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- 详细信息
- 技术资料
- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名:
CID 6451149
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
290297-26-6
- 规格:
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg/50 mg/100 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥662.0 |
|---|---|---|---|
| 规格: | 1 mg | 产品价格: | ¥245.0 |
| 规格: | 5 mg | 产品价格: | ¥520.0 |
| 规格: | 10 mg | 产品价格: | ¥630.0 |
| 规格: | 25 mg | 产品价格: | ¥1260.0 |
| 规格: | 50 mg | 产品价格: | ¥1920.0 |
| 规格: | 100 mg | 产品价格: | ¥3080.0 |
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Netupitant
CAS No. : 290297-26-6
MCE 国际站:Netupitant
产品活性: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 hNK1 的 Ki 值为 0.95 nM。Netupitant 具有止吐作用。
研究领域:GPCR/G Protein | Neuronal Signaling
作用靶点:Neurokinin Receptor
In Vitro: Netupitant (CID-6451149) binds with high affinity the human NK1 receptor (pKi=9.0) with more than 1000 fold selectivity over the NK2 and NK3 (pKi=5.8 for both sites).
Netupitant (1, 10, 100 nM) concentration-dependently antagonizes the stimulatory effects of substance P (SP) showing insurmountable antagonism (pKB=8.87) in CHO NK1 cells.
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 NK1 agonist is dose-dependently counteracted by Netupitant given intraperitoneally (ID50 1.5mg/kg) or orally (ID50 0.5mg/kg).
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.
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