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Brilaroxazine (RP5063) 是一种有效的多模式多巴胺/5-HT 调节剂。 Brilaroxazine 是多巴胺 D2、D3 和 D4 受体、5-HT1A (Ki = 1.5 nM) 和 5-HT2A (Ki = 2.5 nM) 的部分激动剂,具有拮抗活性 5-HT2B 和 5-HT7 受体,Ki 分别为 0.19 nM 和 2.7 nM。 Brilaroxazine 可用于研究神经精神和神经系统疾病的认知障碍。
Brilaroxazine (RP5063) 是一种有效的多模式多巴胺/5-HT 调节剂。 Brilaroxazine 是多巴胺 D2、D3 和 D4 受体、5-HT1A (Ki = 1.5 nM) 和 5-HT2A (Ki = 2.5 nM) 的部分激动剂,具有拮抗活性 5-HT2B 和 5-HT7 受体,Ki 分别为 0.19 nM 和 2.7 nM。 Brilaroxazine 可用于研究神经精神和神经系统疾病的认知障碍。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 1,090 | 现货 | |
5 mg | ¥ 2,650 | 现货 | |
10 mg | ¥ 3,980 | 现货 | |
25 mg | ¥ 6,830 | 现货 | |
50 mg | ¥ 9,220 | 现货 | |
100 mg | ¥ 12,300 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 2,950 | 现货 |
产品描述 | Brilaroxazine (RP5063) is a potent multimodal dopamine/5-HT modulator. Brilaroxazine is a partial agonist of dopamine D2, D3, and D4 receptors, 5-HT1A (Ki =1.5 nM) and 5-HT2A (Ki = 2.5 nM), and has antagonist activity 5-HT2B, and 5-HT7 receptors with Kis of 0.19 nM and 2.7 nM, respectively. Brilaroxazine can be used for research about cognitive impairments in neuropsychiatric and neurological diseases. |
靶点活性 | 5-HT1A receptor:1.5 nM (Ki), 5-HT7 receptor:2.7 nM (Ki), 5-HT2A receptor:2.5 nM (Ki), 5-HT2B receptor:0.19 nM (Ki) |
体内活性 | Brilaroxazine (10 mg/kg) had efficacy in PAH, and mitigated the functional and structural effects of MCT-induced PAH, with significant improvements in pulmonary hemodynamics, right ventricular (RV) hypertrophy, SO2, and pulmonary blood vessel structural changes[3]. |
别名 | RP5063 |
分子量 | 450.36 |
分子式 | C22H25Cl2N3O3 |
CAS No. | 1239729-06-6 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 95 mg/mL (210.94 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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