| CAS NO: | 74863-84-6 |
| 规格: | ≥98% |
| 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 |
| Molecular Weight (MW) | 508.63 |
|---|---|
| Formula | C23H36N6O5S |
| 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 |
| Synonyms | MD-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. |
| 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 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. 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. |
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