化合物 Irdabisant hydrochloride,Irdabisant hydrochloride

化合物 Irdabisant hydrochloride|T61197|TargetMol

价格	￥10600	￥17500	￥13800
包装	25mg	100mg	50mg

最小起订量	1mg
发货地	上海
更新日期	2025-11-17

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产品详情

中文名称:化合物 Irdabisant hydrochloride	英文名称:Irdabisant hydrochloride
CAS:1005398-61-7	品牌: TargetMol
产地: 美国	保存条件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
产品类别: 抑制剂
货号: T61197

Product Introduction

Bioactivity

名称	Irdabisant hydrochloride
描述	Irdabisant hydrochloride (CEP-26401) is a selective, orally active, and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist, demonstrating high affinity with Ki values of 7.2 nM and 2.0 nM for rat and human H3R respectively. It exhibits relatively low hERG current inhibitory activity, with an IC50 of 13.8 μM. This compound has been shown to enhance cognition and promote wakefulness in rat social recognition models, suggesting potential applications in schizophrenia or cognitive impairment research.
体外活性	Irdabisant (CEP-26401, compound 8a) shows antagonist activity with K b, app values of 1.0 nM and 0.4 nM for rat H3R and human H3R, respectively; shows inverse agonist activity with EC 50 values of 2.0 nM and 1.1 nM for rat H3R and human H3R, respectively [1]. Irdabisant has moderate activity at Muscarinic M 2 (K i = 3.7 ± 0.0 μM) and Adrenergic α 1A (K i = 9.8 ± 0.3 μM) receptors, Dopamine transporters (K i = 11 ± 2 μM), Norepinephrine transporters (K i = 10 ± 1 μM), and phosphodiesterase PDE3 (IC 50 = 15 ± 1 μM) [1]. Irdabisant inhibits the cytochrome P450 enzymes CYP1A2, 2C9, 2C19, 2D6, and 3A4 with IC 50 values of greater than 30 μM, indicating less potential for drug-drug interactions [1].
体内活性	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. t 1/2 (h) 2.6 2.9 5.4 i.v. V d (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. t 1/2 (L/kg) 2.9 2.7 5.0 p.o. AUC (ng·h/mL) 984 1190 ± 180 1919 ± 611 p.o. C max (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 / 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 -induced dipsogenia (which manifests as water drinking) with an EC 50 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 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. 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 is effective at 0.3 and 1 mg/kg i.p..
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
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关键字： Irdabisant hydrochloride|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期	2013-04-18 （13年）	注册资本	589.8595万人民币
员工人数	100-500人	年营业额	￥ 1亿以上
主营行业	中间体,天然产物,生物化工,化学试剂,生物技术服务	经营模式	贸易,工厂,试剂,定制,服务

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公司成立：13年
注册资本：589.8595万人民币
企业类型：有限责任公司(自然人投资或控股)
主营产品：抑制剂&激动剂，天然产物，重组蛋白，化合物库，技术服务
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