Ro 10-5824 | CAS#189744-46-5 | D4-selective partial agonist

MedKoo Cat#: 530904 | Name: RO10-5824

Description:

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

RO10-5824 is a D4-selective partial agonist. RO10-5824 is a potent candidate for the management of cocaine use disorders.

Chemical Structure

RO10-5824

CAS#189744-46-5

Theoretical Analysis

MedKoo Cat#: 530904

Name: RO10-5824

CAS#: 189744-46-5

Chemical Formula: C17H20N4

Exact Mass: 280.1688

Molecular Weight: 280.38

Elemental Analysis: C, 72.83; H, 7.19; N, 19.98

Price and Availability

Size	Price	Availability
100mg	USD 1,350.00	2 Weeks
200mg	USD 1,850.00	2 Weeks
500mg	USD 2,650.00	2 Weeks
1g	USD 3,450.00	2 Weeks
2g	USD 4,850.00	2 Weeks

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Synonym

RO10-5824; RO 10-5824; RO-10-5824; RO105824; RO 105824; RO-105824.

IUPAC/Chemical Name

2-methyl-5-((4-phenyl-5,6-dihydropyridin-1(2H)-yl)methyl)pyrimidin-4-amine

InChi Key

KABDATZAOUSYES-UHFFFAOYSA-N

InChi Code

InChI=1S/C17H20N4/c1-13-19-11-16(17(18)20-13)12-21-9-7-15(8-10-21)14-5-3-2-4-6-14/h2-7,11H,8-10,12H2,1H3,(H2,18,19,20)

SMILES Code

NC1=NC(C)=NC=C1CN2CC=C(C3=CC=CC=C3)CC2

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

>2 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

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

RO10-5824 is a D4-selective partial agonist (EC50 = 205 nM) that binds with high affinity (Ki = 5.2 nM), and is approximately 250-fold selectivity over D3 receptors and > 1000-fold selectivity over D2, D1 and D5 receptors.

In vitro activity:

To be determined

In vivo activity:

This study presents data from self administration studies in nonhuman primates that shows that intravenous cocaine-maintained behavior is moderately decreased by doses of Ro10-5824. Reference: CNS Neurol Disord Drug Targets. 2015;14(6):707-15. https://pubmed.ncbi.nlm.nih.gov/26022267/

Preparing Stock Solutions

The following data is based on the product molecular weight 280.38 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:

1. Bergman J, Rheingold CG. Dopamine D₄ Receptor Antagonists for the Treatment of Cocaine Use Disorders. CNS Neurol Disord Drug Targets. 2015;14(6):707-15. doi: 10.2174/1871527314666150529132723. PMID: 26022267. 2. Murai T, Nakako T, Ikeda K, Ikejiri M, Ishiyama T, Taiji M. Lack of dopamine D4 receptor affinity contributes to the procognitive effect of lurasidone. Behav Brain Res. 2014 Mar 15;261:26-30. doi: 10.1016/j.bbr.2013.11.036. Epub 2013 Dec 1. PMID: 24304719.

In vitro protocol:

To be determined

In vivo protocol:

1: Bergman J, Rheingold CG. Dopamine D₄ Receptor Antagonists for the Treatment of Cocaine Use Disorders. CNS Neurol Disord Drug Targets. 2015;14(6):707-15. Review. PubMed PMID: 26022267. 2: Murai T, Nakako T, Ikeda K, Ikejiri M, Ishiyama T, Taiji M. Lack of dopamine D4 receptor affinity contributes to the procognitive effect of lurasidone. Behav Brain Res. 2014 Mar 15;261:26-30. doi: 10.1016/j.bbr.2013.11.036. Epub 2013 Dec 1. PubMed PMID: 24304719.