Didesmethyl cariprazine
目录号 : GC62932
Didesmethyl cariprazine 是 Cariprazine 的代谢物，作为主要的循环活性部分。Didesmethyl cariprazine 的半衰期较长，为 1-3 周。Cariprazine是一种新型抗精神病候选药物，能结合 D3, D2 和 5-HT1A 。
Cas No.:839712-25-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Didesmethyl cariprazine is a metabolite of Cariprazine and acts as the predominant circulating active moiety. Didesmethyl cariprazine has a long half-life of 1-3 weeks. Cariprazine is a antipsychotic drug candidate that exhibits high affinity for the D3 and D2 receptors, and moderate affinity for the 5-HT1A receptor[1].
[1]. Citrome L, et al. Cariprazine for acute and maintenance treatment of adults with schizophrenia: an evidence-based review and place in therapy. Neuropsychiatr Dis Treat. 2018 Oct 5;14:2563-2577.
| Cas No. | 839712-25-3 | SDF | |
| 分子式 | C19H28Cl2N4O | 分子量 | 399.36 |
| 溶解度 | DMSO : 11.36 mg/mL (28.45 mM; ultrasonic and warming and heat to 80°C) | 储存条件 | |
| 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 | 2.504 mL | 12.52 mL | 25.0401 mL |
| 5 mM | 0.5008 mL | 2.504 mL | 5.008 mL |
| 10 mM | 0.2504 mL | 1.252 mL | 2.504 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。
Review of cariprazine in management of psychiatric illness
Ment Health Clin 2018 Mar 23;7(5):221-229.PMID:29955527DOI:10.9740/mhc.2017.09.221.
Schizophrenia and bipolar disorder are severe and debilitating psychiatric disorders. Despite the availability of numerous antipsychotic drugs, many patients still experience poor outcomes and treatment-limiting adverse side effects. Cariprazine is a novel antipsychotic with unique pharmacodynamic and pharmacokinetic properties. It is both a dopamine type 2 and dopamine type 3 partial agonist with 2 equipotent metabolites, desmethyl cariprazine and Didesmethyl cariprazine, of which Didesmethyl cariprazine has a half-life of 1 to 3 weeks. The objective of this article is to review the literature regarding efficacy and tolerability of cariprazine in the management of psychiatric disorders to determine its current place in therapy.