Product Details
Product Name:
PRT-060318 |
CAS No.:
1194961-19-7 |
Purity:
98.82% |
Supply Ability:
10g |
Release date:
2024/11/15 |
Product Introduction
Bioactivity
名稱 | PRT-060318 |
描述 | PRT-060318 (P142-76) is a novel selective inhibitor of the Syk tyrosine kinase, as an approach to HIT treatment. |
細(xì)胞實(shí)驗(yàn) | 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. (Only for Reference) |
體外活性 | 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]. |
體內(nèi)活性 | 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]. |
存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | H2O : 5.6 mg/mL (16.45 mM), Sonication and heating are recommended.
|
關(guān)鍵字 | PRT-060318 | PRT-318 | PRT 060318 | Syk | Inhibitor | inhibit | PRT 318 | Spleen tyrosine kinase | PRT060318 |
相關(guān)產(chǎn)品 | Fostamatinib | R112 | Syk-IN-3 | Ellagic acid | Piceatannol | Cerdulatinib | PRT062607 hydrochloride | Fostamatinib Disodium | ANTHRAQUINONE-2-CARBOXYLIC ACID | GSK1904529A | Cerdulatinib hydrochloride | R406 free base |
相關(guān)庫 | 經(jīng)典已知活性庫 | 酪氨酸激酶分子庫 | 激酶抑制劑庫 | 已知活性化合物庫 | 臨床前化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
Product name |
Price |
|
Suppliers |
Update time |
|
$/ |
|
Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |