| 中文名称: | Cipralisant | ||||
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| 英文名称: | Cipralisant | ||||
| 别名: | GT-2331 5-[2-(5,5-Dimethylhex-1-ynyl)cyclopropyl]-1H-imidazole | ||||
| CAS No: | 213027-19-1 | 分子式: | C14H20N2 | 分子量: | 216.32 |
| CAS No: | 213027-19-1 | ||||
| 分子式: | C14H20N2 | ||||
| 分子量: | 216.32 | ||||
基本信息
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产品编号： |
C11508 |
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产品名称： |
Cipralisant |
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CAS: |
213027-19-1 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
二年 |
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分子量： |
216.32 |
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化学名： |
5-[2-(5,5-Dimethylhex-1-ynyl)cyclopropyl]-1H-imidazole |
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Solubility (25°C)： |
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体外:
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DMSO |
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Ethanol |
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Water |
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体内(现配现用): |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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生物活性
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产品描述 |
一种有效的，选择性的组胺 H3 受体 (histamine H3 receptor) 调节剂，在体外，为组胺 H3 受体的激动剂，在体内为拮抗剂，pKi 值为 9.9，对大鼠组胺 H3 受体的 Ki 值为 0.47nM；Cipralisant 有潜力用于注意力不集中的过度反应症的研究。 |
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靶点 |
H3 receptor 9.9 (pKi) |
rat H3 receptor 0.47nM (Ki) |
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体外研究 |
Cipralisant behaves as a full agonist on adenylyl cyclase inhibition.Cipralisant (HEK cells) potently inhibits forskolin-induced cAMP accumulation, showing that Cipralisant works as a potent full histamine H3 receptor agonist.Cipralisant increases the basal [35S]GTPγS binding activities in membranes from HEK cells expressing the rat histamine H3 receptor (EC50,5.6nM). |
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体内研究 |
Cipralisant (0.3~30mg/kg;s.c.) enhances acquisition over five trials,reaching significance at 1mg/kg.Cipralisant (10mg/kg;p.o.) completely blocks R-α-methylhistamine-induced drinking.Cipralisant promotes wakefulness in the rat.Cipralisant potently and significantly improves performance in the repeated acquisition model,in line with its high affinity for the rat H3 receptor and good CNS penetration.Cipralisant does not appear to be as efficacious as 3mg/kg ciproxifan at its maximally effective dose.Cipralisant behaves as a partial agonist in a rat brain synaptosome model. |
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Animal Model: |
Male SHR pups (35–50g) |
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Dosage: |
0.3~30mg/kg |
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Administration: |
S.c. |
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Result: |
Significantly enhanced performance of the SHR pups in a dose-related manner at 1mg/kg. |
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Animal Model: |
Male Sprague-Dawley rats |
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Dosage: |
10 and 30mg/kg |
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Administration: |
P.o. |
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Result: |
Achieved greater brain exposure and water intake was monitored for 60 min after administration. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
