ABT-925 free base | CAS#220519-06-2 | DRD3 antagonist

MedKoo Cat#: 524126 | Name: ABT-925 free base

Description:

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

ABT-925, also known as A-37203, BSF-201640; DAT-201; Lu-201640; and A-437203, is a selective dopamine D3 receptor (DRD3) antagonist with an approximately 100-fold higher in vitro affinity for dopamine D₃ versus D₂ receptors. ABT-925 was tested in schizophrenia. ABT-925 is a selective dopamine D₃ receptor antagonist with an approximately 100-fold higher in vitro affinity for dopamine D₃ versus D₂ receptors.

Chemical Structure

ABT-925 free base

CAS#220519-06-2 (free base)

Theoretical Analysis

MedKoo Cat#: 524126

Name: ABT-925 free base

CAS#: 220519-06-2 (free base)

Chemical Formula: C20H27F3N6OS

Exact Mass: 456.1919

Molecular Weight: 456.53

Elemental Analysis: C, 52.62; H, 5.96; F, 12.48; N, 18.41; O, 3.50; S, 7.02

Price and Availability

Size	Price	Availability
1mg	USD 150.00	Ready to Ship
5mg	USD 350.00	Ready to Ship
10mg	USD 550.00	Ready to Ship
25mg	USD 1,050.00	Ready to Ship
50mg	USD 1,950.00	Ready to Ship
100mg	USD 3,650.00	Ready to Ship

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Related CAS #

1160247-85-7 (fumarate hydrate) 220519-06-2 (free base) 220519-07-3 (fumarate) ABT-925 HCl

Synonym

A 37203; A-37203; A37203; A 437203; A437203; A-437203; ABT 925; ABT925; ABT-925; BSF 201640; BSF201640; BSF-201640; DAT 201; DAT201; DAT-201; Lu 201640; Lu201640; Lu-201640;

IUPAC/Chemical Name

2-((3-(4-(2-(tert-butyl)-6-(trifluoromethyl)pyrimidin-4-yl)piperazin-1-yl)propyl)thio)pyrimidin-4(3H)-one

InChi Key

KXVAICSRMHXLJN-UHFFFAOYSA-N

InChi Code

InChI=1S/C20H27F3N6OS/c1-19(2,3)17-25-14(20(21,22)23)13-15(26-17)29-10-8-28(9-11-29)7-4-12-31-18-24-6-5-16(30)27-18/h5-6,13H,4,7-12H2,1-3H3,(H,24,27,30)

SMILES Code

O=C1NC(SCCCN2CCN(C3=NC(C(C)(C)C)=NC(C(F)(F)F)=C3)CC2)=NC=C1

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, not in water

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

1160247-85-7; 220519-07-3 (anhydrous) 220519-06-2 (anhydrous free base).

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#A23K02C08

QC Data

View QC data: current batch, Lot#A23K02C08

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

A-437203 is a selective D3 receptor antagonist with Ki of 71, 1.6, and 6220 nM for D2, D3, and D4 receptors.

In vitro activity:

TBD

In vivo activity:

The objective of the study was to compare the abilities of cariprazine, aripiprazole (another DA receptor partial agonist with more D2 receptor preference), and ABT-925 (a selective DA D3 antagonist) to counteract the social deficit and neurochemical alterations induced by the D3 receptor-preferring agonist (+)-PD 128907 (PD) in rats. ABT-925 (3 mg/kg; p.o.) and to a lesser extent aripiprazole (20 mg/kg; p.o.) were effective in blocking the PD-induced disruption of huddling. ABT-925 significantly counteracted the effect of PD at 80 min post-dose. In the nucleus accumbens (nAcc) shell, the highest dose of cariprazine, as well as ABT-925 and aripiprazole, significantly reversed the PD-induced decrease in DA levels. Reference: Front Psychiatry. 2022 Jan 12;12:801641. https://pubmed.ncbi.nlm.nih.gov/35095615/

