Cipralisant maleate
(Synonyms: GT-2331 maleate) 目录号 : GC68869Cipralisant (GT-2331) (maleate) 在体内是一种具有口服活性、低毒、有效、选择性、高亲和力的 histamine H3 receptor 的拮抗剂，在体外是 histamine H3 receptor 的激动剂，对于 histamine H3 receptor，其 pKi 为 9.9，对大鼠 histamine H3 receptor 的Ki为 0.47 nM。Cipralisant (maleate) 有研究注意缺陷多动障碍的潜力。
Cas No.:223420-20-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cipralisant (GT-2331) (maleate) is an orally active, low-toxicity, potent, selective, high affinity histamine H3 receptor full antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor. Cipralisant (maleate) has the potential for attention-deficit peractivity disorder research[1][2][3][4].
Cipralisant (maleate) behaves as a full agonist on adenylyl cyclase inhibition. Cipralisant (maleate) (HEK cells) potently inhibits forskolin-induced cAMP accumulation, showing that Cipralisant (maleate) works as a potent full histamine H3 receptor agonist. Cipralisant (maleate) increases the basal [35S]GTPγS binding activities in membranes from HEK cells expressing the rat histamine H3 receptor (EC50, 5.6 nM)[3].
Cipralisant (maleate) (0.3~30 mg/kg; s.c.) enhances acquisition over five trials, reaching significance at 1 mg/kg[2].
Cipralisant (maleate) (10 mg/kg; p.o.) completely blocks R-α-metlhistamine-induced drinking[3].
Cipralisant (maleate) promotes wakefulness in the rat. Cipralisant (maleate) 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 (maleate) does not appear to be as efficacious as 3 mg/kg ciproxifan at its maximally effective dose [2]. Cipralisant (maleate) behaves as a partial agonist in a rat brain synaptosome model[3].
| Animal Model: | Male SHR pups (35-50 g)[2] |
| Dosage: | 0.3~30 mg/kg |
| Administration: | S.c. |
| Result: | Significantly enhanced performance of the SHR pups in a dose-related manner at 1 mg/kg. |
| Animal Model: | Male Sprague-Dawley rats[3] |
| Dosage: | 10 and 30 mg/kg |
| Administration: | P.o. |
| Result: | Achieved greater brain exposure and water intake was monitored for 60 min after administration. |
[1]. Raddatz R, et al. Histamine H3 antagonists for treatment of cognitive deficits in CNS diseases. Curr Top Med Chem. 2010;10(2):153-169.
[2]. Fox GB, et al. Effects of histamine H(3) receptor ligands GT-2331 and ciproxifan in a repeated acquisition avoidance response in the spontaneously pertensive rat pup. Behav Brain Res. 2002;131(1-2):151-161.
[3]. Ito S, et al. Detailed pharmacological characterization of GT-2331 for the rat histamine H3 receptor. Eur J Pharmacol. 2006;529(1-3):40-46.
[4]. Tedford CE, et al. High antagonist potency of GT-2227 and GT-2331, new histamine H3 receptor antagonists, in two functional models. Eur J Pharmacol. 1998;351(3):307-311.
| Cas No. | 223420-20-0 | SDF | Download SDF |
| 别名 | GT-2331 maleate | ||
| 分子式 | C18H24N2O4 | 分子量 | 332.39 |
| 溶解度 | DMSO : ≥ 100 mg/mL (300.85 mM) | 储存条件 | Store at -20°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.0085 mL | 15.0426 mL | 30.0851 mL |
| 5 mM | 0.6017 mL | 3.0085 mL | 6.017 mL |
| 10 mM | 0.3009 mL | 1.5043 mL | 3.0085 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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