SUVN-911
规格
| Cas Number | 2414674-71-6(DMSO) |
| 规格或纯度 | 10mM in DMSO |
| 包装 | 1ml |
产品信息
| 品牌 | 阿拉丁 |
| 浓度 | 10mM in DMSO |
| 过滤标签 | nAChR,神经元信号传导,膜转运器/离子通道,Compound libraries |
| 储存温度 | 干燥,-80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | SUVN-911 是一种强效、选择性、脑穿透性和口服生物可用性神经元烟碱乙酰胆碱 α4β2 受体拮抗剂，其 K i 为 1.5 nM。SUVN-911 具有抗抑郁活性。 |
| 英文描述 |
SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a K i of 1.5 nM. SUVN-911 has antidepressant activity In Vitro SUVN-911 displays high selectivity for α4β2 over α3β4 nAChR. SUVN-911 shows good selectivity against over 70 receptors which includes GPCRs, ion channels, enzymes, peptides, steroids, second messengers, growth factors and prostaglandins. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo SUVN-911 is devoid of cardiovascular and gastrointestinal side effects . SUVN-911 (1.0-10.0 mg/kg; p.o.; daily; for 3 days) shows significant antidepressant effects . SUVN-911 shows metabolic stability in rats . SUVN-911 (3 mg/kg; p.o.) has shown high oral exposures, longer half-lives and adequate brain penetration in Wistar rats . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Wistar rats (180-230 g) Dosage: 1 mg/kg, 3 mg/kg, 10.0 mg/kg Administration: Oral administration, daily, for 3 days Result: Showed antidepressant like activity with no signs of tachyphylaxis. Animal Model: Male Wistar rats (225 ± 25 g) Dosage: 3 mg/kg (Pharmacokinetic Analysis) Administration: Oral administration Result: AUC=3507 ng*h/mL, T 1/2 =3.34 hours. IC50& Target:Ki: 1.5 nM (α4β2 receptor) |