| Bioactivity | 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[1][2][3]. |
| Invitro | Ezlopitant (CJ-11,974) 可以在体内转化为两种药理活性代谢物：CJ-12458 (一种烯烃代谢物) 和 CJ-12764 (一种苯甲醇)[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Ezlopitant 相关抗体: |
| In Vivo | Ezlopitant (CJ-11,974；2、5、10 mg/kg；腹腔注射；30 分钟) 可减少大鼠中蔗糖和乙醇的操作性自我给药[1]。Pharmacokinetic Parameters of Ezlopitant in Rat, Gerbil, Guinea pig, Ferret, Dog, Monkey [2]. |
| CAS | 147116-64-1 |
| Formula | C31H38N2O |
| Molar Mass | 454.65 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. [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. [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. |
Ezlopitant
CAS: 147116-64-1 F: C31H38N2O W: 454.65
Ezlopitant (CJ-11,974) is a selective, non-peptidic neurokinin-1 (NK-1)-receptor antagonist. Ezlopitant inhibits both ac
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