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Submit ReviewL-371,257
说明： Potent and selective oxytocin receptor antagonist
化学名： 1-[4-[(1-Acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]-4-(2-oxo-2H-3,1-benzoxazin-1(4H)-yl)piperidine
纯度： ≥99% (HPLC)
生物活性 for L-371,257
L-371,257 is a potent, high affinity human oxytocin (OT) receptor antagonist (Ki = 4.6 nM) that displays > 800-fold selectivity over human arginine vasopressin receptors V1a and V2. Antagonizes oxytocin-induced contractions in isolated rat uterine tissue (pA2 = 8.44) and in anesthetised rats following intravenous and intraduodenal administration. Decreases length of U-87MG cell projections induced by retinoic acid (Cat.No.0695). Orally active.
技术数据 for L-371,257
| 分子量 | 507.59 |
| 公式 | C28H33N3O6 |
| 储存 | Store at RT |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 162042-44-6 |
| PubChem ID | 6918320 |
| InChI Key | WDERJSQJYIJOPD-UHFFFAOYSA-N |
| Smiles | CC(N(CC3)CCC3OC(C=C2)=CC(OC)=C2C(N1CCC(N4C(OCC5=C4C=CC=C5)=O)CC1)=O)=O |
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-371,257
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 2.54 | 5 温和加热 超声处理 |
制备储备液 for L-371,257
以下数据基于产品分子量 507.59。 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 |
|---|---|---|---|
| 0.05 mM | 39.4 mL | 197.01 mL | 394.02 mL |
| 0.25 mM | 7.88 mL | 39.4 mL | 78.8 mL |
| 0.5 mM | 3.94 mL | 19.7 mL | 39.4 mL |
| 2.5 mM | 0.79 mL | 3.94 mL | 7.88 mL |
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产品说明书 for L-371,257
参考文献 for L-371,257
参考文献是支持产品生物活性的出版物。
Williams et al (1995) 1-{1-[4-[N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4-yl}-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxyt. antagonist. J.Med.Chem. 38 4634 PMID: 7473590
Tahara et al (1999) Comparison of vasopressin binding sites in human uterine and vascular smooth muscle cells. Eur.J.Pharmacol. 378 137 PMID: 10478574
Tahara et al (2000) Pharmacologic characterization of the oxyt. receptor in human uterine smooth muscle cells. Br.J.Pharmacol. 129 131 PMID: 10694212
If you know of a relevant reference for L-371,257, please let us know.
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关键词: L-371,257, L-371,257 supplier, Potent, selective, oxytocin, receptors, antagonists, OT, Receptors, L371257, Oxytocin, 2410, Tocris Bioscience
3 篇 L-371,257 的引用文献
引用文献是使用了 Tocris 产品的出版物。 L-371,257 的部分引用包括：
Li et al (2021) Oxytocin in the anterior cingulate cortex attenuates neuropathic pain and emotional anxiety by inhibiting presynaptic long-term potentiation Cell Rep 36 109411 PMID: 34289348
Lestanova et al (2017) Downregulation of oxyt. receptor decreases the length of projections stimulated by retinoic acid in the U-87MG cells. Neurochem.Res. 42 1006 PMID: 27995495
Ataka et al (2012) Alteration of antral and proximal colonic motility induced by chronic psychological stress involves central urocortin 3 and vasopressin in rats. Am J Physiol Gastrointest Liver Physiol 303 G519 PMID: 22651925
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