JNJ-37822681 dihydrochloride

目录号: PL09172 纯度: ≥99%
JNJ-37822681 dihydrochloride 是一种高效、特异性、有中枢活性的,能快速解离的多巴胺 D2 受体拮抗剂,对多巴胺 D2L 受体的亲和力适中 (Ki =158 nM),具有研究精神分裂症和躁郁症的潜力。
CAS No. :2108806-02-4
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中文名称
JNJ-37822681 dihydrochloride
英文名称
JNJ-37822681 dihydrochloride
英文别名
Y3XCP46PA8;N-{1-[(3,4-difluorophenyl)methyl]piperidin-4-yl}-6-(trifluoromethyl)pyridazin-3-amine dihydrochloride;JNJ 37822681 dihydrochloride;N-(1-(3,4-difluorobenzyl)piperidin-4-yl)-6-(trifluoromethyl)pyridazin-3-amine;3-Pyridazinamine, N-(1-((3,4-difluorophenyl)methyl)-4-piperidinyl)-6-(trifluoromethyl)-, hydrochloride (1:2);Unii-Y3xcp46PA8;JNJ-37822681 dihydrochloride
Cas No.
2108806-02-4
分子式
C17H19Cl2F5N4
分子量
445.26
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
详情描述
JNJ-37822681 dihydrochloride 是一种高效、特异性、有中枢活性的,能快速解离的多巴胺 D2 受体拮抗剂,对多巴胺 D2L 受体的亲和力适中 (Ki =158 nM),具有研究精神分裂症和躁郁症的潜力。
产品详情
JNJ-37822681 dihydrochloride 是一种高效、特异性、有中枢活性的,能快速解离的多巴胺 D2 受体拮抗剂,对多巴胺 D2L 受体的亲和力适中 (Ki =158 nM),具有研究精神分裂症和躁郁症的潜力。
生物活性
JNJ-37822681 dihydrochloride is a potent, specific, centrally active, fast-dissociating dopamine D 2 receptor antagonist with a moderate binding affinity for the dopamine D 2L receptor (K i =158 nM), which has potential for the treatment of schizophrenia and bipolar disorder.
性状
Solid
IC50 & Target[1][2]
Ki: 158 nM (D2)
体内研究(In Vivo)
JNJ-37822681 (0.0025-40 mg/kg; i.h.; once) blocks D 2 receptors in rat brain at relatively low doses with an ED 50 value of 0.39 mg/kg and has effective in animal models of psychosis.
JNJ-37822681 (0.01-2.5 mg/kg; i.h.; once) induces minimal prolactin release at the lowest doses required for central D 2 receptor blockade. 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
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
ClinicalTrial
参考文献
[1]. Langlois X, et, al. Pharmacology of JNJ-37822681, a specific and fast-dissociating D2 antagonist for the treatment of schizophrenia. J Pharmacol Exp Ther. 2012 Jul;342(1):91-105.
[2]. de Waal EJ, et, al. Differential responses to JNJ-37822681, a specific and fast dissociating dopamine D2 receptor antagonist, in cynomolgus monkey and Sprague-Dawley rat general toxicology studies: clinical observations, prolactin levels, mammary histopat
溶解度数据
In Vitro: DMSO : 33.33 mg/mL (74.86 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)
[1]. Langlois X, et, al. Pharmacology of JNJ-37822681, a specific and fast-dissociating D2 antagonist for the treatment of schizophrenia. J Pharmacol Exp Ther. 2012 Jul;342(1):91-105.
[2]. de Waal EJ, et, al. Differential responses to JNJ-37822681, a specific and fast dissociating dopamine D2 receptor antagonist, in cynomolgus monkey and Sprague-Dawley rat general toxicology studies: clinical observations, prolactin levels, mammary histopat

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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