Desmethyl cariprazine

WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 581298

CAS#: 839712-15-1

Description: Desmethyl Cariprazine Hydrochloride is a derivative of Cariprazine (C183490) which is an orally active D2/D3 dopamine receptor antagonist (1,2,3). Cariprazine is an antipsychotic drug candidate for the potential treatment of schizophrenia, bipolar mania and depression.

Chemical Structure

Desmethyl cariprazine

CAS# 839712-15-1

Instruction

Theoretical Analysis

MedKoo Cat#: 581298
Name: Desmethyl cariprazine
CAS#: 839712-15-1
Chemical Formula: C20H30Cl2N4O
Exact Mass: 412.18
Molecular Weight: 413.390
Elemental Analysis: C, 58.11; H, 7.32; Cl, 17.15; N, 13.55; O, 3.87

Price and Availability

Size	Price	Availability	Quantity
1g	USD -1
2g	USD -1
5g	USD -1
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: Desmethyl cariprazine; Dcar; UNII-286RCD7025;

IUPAC/Chemical Name: Urea, N-(trans-4-(2-(4-(2,3-dichlorophenyl)-1-piperazinyl)ethyl)cyclohexyl)-N'-methyl-

InChi Key: WMQLLTKSISGWHQ-WKILWMFISA-N

InChi Code: InChI=1S/C20H30Cl2N4O/c1-23-20(27)24-16-7-5-15(6-8-16)9-10-25-11-13-26(14-12-25)18-4-2-3-17(21)19(18)22/h2-4,15-16H,5-14H2,1H3,(H2,23,24,27)/t15-,16-

SMILES Code: O=C(NC)N[C@H]1CC[C@H](CCN2CCN(C3=CC=CC(Cl)=C3Cl)CC2)CC1

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.03.00

More Info:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 413.39 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Campbell RH, Diduch M, Gardner KN, Thomas C. Review of cariprazine in management of psychiatric illness. Ment Health Clin. 2018 Mar 23;7(5):221-229. doi: 10.9740/mhc.2017.09.221. eCollection 2017 Sep. PubMed PMID: 29955527; PubMed Central PMCID: PMC6007710.

2: Citrome L. Cariprazine for the Treatment of Schizophrenia: A Review of this Dopamine D3-Preferring D3/D2 Receptor Partial Agonist. Clin Schizophr Relat Psychoses. 2016 Summer;10(2):109-19. doi: 10.3371/1935-1232-10.2.109. Review. PubMed PMID: 27440212.

3: Nakamura T, Kubota T, Iwakaji A, Imada M, Kapás M, Morio Y. Clinical pharmacology study of cariprazine (MP-214) in patients with schizophrenia (12-week treatment). Drug Des Devel Ther. 2016 Jan 14;10:327-38. doi: 10.2147/DDDT.S95100. eCollection 2016. PubMed PMID: 26834462; PubMed Central PMCID: PMC4716719.

4: Citrome L. Cariprazine: chemistry, pharmacodynamics, pharmacokinetics, and metabolism, clinical efficacy, safety, and tolerability. Expert Opin Drug Metab Toxicol. 2013 Feb;9(2):193-206. doi: 10.1517/17425255.2013.759211. Review. PubMed PMID: 23320989.

5: Mészáros GP, Agai-Csongor E, Kapás M. Sensitive LC-MS/MS methods for the quantification of RGH-188 and its active metabolites, desmethyl- and didesmethyl-RGH-188 in human plasma and urine. J Pharm Biomed Anal. 2008 Sep 29;48(2):388-97. doi: 10.1016/j.jpba.2007.12.016. Epub 2007 Dec 23. PubMed PMID: 18242914.

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