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

Irdabisant  (Synonyms: CEP-26401)

目錄號: HY-109968 純度: 99.38%
COA 產(chǎn)品使用指南 技術(shù)支持

Irdabisant (CEP-26401) 是一種具有選擇性、口服活性和血腦屏障滲透性的組胺 H3 受體 (histamine H3 receptor, H3R) 拮抗劑/逆激動劑，對大鼠 H3R 和人 H3R 的 Ki 分別為 7.2 nM 和 2.0 nM。Irdabisant 對 hERG 電流的抑制活性相對較低，IC50 為 13.8 μM。Irdabisant 在大鼠社會認(rèn)知模型中具有認(rèn)知增強(qiáng)和喚醒作用。Irdabisant 可用于精神分裂癥或認(rèn)知障礙的研究。

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Irdabisant Chemical Structure

Irdabisant Chemical Structure

CAS No. : 1005402-19-6

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1198
In-stock
1 mg ￥684
In-stock
5 mg ￥1738
In-stock
10 mg ￥2475
In-stock
25 mg ￥4436
In-stock
50 mg ￥5988
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100 mg 現(xiàn)貨 詢價
200 mg   詢價  
500 mg   詢價  

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Customer Review

Other Forms of Irdabisant:

查看 Histamine Receptor 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
13.8 μM
Compound: 8a, CEP-26401, irdabisant
Inhibition of recombinant human ERG channel expressed in human HEK 293 cells by patch clamp assay
Inhibition of recombinant human ERG channel expressed in human HEK 293 cells by patch clamp assay
[PMID: 21634396]
體外研究
(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.
體內(nèi)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 號
性狀

固體

顏色

Off-white to light yellow

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實驗： 

DMSO 中的溶解度 : 50 mg/mL (159.55 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)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
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻(xiàn)

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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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產(chǎn)品名稱：
Irdabisant
目錄號：
HY-109968
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