Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
Atopaxar, formerly known as E5555, is a potent and orally -active PAR-1 inhibitor. E5555 inhibited the binding of a high-affinity thrombin receptor-activating peptide ([(3)H]haTRAP) to PAR-1 with a half maximal inhibitory concentration (IC(50)) value of 0.019μM. E5555 demonstrated strong inhibitory effects with IC(50) values of 0.064 and 0.031μM, respectively, on human platelet aggregation induced by thrombin and TRAP. With IC(50) values of 0.13 and 0.097μM, respectively, E5555 demonstrated strong and specific inhibitory effects on guinea pig platelet aggregation induced by thrombin and TRAP. E5555 may be used as a treatment for atherothrombotic illness.
Targets |
PAR1
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ln Vitro |
Atopaxar (0.0001-10 μM; 1h) inhibits the binding of haTRAP (high-affinity agonist capture activating peptide) to PAR-1 on the human distal membrane in a concentration suspension manner, with an IC50 of 0.019 μM[2]. Atopaxar does not induce PRP (Rich Wheel) aggregation through ADP, U46619, collagen and PAR-4ap at concentrations up to 20 μM [2].
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ln Vivo |
Atopaxar (30-100 mg/kg; wall) causes dose-induced prolongation of femoral artery occlusion time in a guinea pig model of photochemically induced thrombosis (PIT) [2]. At the highest dose tested, 1000 mg/kg, Atopaxar did not. Animal Model: Guinea pig, PIT model [2] Dosage: Oral Administration: 10 mg/kg, 30 mg/kg, 100 mg/kg Results: Prolonged occlusion time 1.8 -1-fold and 2.4-fold increases at doses of 30 mg/kg and 100 mg/kg, respectively, compared to the control group.
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Animal Protocol |
Guinea pigs, PIT model
Oral administration 10 mg/kg, 30 mg/kg, 100 mg/kg |
References |
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Molecular Formula |
C29H38FN3O5
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Molecular Weight |
527.6374
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Exact Mass |
527.28
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Elemental Analysis |
C, 66.01; H, 7.26; F, 3.60; N, 7.96; O, 15.16
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CAS # |
751475-53-3
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Related CAS # |
Atopaxar hydrobromide; 474550-69-1
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Appearance |
Solid powder
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SMILES |
CCOC1=C(C(=C2C(=C1)CN(C2=N)CC(=O)C3=CC(=C(C(=C3)N4CCOCC4)OC)C(C)(C)C)F)OCC
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InChi Key |
QWKAUGRRIXBIPO-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C29H38FN3O5/c1-7-37-23-15-19-16-33(28(31)24(19)25(30)27(23)38-8-2)17-22(34)18-13-20(29(3,4)5)26(35-6)21(14-18)32-9-11-36-12-10-32/h13-15,31H,7-12,16-17H2,1-6H3
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Chemical Name |
1-(3-tert-butyl-4-methoxy-5-morpholin-4-ylphenyl)-2-(5,6-diethoxy-4-fluoro-3-imino-1H-isoindol-2-yl)ethanone
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Synonyms |
ER-172594-00; ER172594-00; ER 172594-00; E5555; E-5555; E 5555; Atopaxar
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HS Tariff Code |
2934.99.9001
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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)
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Solubility (In Vitro) |
DMSO: ~50 mg/mL (~94.8 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.94 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.94 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 2 mg/mL (3.79 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.8952 mL | 9.4762 mL | 18.9523 mL | |
5 mM | 0.3790 mL | 1.8952 mL | 3.7905 mL | |
10 mM | 0.1895 mL | 0.9476 mL | 1.8952 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.
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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT00540670 | Completed | Drug: Placebo Drug: E5555 50 mg |
Coronary Artery Disease | Eisai Co., Ltd. | October 2007 | Phase 2 |
NCT00619164 | Completed | Drug: E5555 Drug: Placebo |
Acute Coronary Syndrome | Eisai Co., Ltd. | November 2007 | Phase 2 |
NCT00548587 | Completed | Drug: E5555 Drug: Placebo |
Acute Coronary Syndrome | Eisai Inc. | October 2007 | Phase 2 |
NCT00312052 | Completed | Drug: E5555 Drug: Placebo |
Coronary Artery Disease | Eisai Inc. | September 2007 | Phase 2 |
NCT01241669 | Completed | Drug: E5555 | Healthy Subjects | Eisai Inc. | October 2010 | Phase 1 |