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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C20H19N5O3 |
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分子量 | 377.40 | CAS No. | 1622848-92-3 | |
Solubility (25°C)* | 体外 | DMSO | 75 mg/mL (198.72 mM) | |
Ethanol | 30 mg/mL (79.49 mM) | |||
Water | Insoluble | |||
* <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. |
製品説明 | GSK2982772 is an ATP competitive receptor-interacting protein-1 (RIP1) kinase inhibitor with the IC50 value of 1 nM. It has exquisite kinase specificity and excellent activity in blocking many TNF-dependent cellular responses. |
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in vitro | GSK2982772 has excellent activity in both RIP1 cellular systems, preventing TNF induced necrotic cell death, and an ulcerative colitis explant assay blocking spontaneous cytokine release[1]. |
in vivo | GSK2982772 exhibits approximately equivalent RIP1 FP potency against human and monkey RIP1 but was significantly less potent against nonprimate RIP1. GSK2982772 displays a good free fraction in blood in rats (4.2%), dogs (11%), cynomolgus monkeys (11%), and humans (7.4%). The inhibitor has a good pharmacokinetic profile across both rats and monkeys. GSK2982772 distributes into a range of tissues including the colon, liver, kidney, and heart at concentrations comparable to those of blood. However, it has low brain penetration in rat (4%) despite possessing good cell permeability, which is likely due to active extrusion of GSK2982772 from the brain via the efflux drug transporter. It is predicted that GSK2982772 has high bioavailability, moderate to low clearance with a moderate volume, and a terminal half-life in the order of 12 h[1]. |
動物実験 | 動物モデル | TNF/zVAD mouse model |
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投薬量 | 3, 10, and 50 mg/kg | |
投与方法 | oral administration |
Necrostatin-1 Prevents Ferroptosis in a RIPK1- and IDO-Independent Manner in Hepatocellular Carcinoma [ Antioxidants (Basel), 2021, 10(9)1347] | PubMed: 34572979 |
Pleiotropic, non-cell death-associated effects of inhibitors of receptor-interacting protein kinase 1 in the heart [ Mol Cell Biochem, 2021, 10.1007/s11010-021-04136-y] | PubMed: 33811579 |
Inflammatory signals induce MUC16 expression in ovarian cancer cells via NF-κB activation [ Exp Ther Med, 2021, 21(2):163] | PubMed: 33456530 |
Targeted enhancement of the therapeutic window of L19-TNF by transient and selective inhibition of RIPK1-signaling cascade. [ Oncotarget, 2019, 10(62):6678-6690] | PubMed: 31803362 |
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。