VU0152099
规格
| Cas Number | 612514-42-8 |
| 规格或纯度 | ≥98% |
| 纯度 | ≥98% |
| 包装 | 100mg 或 50mg 或 10mg 或 5mg 或 25mg |
产品信息
| 品牌 | 阿拉丁 |
| 溶解性 | DMSO : 12.5 mg/mL (35.17 mM; ultrasonic and warming and heat to 60°C) |
| 过滤标签 | mAChR,GPCR/G Protein,神经元信号传导 |
| 储存温度 | 避光,-80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | VU0152099 是一种强效、选择性和脑穿透性 mAChR M4 阳性异构调节剂，对大鼠 M4 受体的 EC 50 为 0.4 µM。VU0152099 对其他 mAChR 亚型或其他 GPCR 没有活性。VU0152099 没有激动剂活性，但能增强大鼠 M4 受体的反应。 |
| 英文描述 |
VU0152099 is a potent, selective and brain-penetrant mAChR M4 positive allosteric modulator with an EC 50 of 0.4 µM for rat M4 receptor. VU0152099 is inactive for other mAChR subtypes or other GPCRs. VU0152099 has no agonist activity but potentiated responses of M4 to acetylcholine. In Vitro VU0152099 (30 µM) induces a dose-dependent leftward shift of the acetylcholine (ACh) concentration response curve (CRC) with maximal shifts of 30-fold observed with 30 µM. VU0152099 dose-dependently potentiates the response to an EC20 concentration of ACh with EC 50 values of 1.2 µM, and increases the maximal response to ACh to approximately 130%. VU0152099 is a potent positive allosteric modulator that enhance the response of the M4 receptor to the endogenous agonist ACh. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo VU0152099 (56.6 mg/kg; i.p.; once) reverses Amphetamine-induced hyperlocomotion in rats . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague-Dawley rats (270-300 g) injected with Amphetamine Dosage: 56.6 mg/kg Administration: i.p.; once Result: Reversed Amphetamine-induced hyperlocomotion in rats. Form:Solid |