Verucerfont (Synonyms: GSK561679)
目录号: PL04290 纯度: ≥99%
CAS No. :885220-61-1
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中文名称
Verucerfont
中文别名
3-(4-甲氧基-2-甲基苯基)-2,5-二甲基-N-[(1S)-1-(3-甲基-1,2,4-恶二唑-5-基)丙基]吡唑并[1,5-A]嘧啶-7-胺
英文名称
Verucerfont
英文别名
GSK 561679A;3-(4-methoxy-2-methylphenyl)-2,5-dimethyl-N-[(1S)-1-(3-methyl-1,2,4-oxadiazol-5-yl)propyl]pyrazolo[1,5-a]pyrimidin-7-amine
Cas No.
885220-61-1
分子式
C22H26N6O2
分子量
406.48
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Verucerfont 是促肾上腺皮质激素释放因子受体 1 (CRF1) 的拮抗剂,对于 CRF1,CRF2 和 CRF-BP 的 IC50 值分别为 6.1,>1000 和 >1000 nM。
生物活性
Verucerfont is a corticotropin-releasing factor receptor 1 (CRF1) antagonist with IC 50 s of ~6.1, >1000 and >1000?nM for CRF1, CRF2, and CRF-BP, respectively.
性状
Solid
IC50 & Target[1][2]
IC50: 6.1 nM (CRF1), >1000 nM (CRF2), >1000 nM (CRF-BP)
体内研究(In Vivo)
Post hoc analysis shows that the prototypic non-peptide CRF1 receptor antagonist NBI30775 (R121919) and Verucerfont are both significantly different from vehicle, CP-316?311, and pexacerfont (P<0.001 for all comparisons collapse across time-points); the latter three treatments in turn do not differ from each other. A differential effect of treatments over time is also shown by a significant treatment×time interaction (F[20,140]=6.4, P<0.001). Accordingly, detailed Post hoc analysis shows that both NBI30775 and Verucerfont inhibit ACTH release throughout the following 6?h of measurement (P<0.001 vs vehicle at each time-point, and vs the respective pretreatment baseline). has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Schwandt ML, et al. The CRF1 Antagonist Verucerfont in Anxious Alcohol-Dependent Women: Translation of Neuroendocrine, But not of Anti-Craving Effects. Neuropsychopharmacology. 2016 Nov;41(12):2818-2829.
溶解度数据
In Vitro: DMSO : 83.33 mg/mL (205.00 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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