PLX5622

製品コードS8874 バッチS887404

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₁H₁₉F₂N₅O

分子量

395.41

CAS No.

1303420-67-8

Solubility (25°C)*

体外

DMSO

79 mg/mL (199.79 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5.000mg/ml (12.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	PLX5622 is a highly selective CSF-1R inhibitor (IC50 < 10 nmol/L), showing > 20-fold selectivity over KIT and FLT3.
in vitro	PLX5622 is a highly selective CSF-1R inhibitor (IC50 < 10 nmol/L), showing > 20-fold selectivity over KIT and FLT3.
in vivo	In vivo PLX5622 demonstrates desirable PK properties in mice, rats, dogs, and monkeys, with a brain penetrance of ~20%. This compound has low systemic clearance, moderate volume of distribution, and favorable oral bioavailability (F > 30%) in all four species. It is a useful compound for investigating microglial dynamics. It allows for the sustained and specific elimination of microglia, preceding and during pathology development of Alzheimer’s disease (AD). Long-term this compound-mediated microglial depletion is highly robust, sustainable, and specific to the microglial compartment^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Cell-free assays
	濃度	< 10 nM
	反応時間
	実験の流れ
動物実験	動物モデル	AQP1 mice
	投薬量	100 mg/kg
	投与方法	o.g.

参考

https://www.nature.com/articles/s41467-019-11674-z#Sec25
https://pubmed.ncbi.nlm.nih.gov/31434879/
https://pubmed.ncbi.nlm.nih.gov/33058832/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Targeting formyl peptide receptor 2 to suppress neuroinflammation in neuromyelitis optica spectrum disorder [ Theranostics, 2025, 15(10):4495-4506]	PubMed: 40225578
Inhibition of Bruton's tyrosine kinase restricts neuroinflammation following intracerebral hemorrhage [ Theranostics, 2025, 15(2):494-508]	PubMed: 39744694
Integration and functionality of human iPSC-derived microglia in a chimeric mouse retinal model [ J Neuroinflammation, 2025, 22(1):53]	PubMed: 40016767
CD22 blockade exacerbates neuroinflammation in Neuromyelitis optica spectrum disorder [ J Neuroinflammation, 2024, 21(1):313]	PubMed: 39616380
CD22 blockade modulates microglia activity to suppress neuroinflammation following intracerebral hemorrhage [ Pharmacol Res, 2023, 196:106912]	PubMed: 37696483
Microglial Galectin3 enhances endothelial metabolism and promotes pathological angiogenesis via Notch inhibition by competitively binding to Jag1 [ Cell Death Dis, 2023, 14(6):380]	PubMed: 37369647
Microglial Galectin3 enhances endothelial metabolism and promotes pathological angiogenesis via Notch inhibition by competitively binding to Jag1 [ Cell Death Dis, 2023, 14(6):380]	PubMed: 37369647
Microglia-Derived Spp1 Promotes Pathological Retinal Neovascularization via Activating Endothelial Kit/Akt/mTOR Signaling [ J Pers Med, 2023, 13(1)146]	PubMed: 36675807
A novel histone deacetylase inhibitor-based approach to eliminate microglia and retain astrocyte properties in glial cell culture [ J Neurochem, 2022, 10.1111/jnc.15581]	PubMed: 35092690
Distinguished Functions of Microglia in the Two Stages of Oxygen-Induced Retinopathy: A Novel Target in the Treatment of Ischemic Retinopathy [ Life (Basel), 2022, 12(10)1676]	PubMed: 36295111

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。