化合物 Irdabisant hydrochloride,Irdabisant hydrochloride

化合物 Irdabisant hydrochloride|T61197|TargetMol

價(jià)格	￥10600	￥17500	￥13800
包裝	25mg	100mg	50mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-02

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產(chǎn)品詳情

中文名稱:化合物 Irdabisant hydrochloride	英文名稱:Irdabisant hydrochloride
CAS:1005398-61-7	品牌: TargetMol
產(chǎn)地: 美國(guó)	保存條件: Shipping with blue ice.
產(chǎn)品類別: 抑制劑
貨號(hào): T61197

Product Introduction

Bioactivity

Name	Irdabisant hydrochloride
Description	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.
In vitro	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].
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. 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..
Storage	Shipping with blue ice.

關(guān)鍵字： Irdabisant hydrochloride|TargetMol

公司簡(jiǎn)介

TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓，致力于為全球生化領(lǐng)域科學(xué)家的研究提供專業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶群分布于40多個(gè)國(guó)家和地區(qū)，已發(fā)展成為全球知名的化合物庫(kù)和小分子化合物研究供應(yīng)商。 TargetMol?可提供160多種滿足不同需求的化合物庫(kù)，以及多種類型的生化試劑產(chǎn)品，包括12000多種抑制劑、16000多種天然產(chǎn)物和各類多肽、抗體、生命科學(xué)試劑盒等，此外，我們還建設(shè)有CADD（計(jì)算機(jī)輔助藥物設(shè)計(jì)）研究中心、藥理實(shí)驗(yàn)室、藥化合成平臺(tái)三大技術(shù)中心，全方位滿足客戶的定制需求。憑借我們優(yōu)質(zhì)的產(chǎn)品和服務(wù)、快速高效的全球供應(yīng)鏈和專業(yè)的技術(shù)支持，我們將有效幫助您縮短研發(fā)周期，取得更成功的結(jié)果。

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