5.05854

TGR5 Receptor Agonist, Cpd23g

• 同義詞: 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
• 經驗公式（希爾表示法）: C₂₅H₂₅N₃O₂
• CAS號碼: 1415407-60-1
• 分子量：: 399.48
• MDL號碼: MFCD30182262
• 分類程式碼代碼: 12352200
• NACRES: NA.77

屬性

• 化驗: ≥98% (HPLC)
• 品質等級: 100
• 形狀: powder
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: white
• 溶解度: DMSO: 50 mg/mL
• 儲存溫度: 2-8°C
• SMILES 字串: N2(CCN(c5c2cccc5)C(=O)c3cnccc3Oc4c(ccc(c4)C)C)C1CC1
• InChI 密鑰: JQULIQJSYPZQMA-UHFFFAOYSA-N

描述

一般說明

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).

生化／生理作用

Primary Target
TGR5

Reversible: yes

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重構

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他說明

Duan, H., et al. 2012, J. Med. Chem.55, 10475.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全資訊

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable