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Argatroban(MD805 MCI9038 Argipidine)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Argatroban(MD805 MCI9038 Argipidine)图片
CAS NO:74863-84-6
规格:≥98%
包装与价格:
包装价格(元)
1mg电议
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
2g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)508.63
FormulaC23H36N6O5S
CAS No.74863-84-6
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 9 mg/mL (17.7 mM)
Water: <1 mg/mL
Ethanol: 6 mg/mL (11.8 mM)
Other info

Chemical Name: (2R,4R)-4-methyl-1-(((3-methyl-1,2,3,4-tetrahydroquinolin-8-yl)sulfonyl)-L-arginyl)piperidine-2-carboxylic acid

SMILES Code: O=C(O)[C@H]1C[C@H](C)CCN1C([C@H](CCCNC(N)=N)NS(=O)(C2=CC=CC3=C2NCC(C)C3)=O)=O

Exact Mass: 508.2468

SynonymsMD-805; MD 805; MCI-9038; MCI9038; MCI9038; MD805; DK-7419; DK 7419; DK7419; GN1600; GN-1600; GN 1600; MMTQAP; MPQA; Novastan; OM 805; Slonnon; Argipidine.
实验参考方法
In Vitro

In vitro activity: 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. Argatroban can directly induce phenotype conversion of vascular smooth muscle cells with the resultant up-regulation of SMemb, PAI-1, and beta-actin mRNAs.

In VivoArgatroban 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. 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.
Animal model
Formulation & Dosage
References

Br J Pharmacol. 1994 Dec;113(4):1209-14; Jpn J Pharmacol. 1995 Oct;69(2):143-8.