Ezlopitant
Ezlopitant (CJ-11,974) is a selective, non-peptidic neurokinin-1 (NK-1)-receptor antagonist. Ezlopitant inhibits both acute and delayed emetic reactions induced by Cisplatin (HY-17394) in ferrets via acting on NK1 receptors in the central nervous system. Ezlopitant has the potential for pain, chemotherapy-induced emesis and irritable bowel syndrome research.
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- CAS No.: 147116-64-1
- Formule: C31H38N2O
- Masse moléculaire:454.65
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Ezlopitant (CJ-11,974) is converted to two pharmacologically active metabolites: CJ-12458, an alkene metabolite and CJ-12764, a benzylic alcohol[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pharmacokinetic Parameters of Ezlopitant in Rat, Gerbil, Guinea pig, Ferret, Dog, Monkey [2].
| Rat (IV; 1 mg/kg) | Gerbil (IV; 1 mg/kg) | Guinea pig (IV; 0.2 mg/kg) | Ferret (SC; 0.8 mg/kg) | Dog (IV; 1 mg/kg) | Monkey (IV; 1 mg/kg) | |
| Tmax (h) | 5.3 | 0.3 | 0.3 | 0.9 | 0.8 | |
| Cmax (ng/mL) | 18 | 5.98 | 106 | 5.98 | 198 | |
| AUC0-∞ (ng∗h/mL) | 257 | 125 | 35.5 | 528 | 634 | 478 |
| t1/2 (h) | 7.7 | 2.9 | 0.6 | 2.2 | 2.5 | 5.0 |
| CLp (mL/min/kg) | 65 | 136 | 98 | 27 | 27 | 42 |
| F (%) | 15 | 2.1 | 17 | 28 | 2.7 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male, Long-Evans rats (233±2 g)[1]
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Dosage:2, 5 or 10 mg/kg
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Administration:IP; single dose
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Result:Attenuated the number of active lever presses for 5% sucrose.
Highest dose significantly inhibited operant self-administration of 10% ethanol compared with vehicle.
Chemical Information
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CAS No. 147116-64-1
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Masse moléculaire 454.65
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Formule C31H38N2O
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SMILES
COC(C=CC(C(C)C)=C1)=C1CN[C@@H](C2CCN3CC2)[C@@H]3C(C4=CC=CC=C4)C5=CC=CC=C5
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Synonyms
CJ-11,974
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Pia Steensland, et al. The neurokinin 1 receptor antagonist, ezlopitant, reduces appetitive responding for sucrose and ethanol. PLoS One. 2010 Sep 1;5(9):e12527. [Content Brief]
[2]. A E Reed-Hagen, et al. Pharmacokinetics of ezlopitant, a novel non-peptidic neurokinin-1 receptor antagonist in preclinical species and metabolite kinetics of the pharmacologically active metabolites. Biopharm Drug Dispos. 1999 Dec;20(9):429-39. [Content Brief]
[3]. Megumi Tsuchiya, et al. Anti-emetic activity of the novel nonpeptide tachykinin NK1 receptor antagonist ezlopitant (CJ-11,974) against acute and delayed cisplatin-induced emesis in the ferret. Pharmacology. 2002 Nov;66(3):144-52. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Ezlopitant Related Classifications
HY-106982 Related Classifications
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