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Submit ReviewL-168,049
说明： Potent, orally active human glucagon receptor antagonist
化学名： 4-[3-(5-Bromo-2-propoxyphenyl)-5-(4-chlorophenyl)-1H-pyrrol-2-yl]pyridine
纯度： ≥99% (HPLC)
生物活性 for L-168,049
L-168,049 is a very potent and selective, non-competitive antagonist of the human glucagon receptor (hGR). Binds with high affinity to human GR (IC50 = 3.7 nM), and moderate affinity to murine and canine GRs (IC50 values are 63 and 60 nM respectively). In contrast, displays poor affinity for rat, guinea pig, and rabbit glucagon receptors (IC50 > 1 μM). In functional studies, inhibits glucagon-stimulated cAMP synthesis in CHO cells expressing hGR (IC50 = 41 nM), and in murine liver membranes. Orally active in vivo.
化合物库 for L-168,049
L-168,049 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for L-168,049
| 分子量 | 467.79 |
| 公式 | C24H20BrClN2O |
| 储存 | Store at RT |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 191034-25-0 |
| PubChem ID | 5311276 |
| InChI Key | HHBOWXZOLYQFNY-UHFFFAOYSA-N |
| Smiles | CCCOC1=C(C=C(Br)C=C1)C1=C(NC(=C1)C1=CC=C(Cl)C=C1)C1=CC=NC=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.
溶解性数据 for L-168,049
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 46.78 | 100 | |
| ethanol | 46.78 | 100 |
制备储备液 for L-168,049
以下数据基于产品分子量 467.79。 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 | 2.14 mL | 10.69 mL | 21.38 mL |
| 5 mM | 0.43 mL | 2.14 mL | 4.28 mL |
| 10 mM | 0.21 mL | 1.07 mL | 2.14 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.43 mL |
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产品说明书 for L-168,049
参考文献 for L-168,049
参考文献是支持产品生物活性的出版物。
Cascieri et al (1999) Characterization of a novel, non-peptidyl antagonist of the human glucagon receptor. J.Biol.Chem. 274 8694 PMID: 10085108
de Laszlo et al (1999) Potent, orally absorbed glucagon receptor antagonists. Bioorg.Med.Chem.Lett. 9 641 PMID: 10201821
Dallas-Yang et al (2001) Detection of glucagon-dependent GTPgS binding in high-throughput format. Anal.Biochem. 301 156
If you know of a relevant reference for L-168,049, please let us know.
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关键词: L-168,049, L-168,049 supplier, Potent, orally, active, human, glucagon, receptor, antagonists, Receptors, L168049, Glucagon, Receptor, 2311, Tocris Bioscience
1 篇 L-168,049 的引用文献
引用文献是使用了 Tocris 产品的出版物。 L-168,049 的部分引用包括：
Rodriguez-Diaz et al (2018) Paracrine Interactions within the Pancreatic Islet Determine the Glycemic Set Point. Cell Metab 27 549 PMID: 29514065
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Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.