Desmethyl cariprazine
目录号 : GC62926
Desmethyl cariprazine 是 Cariprazine 的活性代谢产物。Cariprazine，是抗精神病药候选药物，结合 D3, D2 和 5-HT1A 的 Ki 为 0.085 nM，0.49 nM，2.6 nM。
Cas No.:839712-15-1
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Desmethyl cariprazine is an active metabolite of Cariprazine[1]. Cariprazine, an antipsychotic drug candidate, exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (2.6 nM)[2].
[1]. Campbell RH, et al. Review of cariprazine in management of psychiatric illness. Ment Health Clin. 2018 Mar 23;7(5):221-229.
[2]. Seneca N, et al. Occupancy of dopamine D2 and D3 and serotonin 5-HT1A receptors by the novel antipsychotic drug candidate, cariprazine (RGH-188), in monkey brain measured using positron emission tomography. Psychopharmacology (Berl). 2011 Dec;218(3):579-8.
| Cas No. | 839712-15-1 | SDF | |
| 分子式 | C20H30Cl2N4O | 分子量 | 413.38 |
| 溶解度 | 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4191 mL | 12.0954 mL | 24.1908 mL |
| 5 mM | 0.4838 mL | 2.4191 mL | 4.8382 mL |
| 10 mM | 0.2419 mL | 1.2095 mL | 2.4191 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.