Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
500mg |
|
||
Other Sizes |
|
Purity: ≥98%
Cariprazine (formerly known as MP-214 and RGH-188; Vraylar; Reagila) is a novel and potent antipsychotic drug that has been approved for the treatment of schizophrenia, as well as for bipolar disorder (manic/mixed and depressive episodes), and as an adjunctive agent for the treatment of major depressive disorders. Cariprazine is a partial agonist of the D3/D2 receptors that selectively binds to the D3 receptor (Ki of 0.085 nM), the D2 receptor (Ki of 0.49 nM), and the 5-HT1A receptor (Ki of 2.6 nM). It is a dopamine D3-preferring receptor. Cariprazine has a relatively low efficaciousness (Emax 30%) but a high potency (pEC50 8.5) in stimulating the formation of inositol phosphate (IP).
Targets |
D2 Receptor ( Ki = 0.49 nM ); D3 receptor ( Ki = 0.085 nM ); 5-HT1A Receptor ( Ki = 2.6 nM )
|
|
---|---|---|
ln Vitro |
|
|
ln Vivo |
|
|
Enzyme Assay |
These tests are conducted in the following solutions: 50 mM Tris (pH 7.4), 100 mM NaCl, 7 mM MgCl2, 1 mM EDTA, and 1 mM DTT. The ligand to be investigated, the membrane suspension (250 μg protein/tube for hD2 and hD3 membranes, and 50 μM GDP for the striatum and hippocampus and 1 μM for D2 and D3 cell membrane) and assay tubes (final volume 250 μL) are put into each tube. 30°C is used for a 10-minute preincubation period. Membranes are cultivated at 30°C for 60 minutes following the addition of 50 pM [35S]GTPγS. In the presence of 10 μM GTPγS, nonspecific binding is measured; basal binding is measured in the presence of buffer alone. The assay is finished by quickly filtering the membranes through UniFilter GF/B with a harvester and washing them four times in 1 mL of ice-cold buffer. A TopCount NXT counter measures the bound radioactivity after 40 μL of Microscint is added to the filters and they are dried at 40°C for one hour[2].
|
|
Cell Assay |
On a tissue culture plate with 24 wells, 500 μL of medium is used to seed cells. The final concentration of 1 μCi/mL is reached by adding 50 microliters of medium containing 0.55 μCi myo-[3H]inositol, and the mixture is incubated for 18–20 hours. After that, cells are passed through three rounds of washing in a buffer that has the following concentrations: 140 mM NaCl, 5 mM KCl, 2 mM CaCl2, 5 mM HEPES, 5 mM Na-HEPES, 20 mM glucose, and 10 mM LiCl (pH 7.4). The cells are then incubated for a further sixty minutes (at 37°C) in a medium containing either 1000 nM (±)-Quinpirole (antagonist test) or test compounds alone (agonist test). The medium is then removed by aspiration, 400 μL of 0.1 M HCl/2 mM CaCl2 is added to lyse the cells, and the supernatants are frozen at -72°C. Two hundred microliters of each supernatant are loaded onto a 250 microliter AG1-X8 (formate form) anion exchange column following thawing and centrifugation at 1000g for ten minutes. Two rounds of column washing in 1.5 mL of distilled water follow the disposal of the effluent. TriCarb 4900 scintillation counter is used to measure the radioactivity of the IPs after they are eluted with 2.5 mL of 1 M ammonium formate/0.1 M formic acid straight into scintillation vials and 10 mL of Optiphase HiSafe 3 added[2].
|
|
Animal Protocol |
|
|
References |
|
Molecular Formula |
C21H32CL2N4O
|
---|---|
Molecular Weight |
463.87
|
Exact Mass |
426.2
|
Elemental Analysis |
C, 59.01; H, 7.55; Cl, 16.59; N, 13.11; O, 3.74
|
CAS # |
839712-12-8
|
Related CAS # |
Cariprazine hydrochloride; 1083076-69-0; Cariprazine-d6; 1308278-67-2; Cariprazine-d8; 1308278-50-3
|
Appearance |
Solid powder
|
SMILES |
CN(C)C(=O)NC1CCC(CC1)CCN2CCN(CC2)C3=C(C(=CC=C3)Cl)Cl
|
InChi Key |
KPWSJANDNDDRMB-UHFFFAOYSA-N
|
InChi Code |
InChI=1S/C21H32Cl2N4O/c1-25(2)21(28)24-17-8-6-16(7-9-17)10-11-26-12-14-27(15-13-26)19-5-3-4-18(22)20(19)23/h3-5,16-17H,6-15H2,1-2H3,(H,24,28)
|
Chemical Name |
3-[4-[2-[4-(2,3-dichlorophenyl)piperazin-1-yl]ethyl]cyclohexyl]-1,1-dimethylurea
|
Synonyms |
GH-188; MP-214; MP214; MP 214; RGH188; RGH 188; Cariprazine; Brand name: Vraylar
|
HS Tariff Code |
2934.99.9001
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
|
|||
---|---|---|---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.34 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1 mg/mL (2.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1558 mL | 10.7789 mL | 21.5578 mL | |
5 mM | 0.4312 mL | 2.1558 mL | 4.3116 mL | |
10 mM | 0.2156 mL | 1.0779 mL | 2.1558 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT05368558 | Recruiting | Drug: Cariprazine Drug: Placebo |
Schizophrenia | AbbVie | August 18, 2022 | Phase 3 |
NCT05913947 | Recruiting | Drug: Lithium Drug: Cariprazine |
Depression, Bipolar | Aalborg University Hospital | December 13, 2022 | Phase 4 |
NCT04777357 | Recruiting | Drug: Cariprazine Drug: Placebo |
Depression Bipolar I Disorder |
AbbVie | April 28, 2021 | Phase 3 |
NCT05439616 | Recruiting | Drug: Cariprazine Drug: Placebo |
Autism Spectrum Disorder | AbbVie | July 7, 2022 | Phase 3 |
NCT04771299 | Recruiting | Drug: Cariprazine Drug: Placebo |
Bipolar I Disorder Cognitive Impairment |
Jayasree Basivireddy | July 7, 2021 | Phase 3 |
Open field activity immediately after injection with ouabain Acute administration of cariprazine inhibits ICV ouabain-induced motoric hyperactivity in rats. Pharmacol Res Perspect . 2015 Feb;3(1):e00073. td> |
The effect of cariprazine on the behavior of mice exposure to the EPM. Psychopharmacology (Berl) . 2013 Mar;226(1):91-100. td> |
The effect of cariprazine on PCP-induced impairment of social interaction (T1) and social recognition memory (T2; T1-T2) in wild-type and D3-receptor knockout mice. Psychopharmacology (Berl) . 2013 Mar;226(1):91-100. td> |