Irdabisant
Based on 1 Customer Validation
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.
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- Pureza: 99.58%
- No. CAS: 1005402-19-6
- Fòrmula: C18H23N3O2
- Peso molecular:313.39
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
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Ver todos los productos específicos de isoformas Histamine Receptor
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Actividad biológica
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rat H3 receptor 7.2 nM (Ki) |
human H3 receptor 2 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
13.8 μM
Compound: 8a, CEP-26401, irdabisant
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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
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[PMID: 21634396] |
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 μM) and Adrenergic α1A (Ki = 9.8 μM) receptors, Dopamine transporters (Ki = 11 μM), Norepinephrine transporters (Ki = 10 μM), and phosphodiesterase PDE3 (IC50 = 15 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Irdabisant (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].
Irdabisant (3-30 mg/kg; p.o.; single dosage) exhibits wake-promoting activity in rat[2].
Irdabisant (3-30 mg/kg; i.p.) increases prepulse inhibition (PPI) in DBA/2NCrl mice[2].
Irdabisant (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 | / |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (adult rats were briefly exposed to a juvenile rat for build social recognition model)[2]
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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.
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Administration:i.v. or p.o.; single dosage
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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.
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Animal Model:Male Sprague-Dawley rats[2]
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Dosage:3, 10 and 30 mg/kg
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Administration:p.o.; single dosage
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Result:Exhibited robust wake promotion with the treated animals awake 90% of the time up to 3 h postdosing at 30 mg/kg.
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Animal Model:Male DBA/2NCrl mice (19-27 g; 7-9 weeks)[2]
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Dosage:3, 10 and 30 mg/kg
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Administration:i.p.; single dosage
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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..
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Animal Model:Male Sprague-Dawley rats, male beagle dogs and male cynomolgus monkeys[1]
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Dosage:1 mg/kg for i.v. and 3 mg/kg for p.o.
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Administration:i.v. and p.o.
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1005402-19-6
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Appearance Solid
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Peso molecular 313.39
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Fòrmula C18H23N3O2
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Color Off-white to light yellow
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SMILES
C[C@H](CCC1)N1CCCOC2=CC=C(C(C=C3)=NNC3=O)C=C2
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Synonyms
CEP-26401
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 50 mg/mL (159.55 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Hudkins RL, et al. Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. J Med Chem. 2011 Jul 14;54(13):4781-92. [Content Brief]
[2]. Raddatz R, et al. CEP-26401 (irdabisant), a potent and selective histamine H₃ receptor antagonist/inverse agonist with cognition-enhancing and wake-promoting activities. J Pharmacol Exp Ther. 2012 Jan;340(1):124-33. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 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 |
Irdabisant Related Classifications
HY-109968 Related Classifications
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