Verubecestat (MK-8931) Trifluoroacetate

製品コードS8173 バッチS817301

印刷

化学情報

Chemical Structure Synonyms MK-8931 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C19H18F5N5O5S
分子量 523.43 CAS No. 2095432-65-6
Solubility (25°C)* 体外 DMSO 81 mg/mL (154.74 mM)
Ethanol 5 mg/mL (9.55 mM)
Water 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.
* <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 Verubecestat (MK-8931) Trifluoroacetateは、強力で選択的なbeta-secretase阻害剤、BACE1 protein阻害剤、またはBeta-site APP-cleaving enzyme 1阻害剤です。
in vitro Verubecestat(MK-8931) effectively reduces Aβ40 in cells with a Ki of 7.8 nM and an IC50 of 13 nM.
in vivo Verubecestat(MK-8931) dramatically lowers CSF and cortex Aβ40 in both rats and cynomolgus monkeys following a single oral dose. Due to the 20 h half-life of MK-8931 it is ideal for once-a-day dosing.

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/27023706/
  • https://pubmed.ncbi.nlm.nih.gov/27418961/

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 BACE1-mediated production of amyloid beta improves hippocampal synaptic function in an experimental model of ischemic stroke [ Journal of Cerebral Blood Flow & Metabolism, 2023, 1235-1250] PubMed: nan
A study of protein-drug interaction based on solvent-induced protein aggregation by fluorescence correlation spectroscopy [ Analyst, 2022, 10.1039/d2an00031h] PubMed: 35253833
Pharmacological inhibition of BACE1 suppresses glioblastoma growth by stimulating macrophage phagocytosis of tumor cells [ Nature Cancer, 2021, 1136-1151] PubMed: 35122055.0
Pharmacological inhibition of BACE1 suppresses glioblastoma growth by stimulating macrophage phagocytosis of tumor cells [ Nat Cancer, 2021, 2(11):1136-1151] PubMed: 35122055
Improving preclinical to clinical translation in Alzheimers disease research [ Alzheimers & Dementia: Translational Research & Clinical Interventions, 2020, e12038] PubMed: 32548237.0
Improving Preclinical to Clinical Translation in Alzheimer's Disease Research [ Alzheimers Dement (N Y), 2020, 6(1):e12038] PubMed: 32548237
Pharmacokinetic, Pharmacodynamics, and Transcriptomics Analysis of Verubecestat Treatment in 5XFAD mice [ Alzheimer's Association, 2020, 16-S2] PubMed: None
Inhibition of BACE1 Facilitates Macrophage-based Immunotherapy to Suppress Malignant Growth of Glioblastoma [ Research Square, 2020, 10.21203/rs.3.rs-61939/v1] PubMed: None
Aβ34 is a BACE1-derived degradation intermediate associated with amyloid clearance and Alzheimer's disease progression. [ Nat Commun, 2019, 10(1):2240] PubMed: 31110178
Multiple BACE1 inhibitors abnormally increase the BACE1 protein level in neurons by prolonging its half-life. [ Alzheimers Dement, 2019, 15(9):1183-1194] PubMed: 31416794

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。