-8°C
Quality Level
General description
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).
Biochem/physiol Actions
Primary Target
TGR5
TGR5
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Duan, H., et al. 2012, J. Med. Chem.55, 10475.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
저장 등급
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
시험 성적서(COA)
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