Argatroban (MCI-9038)

製品コードS2069 バッチS206903

印刷

化学情報

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

C23H36N6O5S
分子量 508.63 CAS No. 74863-84-6
Solubility (25°C)* 体外 DMSO 100 mg/mL (196.6 mM)
Ethanol 100 mg/mL (196.6 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.

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生物活性

製品説明 Argatroban (MCI-9038) is a potent and selective synthetic thrombin inhibitor with Ki ranging from 5 nM to 39 nM, used as an anticoagulant.
in vitro Argatroban is a potent and selective synthetic thrombin inhibitor with Ki values against thrombin ranging from 5 nM to 39 nM. Argatroban has antithrombotic properties in a wide variety of animal models of both platelet-rich and erythrocyte-rich thrombosis. Argatroban dose-dependently prevents thrombus formation with an estimated ED50 of 125 μg/kg in this test. Argatroban produces a dose-dependent increases in the thrombin time with a 511% increase at the highest dose used with only a 73% increase in the APTT at this dose. [1] Argatroban can directly induce phenotype conversion of vascular smooth muscle cells with the resultant up-regulation of SMemb, PAI-1, and beta-actin mRNAs. [2]
in vivo Argatroban inhibits the formation of microthrombi up to 3 hours after middle cerebral artery (MCA) occlusion; beyond 3 hours, it is ineffective. Argatroban also significantly reduces the size of ischemic cerebral lesions at 6 hours after MCA occlusion. [3] Argatroban (0.3 mg/h/rat) significantly decreases the number of microthrombi 1 day after distal middle cerebral artery (dMCA) occlusion in the rat distal middle cerebral artery occlusion model. Argatroban (0.1 and 0.3 mg/h/rat) significantly reverses a decrease in regional cerebral blood flow (rCBF) 1 day after distal middle cerebral artery (dMCA) occlusion. Argatroban (0.3 mg/h/rat) also significantly reduces the size of the cerebral infarction. [4]

プロトコル(参考用のみ)

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：

Argatroban promotes recovery of spinal cord injury by inhibiting the PAR1/JAK2/STAT3 signaling pathway [ Neural Regen Res, 2024, 19(2):434-439] PubMed: 37488908
Tissue factor-induced fibrinogenesis mediates cancer cell clustering and multiclonal peritoneal metastasis [ Cancer Lett, 2023, 553:215983] PubMed: 36404569
Delayed administration of nafamostat mesylate inhibits thrombin-mediated blood-spinal cord barrier breakdown during acute spinal cord injury in rats [ J Neuroinflammation, 2022, 19(1):189] PubMed: 35842640
Thrombin inhibitor argatroban modulates bone marrow stromal cells behaviors and promotes osteogenesis through canonical Wnt signaling [ Life Sci, 2021, 269:119073] PubMed: 33460666
MRG15 orchestrates rhythmic epigenomic remodelling and controls hepatic lipid metabolism [ Nat Metab, 2020, 2(5):447-460] PubMed: 32694659
Detection of subclinical arthritis in mice by a thrombin receptor–derived imaging agent [Friedman B Arthritis Rheumatol, 2018, 70(1):69-79] PubMed: 29164814

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。