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Submit ReviewTC-G 1005 is a potent and selective GPBA agonist (EC50 values are 0.72 nM and 6.2 nM for hTGR5 and mTGR5, respectively). TC-G 1005 is selective for TGR5 over FXR (farnesoid X receptor). TC-G 1005 increases plasma GLP-1 levels and reduces blood glucose in mice. Orally bioavailable.
TC-G 1005 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 399.48 |
公式 | C25H25N3O2 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1415407-60-1 |
PubChem ID | 71450251 |
InChI Key | JQULIQJSYPZQMA-UHFFFAOYSA-N |
Smiles | CC1=CC(OC2=CC=NC=C2C(N3C(C=CC=C4)=C4N(C5CC5)CC3)=O)=C(C)C=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 39.95 | 100 | |
ethanol | 39.95 | 100 |
以下数据基于产品分子量 399.48。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.5 mL | 12.52 mL | 25.03 mL |
5 mM | 0.5 mL | 2.5 mL | 5.01 mL |
10 mM | 0.25 mL | 1.25 mL | 2.5 mL |
50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
参考文献是支持产品生物活性的出版物。
Duan et al (2012) Design, synthesis, and antidiabetic activity of 4-phenoxynicotinamide and 4-phenoxypyrimidine-5-carboxamide derivatives as potent and orally efficacious TGR5 agonists. J.Med.Chem. 55 10475 PMID: 23148522
Urso et al (2020) Bile acids inhibit cholinergic constriction in proximal and peripheral airways from humans and rodents. Am.J.Physiol.Lung Cell.Mol.Physiol. 318 L264 PMID: 31800261
If you know of a relevant reference for TC-G 1005, please let us know.
关键词: TC-G 1005, TC-G 1005 supplier, TC-G1005, TGR5, agonists, agonism, GLP-1, GPBA, glucose, bile, acid, receptors, bioavailable, TCG1005, Receptors, 5129, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 TC-G 1005 的部分引用包括:
Urso et al (2020) Bile acids inhibit cholinergic constriction in proximal and peripheral airways from humans and rodents. Am.J.Physiol.Lung Cell.Mol.Physiol. 318 L264 PMID: 31800261
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