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Submit ReviewL-368,899 hydrochloride is a potent, non-peptide and orally active oxytocin receptor antagonist (IC50 = 8.9 nM) that displays > 40-fold selectivity over vasopressin V1a and V2 receptors (IC50 values are 370 and 570 nM respectively). Antagonizes oxytocin-induced uterine contractions in vitro and in vivo.
L-368,899 hydrochloride 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 | 627.68 |
公式 | C26H42N4O5S2.2HCl |
储存 | Store at -20°C |
纯度 | ≥97% (HPLC) |
PubChem ID | 90488775 |
InChI Key | WJPIJZWOCNBGTR-HILSUTFGSA-N |
Smiles | CC(C=CC=C1)=C1N2CCN(S(C[C@@]34CC[C@@H](C4(C)C)C[C@@H]3NC([C@@H](N)CCS(C)(=O)=O)=O)(=O)=O)CC2.Cl.Cl |
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 | |||
water | 59.12 | 100 | |
DMSO | 59.12 | 100 |
以下数据基于产品分子量 627.68。 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 | 1.59 mL | 7.97 mL | 15.93 mL |
5 mM | 0.32 mL | 1.59 mL | 3.19 mL |
10 mM | 0.16 mL | 0.8 mL | 1.59 mL |
50 mM | 0.03 mL | 0.16 mL | 0.32 mL |
参考文献是支持产品生物活性的出版物。
Williams et al (1994) 1-(((7,7-dimethyl-2(S)-(2(S)-amino-4-(methylsulfonyl)butyramido)bicyclo[2.2.1]-heptan-1(S)-yl)methyl)sulfonyl)-4-(2-methylphenyl)piperazine (L-368,899): an orally bioavailable, non-peptide oxyt. antagonist with potential util J.Med.Chem. 37 565 PMID: 8126695
Mann et al (2003) Attenuation of PGE2α release in ewes infused with the oxyt. antagonist L-368,899. Domest.Anim.Endocrinol. 25 255 PMID: 14550509
Quattropani et al (2005) Discovery and development of a new class of potent, selective, orally active oxyt. receptor antagonist. J.Med.Chem. 48 7882 PMID: 16302826
Borthwick (2010) Oral oxyt. antagonists. J.Med.Chem. 53 6525 PMID: 20550119
If you know of a relevant reference for L-368,899 hydrochloride, please let us know.
关键词: L-368,899 hydrochloride, L-368,899 hydrochloride supplier, Potent, non-peptide, oxytocin, receptor, antagonists, OT, Receptors, L368899, 160312-62-9, Oxytocin, 2641, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 L-368,899 hydrochloride 的部分引用包括:
Xiao et al (2017) Biased OXTergic Modulation of Midbrain DA Systems. Neuron 95 368 PMID: 28669546
Gaetani et al (2010) The fat-induced satiety factor oleoylethanolamide suppresses feeding through central release of oxyt. Nat Commun 30 8096 PMID: 20554860
Pont et al (2012) Oxytocin-stimulated NFAT transcriptional activation in human myometrial cells. Mol.Endocrinol. 26 1743 PMID: 22902539
Xiao et al (2018) OXT functions as a spatiotemporal filter for excitatory synaptic inputs to VTA DA neurons. Elife 7 PMID: 29676731
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We performed ex-vivo slice physiology, and bath applied L-368,899 hydrochloride.