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Submit ReviewL-838,417
说明： GABAA partial agonist; displays subtype selectivity
化学名： 3-(2,5-Difluorophenyl)-7-(1,1-dimethylethyl)-6-[(1-methyl-1H-1,2,4-triazol-5-yl)methoxy]-1,2,4-triazolo[4,3-b]pyridazine
纯度： ≥98% (HPLC)
生物活性 for L-838,417
L-838,417 is a subtype-selective GABAA receptor partial agonist. Selectively binds to α1, α2, α3 and α5 subunits (Ki values are 0.79, 0.67, 0.67 and 2.25 nM respectively) but displays no efficacy at α1 (α1-sparing). Exhibits non-sedative anxiolytic, antinociceptive and anti-inflammatory activity in vivo.
许可信息
Manufactured and sold under license from Merck & Co., Inc. for use solely for preclinical research purposes (ie: not for administration to or other use in humans)
化合物库 for L-838,417
L-838,417 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-838,417
| 分子量 | 399.4 |
| 公式 | C19H19F2N7O |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 286456-42-6 |
| PubChem ID | 9908880 |
| InChI Key | BQDUNOMMYOKHEP-UHFFFAOYSA-N |
| Smiles | FC(C=CC(F)=C3)=C3C1=NN=C2N1N=C(OCC4=NC=NN4C)C(C(C)(C)C)=C2 |
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-838,417
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 19.97 | 50 |
制备储备液 for L-838,417
以下数据基于产品分子量 399.4。 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 |
|---|---|---|---|
| 0.5 mM | 5.01 mL | 25.04 mL | 50.08 mL |
| 2.5 mM | 1 mL | 5.01 mL | 10.02 mL |
| 5 mM | 0.5 mL | 2.5 mL | 5.01 mL |
| 25 mM | 0.1 mL | 0.5 mL | 1 mL |
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产品说明书 for L-838,417
参考文献 for L-838,417
参考文献是支持产品生物活性的出版物。
McCabe et al (2004) Subtype-selective GABAergic drugs facilitate extinction of mouse operant behaviour. Neuropharmacology 46 171 PMID: 14680756
McMahon and France (2006) Differential behavioural effects of low efficacy positive GABAA modulators in combination with benzodiazepines and a neuroactive steroid in rhesus monkeys. Br.J.Pharmacol. 147 260 PMID: 16331290
Knabl et al (2008) Reversal of pathological pain through specific spinal GABAA receptor subtypes. Nature 451 330 PMID: 18202657
Soderhielm et al (2018) Probing the molecular basis for affinity/potency- and efficacy-based subtype-selectivity exhibited by benzodiazepine-site modulators at GABAA receptors. Biochem.Pharmacol. 158 339 PMID: 30121248
If you know of a relevant reference for L-838,417, please let us know.
按产品操作查看相关产品
关键词: L-838,417, L-838,417 supplier, Subtype-selective, GABAA, partial, agonists, Receptors, L838417, merck, 3250, Tocris Bioscience
3 篇 L-838,417 的引用文献
引用文献是使用了 Tocris 产品的出版物。 L-838,417 的部分引用包括：
Gee et al (2010) Limiting activity at beta1-subunit-containing GABAA receptor subtypes reduces ataxia. J Pharmacol Exp Ther 332 1040 PMID: 19940102
De la Luz-Cuellar et al (2019) Blockade of spinal α5-GABAA receptors differentially reduces reserpine-induced fibromyalgia-type pain in female rats. Eur J Pharmacol 858 172443 PMID: 31181208
Soderhielm et al (2018) Probing the molecular basis for affinity/potency- and efficacy-based subtype-selectivity exhibited by benzodiazepine-site modulators at GABAA receptors. Biochem Pharmacol 158 339 PMID: 30121248
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