Argatroban (MD805; MCI9038; Argipidine)

Alias: MD 805; MD-805; MCI9038; MCI-9038; MCI9038; MD805; DK-7419; DK 7419; DK7419; GN-1600; GN1600;GN 1600; MPQA; MMTQAP; Novastan; Argipidine; OM 805; Slonnon
Cat No.:V1851 Purity: ≥98%
Argatroban (MD-805; MCI-9038; Argipidine)is a potent and selective synthetic thrombin inhibitor with Ki ranging from 5 nM to 39 nM.
Argatroban (MD805; MCI9038; Argipidine) Chemical Structure CAS No.: 74863-84-6
Product category: Thrombin
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
250mg
500mg
Other Sizes

Other Forms of Argatroban (MD805; MCI9038; Argipidine):

  • Argatroban hydrate (MD805; MCI9038; Argipidine)
  • Argatroban-d3 (Argatroban-d3)
Official Supplier of:
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Alternate Text
Top Publications Citing lnvivochem Products
Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Argatroban (MD-805; MCI-9038; Argipidine) is a potent and selective synthetic thrombin inhibitor with Ki ranging from 5 nM to 39 nM. Argatroban is a thrombin inhibitor that is used as an anticoagulant. In 2000, the FDA approved argatroban for the prevention or treatment of thrombosis in patients suffering from heparin-induced thrombocytopenia (HIT). Argatroban binds to the thrombin active site reversibly and functions as a direct thrombin inhibitor. Argatroban inhibits thrombin-catalyzed or -induced reactions, such as fibrin formation, the activation of coagulation factors V, VIII, and XIII, the activation of protein C, and platelet aggregation, to produce its anticoagulant effects.

Biological Activity I Assay Protocols (From Reference)
Targets
Thrombin (Ki = 5-39 nM)
ln Vitro
Argatroban is a potent and selective synthetic thrombin inhibitor with Ki values against thrombin ranging from 5 nM to 39 nM. In numerous animal models of thrombosis that is both platelet-rich and erythrocyte-rich, argatroban exhibits antithrombotic characteristics. Argatroban inhibits thrombus formation in a dose-dependent manner; in this test, its estimated ED50 was 125 μg/kg. Argatroban increases thrombin time in a dose-dependent manner; at the highest dose used, this increase was 511%, but the APTT increased only by 73%.[1] Argatroban has the ability to directly cause vascular smooth muscle cells to change phenotype, which leads to an increase in the mRNAs for SMemb, PAI-1, and beta-actin.[2]
ln Vivo
Argatroban prevents the growth of microthrombi for three hours following middle cerebral artery (MCA) occlusion; after that, it has no further effect. Six hours following MCA occlusion, argatroban also significantly reduces the size of ischemic cerebral lesions. In [3] In the rat model of distal middle cerebral artery occlusion, argatroban (0.3 mg/h/rat) significantly reduces the number of microthrombi 1 day after distal middle cerebral artery (dMCA) occlusion. One day after distal middle cerebral artery (dMCA) occlusion, a reduction in regional cerebral blood flow (rCBF) is significantly reversed by argatroban (0.1 and 0.3 mg/h/rat). Argatroban (0.3 mg/h/rat) also greatly diminishes the cerebral infarction's size.[4]
Animal Protocol


References

[1]. Br J Pharmacol . 1994 Dec;113(4):1209-14.

[2]. Eur J Pharmacol . 2003 Feb 7;461(1):9-17.

[3]. Jpn J Pharmacol . 1995 Oct;69(2):143-8.

[4]. J Pharmacol Exp Ther . 1996 Aug;278(2):780-5.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C23H36N6O5S
Molecular Weight
508.63
Exact Mass
508.2468
Elemental Analysis
C, 54.31; H, 7.13; N, 16.52; O, 15.73; S, 6.30
CAS #
74863-84-6
Appearance
Solid powder
SMILES
C[C@@H]1CCN([C@H](C1)C(=O)O)C(=O)[C@H](CCCN=C(N)N)NS(=O)(=O)C2=CC=CC3=C2NCC(C3)C
InChi Key
KXNPVXPOPUZYGB-IOVMHBDKSA-N
InChi Code
InChI=1S/C23H36N6O5S/c1-14-8-10-29(18(12-14)22(31)32)21(30)17(6-4-9-26-23(24)25)28-35(33,34)19-7-3-5-16-11-15(2)13-27-20(16)19/h3,5,7,14-15,17-18,27-28H,4,6,8-13H2,1-2H3,(H,31,32)(H4,24,25,26)/t14-,15?,17+,18-/m1/s1
Chemical Name
(2R,4R)-1-[(2S)-5-(diaminomethylideneamino)-2-[(3-methyl-1,2,3,4-tetrahydroquinolin-8-yl)sulfonylamino]pentanoyl]-4-methylpiperidine-2-carboxylic acid
Synonyms
MD 805; MD-805; MCI9038; MCI-9038; MCI9038; MD805; DK-7419; DK 7419; DK7419; GN-1600; GN1600;GN 1600; MPQA; MMTQAP; Novastan; Argipidine; OM 805; Slonnon
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~9 mg/mL (~17.7 mM)
Water: <1 mg/mL
Ethanol: ~6 mg/mL (~11.8 mM)
Solubility (In Vivo)
2% DMSO+40% PEG 300+2% Tween 80+ddH2O: 5mg/mL (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.9661 mL 9.8303 mL 19.6607 mL
5 mM 0.3932 mL 1.9661 mL 3.9321 mL
10 mM 0.1966 mL 0.9830 mL 1.9661 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
/

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
+
+
+

Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05226442 Recruiting Drug: Unfractionated heparin
Drug: Argatroban
Extracorporeal Membrane
Oxygenation Complication
Anticoagulants and Bleeding
Disorders
Medical University of Vienna December 1, 2021 Phase 2
Phase 3
NCT04925167 Recruiting Drug: unfractionated heparin
Drug: Argatroban
Respiratory Failure Beijing Chao Yang Hospital July 6, 2021 Not Applicable
NCT03735979 Active
Recruiting
Drug: Argatroban
Drug: Eptifibatide
Acute Ischemic Stroke Washington University School of
Medicine
October 15, 2019 Phase 3
NCT00039858 Completed Drug: Argatroban Thrombocytopenia
Thrombosis
Encysive Pharmaceuticals September 2003 Phase 4
NCT05325346 Completed Drug: VLX-1005
Drug: Argatroban
Heparin-induced Thrombocytopenia Veralox Therapeutics March 7, 2022 Phase 1
Contact Us