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MedKoo Cat#: 150021 | Name: AMG-580

Description:

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

AMG-580 is a selective small-molecule antagonist with subnanomolar affinity for PDE10A. AMG580 is a potential imaging biomarker for mapping PDE10A distribution. Radiolabeled AMG 580 may be suitable for further development as a noninvasive radiotracer for target coverage measurements in clinical studies.

Chemical Structure

AMG-580
AMG-580
CAS#1227067-71-1

Theoretical Analysis

MedKoo Cat#: 150021

Name: AMG-580

CAS#: 1227067-71-1

Chemical Formula: C26H24FN5O3

Exact Mass: 473.1863

Molecular Weight: 473.51

Elemental Analysis: C, 65.95; H, 5.11; F, 4.01; N, 14.79; O, 10.14

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
AMG580; AMG-580; AMG 580;
IUPAC/Chemical Name
1-[4-[3-[4-(1H-Benzimidazole-2-carbonyl)phenoxy]pyrazin-2-yl]piperidin-1-yl]-2-fluoropropan-1-one
InChi Key
NWONINZVPVTBGN-UHFFFAOYSA-N
InChi Code
1S/C26H24FN5O3/c1-16(27)26(34)32-14-10-17(11-15-32)22-25(29-13-12-28-22)35-19-8-6-18(7-9-19)23(33)24-30-20-4-2-3-5-21(20)31-24/h2-9,12-13,16-17H,10-11,14-15H2,1H3,(H,30,31)
SMILES Code
CC(F)C(N1CCC(C2=NC=CN=C2OC3=CC=C(C(C4=NC5=CC=CC=C5N4)=O)C=C3)CC1)=O
Appearance
To be determined
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
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
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

Preparing Stock Solutions

The following data is based on the product molecular weight 473.51 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.

Recalculate based on batch purity %
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
1: Chen H, Lester-Zeiner D, Shi J, Miller S, Glaus C, Hu E, Chen N, Able J, Biorn C, Wong J, Ma J, Michelsen K, Hill Della Puppa G, Kazules T, Dou HH, Talreja S, Zhao X, Chen A, Rumfelt S, Kunz RK, Ye H, Thiel OR, Williamson T, Davis C, Porter A, Immke D, Allen JR, Treanor J. AMG 580: a novel small molecule phosphodiesterase 10A (PDE10A) positron emission tomography tracer. J Pharmacol Exp Ther. 2015 Feb;352(2):327-37. doi: 10.1124/jpet.114.220517. Epub 2014 Dec 11. PMID: 25502803 . 2: Hu E, Chen N, Kunz RK, Hwang DR, Michelsen K, Davis C, Ma J, Shi J, Lester- Zeiner D, Hungate R, Treanor J, Chen H, Allen JR. Discovery of Phosphodiesterase 10A (PDE10A) PET Tracer AMG 580 to Support Clinical Studies. ACS Med Chem Lett. 2016 May 19;7(7):719-23. doi: 10.1021/acsmedchemlett.6b00185. PMID: 27437084; PMCID: PMC4948002. 3: Hwang DR, Hu E, Allen JR, Davis C, Treanor J, Miller S, Chen H, Shi B, Narayanan TK, Barret O, Alagille D, Yu Z, Slifstein M. Radiosynthesis and initial characterization of a PDE10A specific PET tracer [18F]AMG 580 in non- human primates. Nucl Med Biol. 2015 Aug;42(8):654-63. doi: 10.1016/j.nucmedbio.2015.04.004. Epub 2015 Apr 16. PMID: 25935386.