1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  2. Histamine Receptor
  3. Irdabisant

Irdabisant  (Synonyms: CEP-26401)

目录号: HY-109968 纯度: 99.38%
COA 产品使用指南

Irdabisant (CEP-26401) 是一种具有选择性、口服活性和血脑屏障渗透性的组胺 H3 受体 (histamine H3 receptor, H3R) 拮抗剂/逆激动剂,对大鼠 H3R 和人 H3R 的 Ki 分别为 7.2 nM 和 2.0 nM。Irdabisant 对 hERG 电流的抑制活性相对较低,IC50 为 13.8 μM。Irdabisant 在大鼠社会认知模型中具有认知增强和唤醒作用。Irdabisant 可用于精神分裂症或认知障碍的研究。

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Irdabisant Chemical Structure

Irdabisant Chemical Structure

CAS No. : 1005402-19-6

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10 mM * 1 mL in DMSO ¥1930
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Other Forms of Irdabisant:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment[1][2].

IC50 & Target[1]

rat H3 receptor

7.2 nM (Ki)

human H3 receptor

2 nM (Ki)

体外研究
(In Vitro)

Irdabisant (CEP-26401, compound 8a) shows antagonist activity with Kb, app values of 1.0 nM and 0.4 nM for rat H3R and human H3R, respectively; shows inverse agonist activity with EC50 values of 2.0 nM and 1.1 nM for rat H3R and human H3R, respectively[1].
Irdabisant has moderate activity at Muscarinic M2 (Ki = 3.7 ± 0.0 μM) and Adrenergic α1A (Ki = 9.8 ± 0.3 μM) receptors, Dopamine transporters (Ki = 11 ± 2 μM), Norepinephrine transporters (Ki = 10 ± 1 μM), and phosphodiesterase PDE3 (IC50 = 15 ± 1 μM)[1].
Irdabisant inhibits the cytochrome P450 enzymes CYP1A2, 2C9, 2C19, 2D6, and 3A4 with IC50 values of greater than 30 μM, indicating less potential for drug-drug interactions[1].

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

体内研究
(In Vivo)

CEP-26401 (0.01-0.3 mg/kg; p.o.; single dosage) dose-dependently inhibits H3R agonist RAMH-induced dipsogenia[1].
CEP-26401 (0.0001-0.1 mg/kg; i.v. or p.o.; single dosage) improves performance in the rat social recognition model of short-term memory[1].
CEP-26401 (3-30 mg/kg; p.o.; single dosage) exhibits wake-promoting activity in rat[2].
CEP-26401 (3-30 mg/kg; i.p.) increases prepulse inhibition (PPI) in DBA/2NCrl mice[2].
CEP-26401 (1 mg/kg for i.v. and 3 mg/kg for p.o.; single dosage) is rapidly absorbed with high oral bioavailability in rat and monkey, and shows a moderate clearance in monkey and dog compared to the rat[1].
Pharmacokinetic Parameters of Irdabisant (compound 8a) in rats, dogs and monkeys[1].

Rat Dog Monkey
i.v. t1/2 (h) 2.6 2.9 5.4
i.v. Vd (L/kg) 9.4 3.5 ± 1.1 3.8 ± 0.9
i.v. CL (mL/min/kg) 42 13.2 ± 1.5 7.7 ± 1.8
p.o. t1/2 (L/kg) 2.9 2.7 5.0
p.o. AUC (ng·h/mL) 984 1190 ± 180 1919 ± 611
p.o. Cmax (ng/mL) 270 230 ± 70 760 ± 74
p.o. F (%) 83 22 ± 2 83 ± 18
Brain to plasma ratio 2.6 ± 0.2 2.4 ± 0.4 /

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

Animal Model: Male Sprague-Dawley rats (i.p. 10 mg/kg RAMH-induced dipsogenia model)[1]
Dosage: 0.01-0.3 mg/kg
Administration: p.o.; single dosage
Result: Dose-dependently inhibited H3R agonist RAMH (HY-100999)-induced dipsogenia (which manifests as water drinking) with an EC50 value of 0.06 mg/kg.
Animal Model: Male Sprague-Dawley rats (adult rats were briefly exposed to a juvenile rat for build social recognition model)[2]
Dosage: 0.0001, 0.001, 0.01 and 0.1 mg/kg for i.p.; 0.01 and 0.1 mg/kg for p.o.
Administration: i.v. or p.o.; single dosage
Result: Effectively reduced the ratio of investigation duration (RID) at doses over the range from 0.001 to 0.1 mg/kg i.p. and at 0.01 and 0.1 mg/kg p.o., demonstrating potent enhancement of short-term sensory memory in this model.
Animal Model: Male Sprague-Dawley rats[2]
Dosage: 3, 10 and 30 mg/kg
Administration: p.o.; single dosage
Result: Exhibited robust wake promotion with the treated animals awake 90% of the time up to 3 h postdosing at 30 mg/kg.
Animal Model: Male DBA/2NCrl mice (19-27 g; 7-9 weeks)[2]
Dosage: 3, 10 and 30 mg/kg
Administration: i.p.; single dosage
Result: Increased prepulse inhibition (PPI) in DBA/2NCrl mice, whereas the antipsychotic Risperidone (HY-11018) is effective at 0.3 and 1 mg/kg i.p..
Animal Model: Male Sprague-Dawley rats, male beagle dogs and male cynomolgus monkeys[1]
Dosage: 1 mg/kg for i.v. and 3 mg/kg for p.o.
Administration: i.v. and p.o.
Result: Exhibited rapid absorption with high oral bioavailability in rat and monkey, and showed a moderate clearance in monkey and dog compared to the rat.
Clinical Trial
分子量

313.39

Formula

C18H23N3O2

CAS 号
性状

固体

颜色

Off-white to light yellow

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 : 50 mg/mL (159.55 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1909 mL 15.9546 mL 31.9091 mL
5 mM 0.6382 mL 3.1909 mL 6.3818 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

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

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 3.1909 mL 15.9546 mL 31.9091 mL 79.7728 mL
5 mM 0.6382 mL 3.1909 mL 6.3818 mL 15.9546 mL
10 mM 0.3191 mL 1.5955 mL 3.1909 mL 7.9773 mL
15 mM 0.2127 mL 1.0636 mL 2.1273 mL 5.3182 mL
20 mM 0.1595 mL 0.7977 mL 1.5955 mL 3.9886 mL
25 mM 0.1276 mL 0.6382 mL 1.2764 mL 3.1909 mL
30 mM 0.1064 mL 0.5318 mL 1.0636 mL 2.6591 mL
40 mM 0.0798 mL 0.3989 mL 0.7977 mL 1.9943 mL
50 mM 0.0638 mL 0.3191 mL 0.6382 mL 1.5955 mL
60 mM 0.0532 mL 0.2659 mL 0.5318 mL 1.3295 mL
80 mM 0.0399 mL 0.1994 mL 0.3989 mL 0.9972 mL
100 mM 0.0319 mL 0.1595 mL 0.3191 mL 0.7977 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.

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产品名称:
Irdabisant
目录号:
HY-109968
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