Cariprazine-d6 |
| رقم الكتالوجGC46007 |
Cariprazine D6 (RGH-188 D6) هو الديوتيريوم المسمى Cariprazine
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1308278-67-2
Sample solution is provided at 25 µL, 10mM.
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Cariprazine-d6 is intended for use as an internal standard for the quantification of cariprazine by GC- or LC-MS. Cariprazine is a dopamine D3 and D2 receptor antagonist and partial agonist.1 It binds to D3, D2S, and D2L receptors with Ki values of 0.085, 0.7, and 0.5 nM, respectively, as well as six additional human receptors (Kis = 0.58-208.9 nM) in a panel of 22 human and rat receptors, channels, and transporters at 1 μM. Cariprazine increases inositol phosphate accumulation (EC50 = 3.16 nM) and reduces quinpirole-induced increases in inositol phosphate accumulation (Kb = 0.6 nM) in A9 cells expressing the human D2 receptor. It inhibits forskolin-induced cAMP accumulation (EC50 = 2.63 nM) and reverses 7-OH-DPAT-induced inhibition of forskolin-induced cAMP accumulation (Kb = 0.27 nM) in CHO cells expressing the human D3 receptor. Cariprazine prevents phencyclidine-induced impairment of social recognition, spatial working memory, and extradimensional attention set-shifting in wild-type, but not D3 receptor knockout, mice when administered at doses ranging from 5 to 20 μg/kg.2 Formulations containing cariprazine have been used in the treatment of schizophrenia and bipolar disorder.
|1. Kiss, B., HorvÁth, A., NÉmethy, Z., et al. Cariprazine (RGH-188), a dopamine D3 receptor-preferring, D3/D2 dopamine receptor antagonist-partial agonist antipsychotic candidate: In vitro and neurochemical profile. J. Pharmacol. Exp. Ther. 333(1), 328-340 (2010).|2. Zimnisky, R., Chang, G., GyertyÁn, I., et al. Cariprazine, a dopamine D3-receptor-preferring partial agonist, blocks phencyclidine-induced impairments of working memory, attention set-shifting, and recognition memory in the mouse. Psychopharmacology (Berl) 226(1), 91-100 (2013).
| Cas No. | 1308278-67-2 | SDF | |
| Canonical SMILES | O=C(N(C([2H])([2H])[2H])C([2H])([2H])[2H])N[C@H](CC1)CC[C@@H]1CCN(CC2)CCN2C3=C(Cl)C(Cl)=CC=C3 | ||
| Formula | C21H26D6Cl2N4O | M.Wt | 433.5 |
| الذوبان | DMSO : 33.33 mg/mL (76.89 mM; ultrasonic and warming and heat to 160°C); DMSO : 2 mg/mL (4.61 mM; ultrasonic and warming and heat to 60°C) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3068 mL | 11.534 mL | 23.0681 mL |
| 5 mM | 0.4614 mL | 2.3068 mL | 4.6136 mL |
| 10 mM | 0.2307 mL | 1.1534 mL | 2.3068 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 5 reference(s) in Google Scholar.)
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