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Netupitant
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Netupitant图片
CAS NO:290297-26-6
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
奈妥吡坦
CID 6451149
产品介绍
Netupitant (CID-6451149) 是高效、选择性、具有口服活性的 Neurokinin-1 受体 (NK1) 拮抗剂,在 CHO 细胞中对 hNK1Ki值为 0.95 nM。Netupitant 具有止吐作用。
生物活性

Netupitant (CID-6451149) is a highly potent, selective and orally activeneurokinin-1 (NK1)receptor antagonist with aKiof 0.95 nM for hNK1in CHO cells. Netupitant has antiemetic affect[1][2][3].

体外研究
(In Vitro)

Netupitant (CID-6451149) binds with high affinity the human NK1receptor (pKi=9.0) with more than 1000 fold selectivity over the NK2and NK3(pKi=5.8 for both sites)[2].
Netupitant (1, 10, 100 nM) concentration-dependently antagonizes the stimulatory effects of substance P (SP) showing insurmountable antagonism (pKB=8.87) in CHO NK1cells[2].

体内研究
(In Vivo)

Netupitant (CID-6451149; 1-10 mg/kg; ip) dose-dependently inhibits SP-elicited the typical scratching, biting and licking response in mice. In gerbils, foot tapping behavior evoked by the intracerebroventricular injection of a NK1agonist is dose-dependently counteracted by Netupitant given intraperitoneally (ID501.5mg/kg) or orally (ID500.5mg/kg)[2].
Netupitant (0.1-3 mg/kg; i.v.) produces a concentration-dependent inhibition (mean pKB=9.24) of the responses to SP-methylester (SP-OMe) in the detrusor muscle. Netupitant decreases the frequency of reflex bladder contractions[3].

Clinical Trial
分子量

578.59

性状

Solid

Formula

C30H32F6N4O

CAS 号

290297-26-6

中文名称

奈妥吡坦;萘妥吡坦

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 9.09 mg/mL(15.71 mM;ultrasonic and warming and heat to 60℃)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.7283 mL8.6417 mL17.2834 mL
5 mM0.3457 mL1.7283 mL3.4567 mL
10 mM0.1728 mL0.8642 mL1.7283 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。