阿加曲班单水合物
货号：
IA3410
品牌：
Jinpan
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产品简介
| 有效期 | 2年 |
| 描述 | 是 thrombin 选择性抑制剂。 |
| MDL | MFCD00895735 |
| 别名 | (2R,4R)-1-[(2S)-5-(氨基亚氨甲基)氨基-1-氧代-2-[(3-甲基-1,2,3,4-四氢喹啉-8-基)磺酰胺基]戊烷]-4-甲基哌啶-2-甲酸 |
| 英文名称 | Argatroban Monohydrate |
| CAS | 141396-28-3 |
| 分子式 | C23H36N6O5S·H2O |
| 分子量 | 526.65 |
| 储存条件 | -20℃ |
| 纯度 | ≥98% |
| 外观（性状） | Solid |
| 单位 | 瓶 |
| 生物活性 | Argatroban (Argatroban hydrate, Argipidine) 是一种直接的、选择性的thrombin抑制剂，具有抗凝活性。[1] |
| 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]. |
| SMILES | O=C([C@@H]1N(C([C@@H](NS(=O)(C2=CC=CC3=C2NCC(C)C3)=O)CCCNC(N)=N)=O)CC[C@@H](C)C1)O.O |
| 靶点 | Thrombin |
| 动物实验 | 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.[2] |
| 细胞实验 | Animal Models: Mice that were injected with MDA-231 breast cancer cells into the left heart ventricle; Dosages: 9 mg/kg/day; Administration: i.p.[2] |
| 数据来源文献 | [1] Andreas Koster, et al. Biologics. 2007, 1(2): 105-112. [2] Asanuma K, et al. Breast Cancer. 2013, 20(3):241-6. |
| 规格 | 5mg 10mg 25mg |