BMS-986141
Based on 1 Customer Validation
BMS-98614 is an orally active, selective thrombin receptor protease-activated receptor-4 (PAR-4) antagonist with an IC50 value of 0.4 nM. BMS-98614 has excellent antithrombotic effect.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.15%
- No. CAS: 1478711-48-6
- Fòrmula: C27H23N5O5S2
- Peso molecular:561.63
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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PAR4 .4 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Platelet | IC50 |
>1000 nM
Compound: 49; BMS-986141
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Antiplatelet activity against collagen agonist peptide-induced human platelet assessed as inhibition of platelet aggregation
Antiplatelet activity against collagen agonist peptide-induced human platelet assessed as inhibition of platelet aggregation
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[PMID: 35729784] |
| Platelet | IC50 |
>1000 nM
Compound: 49; BMS-986141
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Antiplatelet activity against PAR1 agonist peptide-induced human platelet assessed as inhibition of platelet aggregation
Antiplatelet activity against PAR1 agonist peptide-induced human platelet assessed as inhibition of platelet aggregation
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[PMID: 35729784] |
| Platelet | IC50 |
>1000 nM
Compound: 49; BMS-986141
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Antiplatelet activity against U46619 agonist peptide-induced human platelet assessed as inhibition of platelet aggregation
Antiplatelet activity against U46619 agonist peptide-induced human platelet assessed as inhibition of platelet aggregation
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[PMID: 35729784] |
| Platelet | IC50 |
2.1 nM
Compound: 49; BMS-986141
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Antiplatelet activity in human platelet-rich plasma assessed as inhibition of gamma thrombin induced platelet aggregation preincubated for 5 mins followed by gamma thrombin addition and measured upto 15 mins by plate reader assay
Antiplatelet activity in human platelet-rich plasma assessed as inhibition of gamma thrombin induced platelet aggregation preincubated for 5 mins followed by gamma thrombin addition and measured upto 15 mins by plate reader assay
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[PMID: 35729784] |
| Platelet | IC50 |
2.2 nM
Compound: 49; BMS-986141
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Antiplatelet activity against PAR4 agonist peptide-induced human platelet assessed as inhibition of platelet aggregation
Antiplatelet activity against PAR4 agonist peptide-induced human platelet assessed as inhibition of platelet aggregation
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[PMID: 35729784] |
| Platelet | IC50 |
>1000 nM
Compound: 49; BMS-986141
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Antiplatelet activity against ADP agonist peptide-induced human platelet assessed as inhibition of platelet aggregation
Antiplatelet activity against ADP agonist peptide-induced human platelet assessed as inhibition of platelet aggregation
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[PMID: 35729784] |
BMS-986141 (compound 49) (0-1 μM) inhibits platelet aggregation induced by PAR4 agonist peptide with an IC50 value of 2.2 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Monkey arterial thrombosis (AT) and mesenteric bleeding time (MBT) models[2]
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Dosage:0.05, 0.1, 0.5 mg/kg
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Administration:p.o., 2 hours
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Result:Inhibited PAR4-AP-induced platelet aggregation in human and monkey blood with IC50 of 1.8 and 1.3 nM, respectively.
Reduced the thrombus weight by 36%, 63% and 88% at concentrations of 0.05, 0.1 and 0.5 mg/kg, respectively in AT model.
Increased MBT by 1.2 times.
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Animal Model:Rat, dog and monkey[1]
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Dosage:0.5, 1, 2 mpk
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Administration:i.v., 0.5 mpk, 10 min or p.o., 2 mpk for rat, 1 mpk for dog and monkey
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Result:The pharmacokinetic parameters of BMS-986141 (compound 49)
Parameters rat dog monkey t1/2(h) 3.7 ± 0.4 13 75 ± 12 CL (mL/min/kg) 14.3 ± 0.4 8.5 12 ± 2 Vss(L/kg) 2.7 ± 0.3 2.7 14 ± 5 F (%) 31 25 36
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1478711-48-6
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Appearance Solid
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Peso molecular 561.63
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Fòrmula C27H23N5O5S2
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Color White to off-white
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SMILES
O=C(N(C)C)C1=CC=C(C2=NC(COC3=C4C=C(C5=CN6C(SC(OC)=N6)=N5)OC4=CC(OC)=C3)=CS2)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMF : 8.33 mg/mL (14.83 mM; ultrasonic and warming and heat to 60°C)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMF | 1 mM | 1.7805 mL | 8.9027 mL | 17.8053 mL | 44.5133 mL |
| 5 mM | 0.3561 mL | 1.7805 mL | 3.5611 mL | 8.9027 mL | |
| 10 mM | 0.1781 mL | 0.8903 mL | 1.7805 mL | 4.4513 mL |
BMS-986141 Related Classifications
HY-150790 Related Classifications
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