Brexpiprazole-d8
(Synonyms: 依匹唑派杂质,OPC-34712-d8) 目录号 : GC46948
An internal standard for the quantification of brexpiprazole
Cas No.:1427049-21-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Brexpiprazole-d8 is intended for use as an internal standard for the quantification of brexpiprazole by GC- or LC-MS. Brexpiprazole is a serotonin (5-HT) and dopamine receptor modulator that has high affinity (Ki = <1 nM) for 5-HT1A and 5-HT2A serotonin, dopamine D2L, and α1B-, and α2C-adrenergic receptors in CHO cell membranes expressing the human receptors.1 It acts as a partial agonist of 5-HT1A, D2L, and D3 receptors (EC50s = 0.49, 4.0, and 2.8 nM, respectively) and an antagonist of 5-HT2A, 5-HT2B, as well as α1B- and α2C-adrenergic receptors (IC50s = 6.5, 14, 0.66, and 63 nM, respectively) in vitro. In vivo, brexpiprazole dose-dependently reduces conditioned avoidance response (CAR) time, inhibits locomoter hyperactivity induced by apomorphine and amphetamine, and reverses cognitive defects induced by subchronic PCP administration in rats.2 It also reduces apomorphine-induced eye blinking in cynomolgus monkeys. Formulations containing brexpiprazole have been used in the treatment of schizophrenia and major depressive disorder.
1.Maeda, K., Sugino, H., Akazawa, H., et al.Brexpiprazole I: In vitro and in vivo characterization of a novel serotonin-dopamine activity modulatorJ. Pharmacol. Exp. Ther.350(3)589-604(2014) 2.Maeda, K., Lerdrup, L., Sugino, H., et al.Brexpiprazole II: Antipsychotic-like and procognitive effects of a novel serotonin-dopamine activity modulatorJ. Pharmacol. Exp. Ther.350(3)605-614(2014)
| Cas No. | 1427049-21-5 | SDF | |
| 别名 | 依匹唑派杂质,OPC-34712-d8 | ||
| Canonical SMILES | O=C1C=CC2=C(C=C(OCCCCN3C([2H])([2H])C([2H])([2H])N(C4=C(C=CS5)C5=CC=C4)C([2H])([2H])C3([2H])[2H])C=C2)N1 | ||
| 分子式 | C25H19D8N3O2S | 分子量 | 441.6 |
| 溶解度 | DMSO: soluble | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2645 mL | 11.3225 mL | 22.6449 mL |
| 5 mM | 0.4529 mL | 2.2645 mL | 4.529 mL |
| 10 mM | 0.2264 mL | 1.1322 mL | 2.2645 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。