PLX5622

PLX5622

• CAS Number: 1303420-67-8
• UNSPSC Description: PLX5622 is a highly selective brain penetrant and orally active CSF1R inhibitor (IC50=0.016 μM; Ki=5.9 nM). PLX5622 allows for extended and specific microglial cells elimination, preceding and during pathology development. PLX5622 demonstrates desirable PK properties in varies animals[1][2].
• Target Antigen: c-Fms
• Type: Reference compound
• Related Pathways: Protein Tyrosine Kinase/RTK
• Field of Research: Neurological Disease
• Assay Protocol: https://www.medchemexpress.com/plx5622.html
• Purity: 99.95
• Solubility: DMSO : 50 mg/mL (ultrasonic)|Ethanol : 3.33 mg/mL (ultrasonic;warming;heat to 60°C)|H2O : < 0.1 mg/mL
• Smiles: COC1=NC=C(F)C=C1CNC2=NC(F)=C(CC3=CNC4=NC=C(C)C=C43)C=C2
• Molecular Weight: 395.41
• References & Citations: [1]Spangenberg E, et al. Sustained microglial depletion with CSF1R inhibitor impairs parenchymal plaque development in an Alzheimer's disease model. Nat Commun. 2019 Aug 21;10(1):3758.|[2]Lee S, et al. Targeting macrophage and microglia activation with colony stimulating factor 1 receptor inhibitor is an effective strategy to treat injury-triggered neuropathic pain. Mol Pain. 2018 Jan-Dec;14:1744806918764979.|[3]Badimon A, et al. Negative feedback control of neuronal activity by microglia. Nature. 2020;586(7829):417-423.|[4]Andrew J. Riquier, et al. Astrocytic response to neural injury is larger during development than in adulthood and is not predicated upon the presence of microglia, Brain, Behavior, & Immunity-Health, Volume 1, 2020, 100010, ISSN 2666-3546.|[5]Liu Y, et al. Concentration-dependent effects of CSF1R inhibitors on oligodendrocyte progenitor cells ex vivo and in vivo. Exp Neurol. 2019;318:32-41.|[6]Spangenberg EE, et al. Eliminating microglia in Alzheimer's mice prevents neuronal loss without modulating amyloid-β pathology. Brain. 2016;139(Pt 4):1265-1281.Basic Res Cardiol. 2022 Oct 24;117(1):52.|bioRxiv. 2021 Feb 26.|bioRxiv. 2021 Feb 27.|bioRxiv. 2023 May 3.|bioRxiv. 2023 Nov 16.|bioRxiv. 2023 Oct 28.|bioRxiv. 2024 July 02.|bioRxiv. 2024 Nov 4:2024.11.04.621917.|Brain Behav Immun. 2023 Aug 28.|Brain. 2024 Mar 11:awae051.|Cell Death Differ. 2024 May 8.|Cell Death Discov. 2023 Oct 21;9(1):388.|Cell Mol Biol Lett. 2024 Aug 28;29(1):114.|Cell Rep. 2020 Aug 11;32(6):108041.|Cell Rep. 2023 Jun 6;42(6):112617.|Cell. 2023 Sep 28;186(20):4454-4471.e19.|Clin Transl Med. 2024 Apr;14(4):e1665.|Elife. 2021 Jun 23;10:e67772.|EMBO Mol Med. 2022 Dec 21;e17175.|eNeuro. 2023 Oct 27:ENEURO.0323-23.2023.|Eur Arch Psychiatry Clin Neurosci. 2021 Sep 4.|FASEB J. 2024 Jan 31;38(2):e23419.|Fluids Barriers CNS. 2023 Jun 9;20(1):42.|Free Radic Biol Med. 2024 Nov 20.|Glia. 2021 Jul 26.|Immunity. 2024 Oct 9:S1074-7613(24)00458-8.|Int J Mol Sci. 2023 Nov 27, 24(23), 16803.|iScience. 2023 Jun 27.|IUBMB Life. 2024 Sep 2.|J Exp Med. 2023 Mar 6;220(3):e20220857.|J Neuroinflammation. 2022 Dec 14;19(1):300.|J Neuroinflammation. 2023 Nov 17;20(1):269.|J Neuroinflammation. 2024 Apr 10;21(1):88.|JCI Insight. 2024 Feb 6;9(6):e175015.|Mol Pain. Jan-Dec 2020;16:1744806920934998. |Nat Neurosci. 2024 Jun 27.|Nature Cardiovascular Research. 2022 Jul;1(7):649-664.|Nature. 2021 Feb;590(7847):612-617.|Neurobiol Dis. 2022 Nov 1;175:105914.|NMR Biomed. 2024 Aug 20:e5222.|NPJ Parkinsons Dis. 2024 Feb 2;10(1):32.|Patent. US20230203500A1.|PLoS One. 2022 Aug 18;17(8):e0269140.|Research Square Preprint. 2021 Mar.|STAR Protoc. 2021 Jul 7;2(3):100666.|STAR Protoc. 2021 Jun 11;2(2):100613.|STAR Protoc. 2021, 100665.|The University of Texas at San Antonio. 2023 May.|bioRxiv. 2024 Aug 12:2024.08.12.607566.|Nat Commun. 2023 Dec 13;14(1):8273.
• Shipping Conditions: Room Temperature
• Storage Conditions: -20°C, 3 years; 4°C, 2 years (Powder)
• Clinical Information: Phase 1