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Submit ReviewL-817,818 is a potent and selective somatostatin sst5 receptor agonist. Ki values are 0.4, 3.3, 52, 64 and 82 nM for cloned human sst5, sst1, sst2, sst3 and sst4 receptors respectively. Inhibits growth hormone release from rat pituitary cells (EC50 = 3.1 nM) and insulin release from mouse pancreatic islets (EC50 = 0.3 nM) in vitro.
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分子量 | 536.67 |
公式 | C33H36N4O3 |
储存 | Store at -20°C |
纯度 | ≥99% (HPLC) |
CAS Number | 217480-27-8 |
PubChem ID | 9937014 |
InChI Key | NFVRGDRCCNEGBS-KCWXNJEJSA-N |
Smiles | O=C(CC1=C(C4=CC=C(C=CC=C5)C5=C4)NC2=C1C=CC3=C2C=CC=C3)N[C@@H]([C@](OC[C@@H](N)C)=O)CCCCN |
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 | 53.67 | 100 |
以下数据基于产品分子量 536.67。 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 | 1.86 mL | 9.32 mL | 18.63 mL |
5 mM | 0.37 mL | 1.86 mL | 3.73 mL |
10 mM | 0.19 mL | 0.93 mL | 1.86 mL |
50 mM | 0.04 mL | 0.19 mL | 0.37 mL |
参考文献是支持产品生物活性的出版物。
Rohrer et al (1998) Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry. Science 282 737 PMID: 9784130
Rohrer and Schaeffer (2000) Identification and characterization of subtype selective somatostatin receptor agonists. J.Physiol.Paris 94 211 PMID: 11087999
Strowski et al (2000) Somatostatin inhibits Ins and glucagon secretion via two receptor subtypes: An in vitro study of pancreatic islets from somatostatin receptor 2 knockout mice. Endocrinology 141 111 PMID: 10614629
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关键词: L-817,818, L-817,818 supplier, Potent, selective, sst5, agonists, Receptors, Somatostatin, L817818, 1980, Tocris Bioscience
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