PRT-060318 2HCl

製品コードS7738 バッチS773801

印刷

化学情報

Chemical Structure Synonyms PRT318 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C18H24N6O.2HCl
分子量 413.34 CAS No. 1194961-19-7(freebase)
Solubility (25°C)* 体外 DMSO 75 mg/mL (181.44 mM)
Water 75 mg/mL (181.44 mM)
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
water
75.0mg/ml Taking the 1 mL working solution as an example, add 75 mg of this product to 1 ml of ddH2O, mix evenly to make it clear, 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 PRT-060318 (PRT318) is a novel selective inhibitor of the Syk tyrosine kinase, as an approach to HIT treatment.
in vitro PRT318 inhibits platelet activation via GPVI/FcRγ, an ITAM receptor complex, but not via ADP or thrombin, which are G-protein coupled receptors[1]. PRT318 effectively antagonizes CLL(chronic lymphocytic leukemia) cell survival after BCR triggering and in nurse-like cell-co-cultures. PRT318 inhibits Syk and extracellular signal-regulated kinase phosphorylation after BCR triggering[2].
in vivo In both rabbit and pig models, intravenous infusion of PRT060318 targets maximal inhibition of Syk kinase activity and significantly inhibits arterial thrombosis. The antithrombotic activity of PRT060318 in pigs is remarkable because it was achieved with complete inhibition of CVXN-induced platelet aggregation, with no effect on ADP-induced platelet aggregation, and no prolongation of ear bleeding time[3]. Also, Syk inhibitor PRT318 is an active agent in HIT. Inhibition of Syk signaling with the orally bio-available PRT318 limits the thrombocytopenic and thrombotic effects of HIT IC in vivo[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 LY3，LY4，LY7,LY18 cell lines
濃度 0-3μM
反応時間 0-72h
実験の流れ

The numbers of cells treated with various doses of PRT318 are followed over time. PRT318 inhibits growth of the sensitive cell lines in a dose-dependent manner. Two sensitive (LY7 and LY18) and 2 resistant (LY3 and LY4) cell lines are treated with indicated doses of PRT318.
動物実験 動物モデル C57Bl/6 Mice; transgenic HIT mice
投薬量 30 mg/kg
投与方法 orally via gavage

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：

D-dimer and CoV-2 spike-immune complexes contribute to the production of PGE2 and proinflammatory cytokines in monocytes [ PLoS Pathog, 2022, 18(4):e1010468] PubMed: 35385545
IgG-aggregates rapidly upregulate FcgRI expression at the surface of human neutrophils in a FcgRII-dependent fashion: A crucial role for FcgRI in the generation of reactive oxygen species [ FASEB J, 2020, 34(11):15208-15221] PubMed: 32946139
cAMP- and cGMP-elevating agents inhibit GPIbα-mediated aggregation but not GPIbα-stimulated Syk activation in human platelets. [ Cell Commun Signal, 2019, 17(1):122] PubMed: 31519182
SYK Targeting Represents a Potential Therapeutic Option for Relapsed Resistant Pediatric ETV6-RUNX1 B-Acute Lymphoblastic Leukemia Patients [ Int J Mol Sci, 2019, 20(24)E6175] PubMed: 31817853
Low catalase expression confers redox hypersensitivity and identifies an indolent clinical behavior in CLL [Cavallini C Blood, 2018, 131(17):1942-1954] PubMed: 29467184
Stress Granules Modulate SYK to Cause Microglial Cell Dysfunction in Alzheimer's Disease. [Ghosh S, et al. EBioMedicine, 2015, 2(11):1785-98] PubMed: 26870803
Stress Granules Modulate SYK to Cause Microglial Cell Dysfunction in Alzheimer's Disease [Hammitzsch A EBioMedicine, 2015, 2(11):1785-98] PubMed: 26870803

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。