2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. Cipralisant maleate

Cipralisant maleate  (Synonyms: GT-2331 maleate)

目录号: HY-106993A 纯度: 99.84%
COA 产品使用指南

摩尔计算器

Cipralisant (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。

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Cipralisant maleate Chemical Structure

Cipralisant maleate Chemical Structure

CAS No. : 223420-20-0

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1 mg ￥3600
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Customer Review

Other Forms of Cipralisant maleate:

Cipralisant maleate 相关抗体

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H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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 hyperactivity disorder research[1][2][3][4]. Cipralisant (maleate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target[3][4]

H3 receptor

9.9 (pKi)

rat H3 receptor

0.47 nM (Ki)

体外研究
(In Vitro)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cipralisant maleate 相关抗体:
体内研究
(In Vivo)

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-methylhistamine-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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
分子量

332.39

Formula

C18H24N2O4
CAS 号
性状

固体

颜色

White to off-white

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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : ≥ 100 mg/mL (300.85 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 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 6.0170 mL
查看完整储备液配制表

* 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, 6 months; -20°C, 1 month。-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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

Cipralisant maleate 相关分类

完整储备液配制表

* 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, 6 months; -20°C, 1 month。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0085 mL 15.0426 mL 30.0851 mL 75.2128 mL
5 mM 0.6017 mL 3.0085 mL 6.0170 mL 15.0426 mL
10 mM 0.3009 mL 1.5043 mL 3.0085 mL 7.5213 mL
15 mM 0.2006 mL 1.0028 mL 2.0057 mL 5.0142 mL
20 mM 0.1504 mL 0.7521 mL 1.5043 mL 3.7606 mL
25 mM 0.1203 mL 0.6017 mL 1.2034 mL 3.0085 mL
30 mM 0.1003 mL 0.5014 mL 1.0028 mL 2.5071 mL
40 mM 0.0752 mL 0.3761 mL 0.7521 mL 1.8803 mL
50 mM 0.0602 mL 0.3009 mL 0.6017 mL 1.5043 mL
60 mM 0.0501 mL 0.2507 mL 0.5014 mL 1.2535 mL
80 mM 0.0376 mL 0.1880 mL 0.3761 mL 0.9402 mL
100 mM 0.0301 mL 0.1504 mL 0.3009 mL 0.7521 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Cipralisant223420-20-0GT-2331GT2331GT 2331Histamine Receptororallyactivelow-toxicitypotentselectiveaffinityattention-deficithyperactivityInhibitorinhibitorinhibit

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目录号：
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