| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S89334-5mg买3赠1 |
99.60% | ￥470.00 |
8 | - | - | - | - |
|
S89334-10mg买3赠1 |
99.60% | ￥820.00 |
8 | - | - | - | - |
|
S89334-25mg促销 |
99.60% | ￥1730.00 ￥1380.00 |
6 | - | - | - | - |
|
S89334-100mg促销 |
99.60% | ￥3710.00 ￥2960.00 |
6 | - | - | - | - |
|
| 产品描述： | RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca2+ mobilization assay. RTICBM-189 has pIC50s of 5.29 and 6.25 for hCB1 and mCB1, respectively. RTICBM-189 significantly and selectively attenuates the reinstatement of the addictive agent-seeking behavior in rats | ||||||||||||||||||||
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| 靶点： | CB1:7.54 (pIC50);hCB1:5.29 (pIC50);mCB1:6.25 (pIC50) | ||||||||||||||||||||
| 体外研究： | RTICBM-189 (10 mg/kg；腹腔注射)迅速吸收进入体循环，在给药后 0.4 小时的 tmax,plasma 观察到峰值血浆浓度 (Cmax,plasma=288.4 ng/mL)。大脑峰值水平也在 0.4 小时 (tmax,brain) 时达到，Cmax,brain 为 594.6 ng/mL Animal Model: Adult male Sprague-Dawley rats weighing 280-300 g Dosage: 10 mg/kg Administration: IP Result: Significantly attenuated drug-induced reinstatement of the cocaine-seeking behavior. Animal Model: Male Sprague-Dawley rats weighing 258-277 g Dosage: 10 mg/kg (Pharmacokinetic Analysis) Administration: IP Result: Plasma: Cmax (288.4 ng/mL), tmax (0.4 hours), CL_F (240.6 mL/min/kg), AUCinf (715.2 ng/mL × h), half-life t1/2 (9.9 hours). Brain: Cmax (594.6 ng/mL), tmax (0.4 hours), CL_F (120.7 mL/min/kg), AUCinf (1438.2 ng/mL × h). | ||||||||||||||||||||
| 体内研究： | RTICBM-189 (10 mg/kg；腹腔注射)迅速吸收进入体循环，在给药后 0.4 小时的 tmax,plasma 观察到峰值血浆浓度 (Cmax,plasma=288.4 ng/mL)。大脑峰值水平也在 0.4 小时 (tmax,brain) 时达到，Cmax,brain 为 594.6 ng/mL。 | ||||||||||||||||||||
| 参考文献： | 1. Nguyen T, et al. Development of 3-(4-Chlorophenyl)-1-(phenethyl)urea Analogues as Allosteric Modulators of the Cannabinoid Type-1 Receptor: RTICBM-189 is Brain Penetrant and Attenuates Reinstatement of Cocaine-Seeking Behavior [published online ahead of print, 2021 Dec 20]. J Med Chem. 2021;10.1021/acs.jmedchem.1c01432. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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