Argatroban Monohydrate

製品コードS5074 バッチS507401

印刷

化学情報

Synonyms

Argatroban hydrate, Argipidine,MCI-9038 Monohydrate

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₃H₃₆N₆O₅S.H₂O

分子量

526.65

CAS No.

141396-28-3

Solubility (25°C)*

体外

DMSO

100 mg/mL (189.87 mM)

Ethanol

40 mg/mL (75.95 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution

5%DMSO 1 Corn oil

2.25mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 45 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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	Argatroban (Argatroban hydrate, Argipidine,MCI-9038 Monohydrate) is a direct, selective thrombin inhibitor with anticoagulant effects.
in vitro	Argatroban is highly selective for thrombin and has little or no effect on related serine proteases (trypsin, factor Xa, plasmin, and kallikrein). Argatroban is effective against free, fibrin-bound and clot-bound thrombin with comparable half-maximal inhibitory concentrations (IC50), and argatroban is also effective in inhibiting platelet aggregation and thromboxane generation in the presence of both free and clot-bound thrombin^[1]. Argatroban binds thrombin and inhibits its activity without the requirement of coenzymes, unlike antithrombin III or heparin cofactor II. Argatroban decreases bone metastasis of B16 mouse melanoma cells by inactivating thrombin activity. Moreover, argatroban has potential to inhibit PAR-2 activation by interfering with the thrombogenic cycle. It does not have toxic effect for tumor cells^[2].
in vivo	Within a clinically relevant dose range (from 1–3 μg/kg/min in prevention or treatment of thrombotic events in HIT to up to 25 μg/kg/min in PCI in HIT patients), argatroban exhibits linear pharmacokinetic behavior, and steady state levels are attained within 1 hour after the start of an infusion. The elimination half-life of argatroban in healthy subjects is about 45 minutes, with a corresponding decline in its anticoagulant effects which reach their pretreatment level within 2–4 hours after cessation of an infusion. Argatroban lacks major drug–drug interactions with CYP3A4/5 inhibitors such as erythromycin or with acetaminophen, warfarin, and digoxin. However, in patients with hepatic impairment, area under the concentration versus time curve (AUC), maximum concentration, and half-life of argatroban were increased approximately 2- to 3-fold, and clearance was one-fourth that of healthy volunteers. The increase in plasma concentrations in these patients coincided with increased pharmacodynamic effects^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	MDA-231 breast cancer cells
	濃度	0.1-1 μM
	反応時間	4 h
	実験の流れ	Tissue factor (TF) activity was measured as factor X (FX) activation by the factor VIIa (FVIIa)/TF complex on MDA-231 cells. MDA-231 cells were starved in serum-free medium for 24 h, following incubation with FBS for 24 h (24-well plate, 2.0 × 10⁵ cells/well). After starvation, MDA-231 cells were treated with thrombin (0.1-10 U/ml) in presence or absence of argatroban (0.1-1 μM) for 4 h.
動物実験	動物モデル	Mice that were injected with MDA-231 breast cancer cells into the left heart ventricle
	投薬量	9 mg/kg/day
	投与方法	i.p.

参考

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：

Tissue factor-induced fibrinogenesis mediates cancer cell clustering and multiclonal peritoneal metastasis [ Cancer Lett, 2023, 553:215983]	PubMed: 36404569
Thrombin inhibitor argatroban modulates bone marrow stromal cells behaviors and promotes osteogenesis through canonical Wnt signaling [ Life Sci, 2021, 269:119073]	PubMed: 33460666

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。

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