GSK1482160 | CAS#1001389-72-5 | P2X7 receptor allosteric modulator

MedKoo Cat#: 530649 | Name: GSK1482160

Description:

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

GSK1482160 is a potent and selective P2X7 receptor allosteric modulator with nanomolar binding affinity and high selectivity. GSK1482160 has been successfully radiolabeled and utilized for imaging P2X7 levels in a mouse model of lipopolysaccharide-induced systemic inflammation.

Chemical Structure

GSK1482160

CAS#1001389-72-5

Theoretical Analysis

MedKoo Cat#: 530649

Name: GSK1482160

CAS#: 1001389-72-5

Chemical Formula: C14H14ClF3N2O2

Exact Mass: 334.0696

Molecular Weight: 334.72

Elemental Analysis: C, 50.24; H, 4.22; Cl, 10.59; F, 17.03; N, 8.37; O, 9.56

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.

Bulk Inquiry

Related CAS #

1695551-19-9 (isomer) 1001389-72-5

Synonym

GSK1482160; GSK-1482160; GSK 1482160.

IUPAC/Chemical Name

(2S)-N-[[2-Chloro-3-(trifluoromethyl)phenyl]methyl]-1-methyl-5-oxo-2-pyrrolidinecarboxamide

InChi Key

IHRKNQDNYKZPNL-JTQLQIEISA-N

InChi Code

InChI=1S/C14H14ClF3N2O2/c1-20(13(22)10-5-6-11(21)19-10)7-8-3-2-4-9(12(8)15)14(16,17)18/h2-4,10H,5-7H2,1H3,(H,19,21)/t10-/m0/s1

SMILES Code

ClC1=C(C=CC=C1CN(C([C@@H]2CCC(N2)=O)=O)C)C(F)(F)F

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

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 334.72 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

1: Han J, Liu H, Liu C, Jin H, Perlmutter JS, Egan TM, Tu Z. Pharmacologic characterizations of a P2X7 receptor-specific radioligand, [11C]GSK1482160 for neuroinflammatory response. Nucl Med Commun. 2017 May;38(5):372-382. doi: 10.1097/MNM.0000000000000660. PubMed PMID: 28338530; PubMed Central PMCID: PMC5401628. 2: Territo PR, Meyer JA, Peters JS, Riley AA, McCarthy BP, Gao M, Wang M, Green MA, Zheng QH, Hutchins GD. Characterization of (11)C-GSK1482160 for Targeting the P2X7 Receptor as a Biomarker for Neuroinflammation. J Nucl Med. 2017 Mar;58(3):458-465. doi: 10.2967/jnumed.116.181354. Epub 2016 Oct 20. PubMed PMID: 27765863. 3: Gao M, Wang M, Green MA, Hutchins GD, Zheng QH. Synthesis of [(11)C]GSK1482160 as a new PET agent for targeting P2X(7) receptor. Bioorg Med Chem Lett. 2015 May 1;25(9):1965-70. doi: 10.1016/j.bmcl.2015.03.021. Epub 2015 Mar 14. PubMed PMID: 25819093. 4: Solini A, Usuelli V, Fiorina P. The dark side of extracellular ATP in kidney diseases. J Am Soc Nephrol. 2015 May;26(5):1007-16. doi: 10.1681/ASN.2014070721. Epub 2014 Dec 1. Review. PubMed PMID: 25452669; PubMed Central PMCID: PMC4413770. 5: Ochoa-Cortes F, Liñán-Rico A, Jacobson KA, Christofi FL. Potential for developing purinergic drugs for gastrointestinal diseases. Inflamm Bowel Dis. 2014 Jul;20(7):1259-87. doi: 10.1097/MIB.0000000000000047. Review. PubMed PMID: 24859298; PubMed Central PMCID: PMC4340257. 6: Ali Z, Laurijssens B, Ostenfeld T, McHugh S, Stylianou A, Scott-Stevens P, Hosking L, Dewit O, Richardson JC, Chen C. Pharmacokinetic and pharmacodynamic profiling of a P2X7 receptor allosteric modulator GSK1482160 in healthy human subjects. Br J Clin Pharmacol. 2013 Jan;75(1):197-207. doi: 10.1111/j.1365-2125.2012.04320.x. PubMed PMID: 22568863; PubMed Central PMCID: PMC3555059.