Preparing Stock Solutions

The following data is based on the product molecular weight 456.53 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. Kehr J, Wang FH, Ichinose F, Yoshitake S, Farkas B, Kiss B, Adham N. Preferential Effects of Cariprazine on Counteracting the Disruption of Social Interaction and Decrease in Extracellular Dopamine Levels Induced by the Dopamine D3 Receptor Agonist, PD-128907 in Rats: Implications for the Treatment of Negative and Depressive Symptoms of Psychiatric Disorders. Front Psychiatry. 2022 Jan 12;12:801641. doi: 10.3389/fpsyt.2021.801641. PMID: 35095615; PMCID: PMC8789685. 2. Ramirez AD, Wong SK, Menniti FS. Pramipexole inhibits MPTP toxicity in mice by dopamine D3 receptor dependent and independent mechanisms. Eur J Pharmacol. 2003 Aug 15;475(1-3):29-35. doi: 10.1016/s0014-2999(03)02087-9. PMID: 12954356.

In vitro protocol:

TBD

In vivo protocol:

1: Kehr J, Wang FH, Ichinose F, Yoshitake S, Farkas B, Kiss B, Adham N. Preferential Effects of Cariprazine on Counteracting the Disruption of Social Interaction and Decrease in Extracellular Dopamine Levels Induced by the Dopamine D3 Receptor Agonist, PD-128907 in Rats: Implications for the Treatment of Negative and Depressive Symptoms of Psychiatric Disorders. Front Psychiatry. 2022 Jan 12;12:801641. doi: 10.3389/fpsyt.2021.801641. PMID: 35095615; PMCID: PMC8789685. 2: Pich EM, Collo G. Pharmacological targeting of dopamine D3 receptors: Possible clinical applications of selective drugs. Eur Neuropsychopharmacol. 2015 Sep;25(9):1437-47. doi: 10.1016/j.euroneuro.2015.07.012. Epub 2015 Jul 21. PMID: 26298833. 3: Bhathena A, Wang Y, Kraft JB, Idler KB, Abel SJ, Holley-Shanks RR, Robieson WZ, Spear B, Redden L, Katz DA. Association of dopamine-related genetic loci to dopamine D3 receptor antagonist ABT-925 clinical response. Transl Psychiatry. 2013 Apr 9;3(4):e245. doi: 10.1038/tp.2013.22. PMID: 23571810; PMCID: PMC3641409. 4: Gross G, Wicke K, Drescher KU. Dopamine D₃ receptor antagonism--still a therapeutic option for the treatment of schizophrenia. Naunyn Schmiedebergs Arch Pharmacol. 2013 Feb;386(2):155-66. doi: 10.1007/s00210-012-0806-3. Epub 2012 Nov 6. PMID: 23128852. 5: Redden L, Rendenbach-Mueller B, Abi-Saab WM, Katz DA, Goenjian A, Robieson WZ, Wang Y, Goss SL, Greco N 4th, Saltarelli MD. A double-blind, randomized, placebo-controlled study of the dopamine D₃ receptor antagonist ABT-925 in patients with acute schizophrenia. J Clin Psychopharmacol. 2011 Apr;31(2):221-5. doi: 10.1097/JCP.0b013e31820e4818. PMID: 21346607. 6: Wan K, Rieser M, El-Shourbagy T. Quantitative Determination of ABT-925 in Human Plasma by On-Line SPE and LC-MS/MS: Validation and Sample Analysis in Phase II Studies. Pharmaceutics. 2010 May 4;2(2):171-181. doi: 10.3390/pharmaceutics2020171. PMID: 27721349; PMCID: PMC3986714. 7: Day M, Bain E, Marek G, Saltarelli M, Fox GB. D3 receptor target engagement in humans with ABT-925 using [11C](+)-PHNO PET. Int J Neuropsychopharmacol. 2010 Apr;13(3):291-2. doi: 10.1017/S1461145710000180. Epub 2010 Mar 3. PMID: 20196920. 8: Graff-Guerrero A, Redden L, Abi-Saab W, Katz DA, Houle S, Barsoum P, Bhathena A, Palaparthy R, Saltarelli MD, Kapur S. Blockade of [11C](+)-PHNO binding in human subjects by the dopamine D3 receptor antagonist ABT-925. Int J Neuropsychopharmacol. 2010 Apr;13(3):273-87. doi: 10.1017/S1461145709990642. Epub 2009 Sep 15. PMID: 19751545.