Cipralisant maleate

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Cipralisant maleate

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

223420-20-0

GT-2331 maleate

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pK_i为 9.9，对大鼠histamine H3 receptor的K_i为 0.47 nM。Cipralisant (maleate) 有研究注意缺陷多动障碍的潜力。

生物活性

Cipralisant (GT-2331) (maleate) is an orally active, low-toxicity, potent, selective, high affinityhistamine H3 receptorfull antagonist in vivo, and an agonist in vitro, with apK_iof 9.9 forhistamine H3 receptorand aK_iof 0.47 nM for rathistamine H3 receptor. Cipralisant (maleate) has the potential for attention-deficit hyperactivity disorder research^[1]^[2]^[3]^[4].

IC₅₀& Target^[3]^[4]

H₃receptor

9.9 (pKi)

rat H₃receptor

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].

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].

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

性状

Solid

Formula

C₁₈H₂₄N₂O₄

CAS 号

223420-20-0

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

In Vitro:

DMSO : ≥ 100 mg/mL(300.85 mM)

*"≥" 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
10 mM	0.3009 mL	1.5043 mL	3.0085 mL

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。