Orniplabin
Orniplabin (SMTP-7) is a plasminogen modulator with a human EC50 of 65 μM. Orniplabin enhances activation of plasminogen by plasminogen activators and increases fibrin-binding of plasminogen. Orniplabin elevates plasma levels of plasmin-α2-antiplasmin complex in vivo. Orniplabin can be used for the research of pulmonary embolism, thrombotic stroke.
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- No. CAS: 733805-92-0
- Fòrmula: C51H68N2O10
- Peso molecular:869.09
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Almacenamiento:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
Descripciòn
In Vitro
Orniplabin (65-100 μM) potently enhances u-PA-catalyzed activation of purified human plasminogen with an EC10 of 65 μM and a maximal 102-fold enhancement, increasing catalytic turnover by modifying plasminogen[1].
Orniplabin (100 μM; 30 min) enhances u-PA-catalyzed conversion of purified human plasminogen to active two-chain plasmin[1].
Orniplabin (120 μM) induces a conformational change in purified human plasminogen, as shown by a reduced elution time in size-exclusion chromatography[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Orniplabin (5 mg/kg; i.v.; bolus injection; administered ~20 minutes post-embolization) enhances thrombus clearance ~3-fold in a rat pulmonary embolism model, and further increases clearance when combined with scu-PA[1].
Orniplabin (5-30 mg/kg; i.v.; bolus injection) does not increase bleeding risk in healthy male ICR mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR (male, 7 weeks of age)[1]
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Dosage:5 mg/kg; 10 mg/kg
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Administration:i.v.; bolus injection
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Result:Elevated plasma Pm-AP levels ~1.5-fold relative to saline-treated controls.
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Animal Model:Wistar (male, ~120 g)[1]
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Dosage:5 mg/kg (alone); 5 mg/kg (with scu-PA)
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Administration:i.v.; bolus injection; administered ~20 minutes post-embolization
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Result:Increased the clot clearance rate to 19.8% per 20 minutes, a ~3-fold increase relative to the spontaneous clearance rate of 6.4% per 20 minutes observed in saline-treated controls.
Increased the clot clearance rate to 42.3% per 20 minutes when combined with scu-PA.
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Animal Model:ICR (male, 6 weeks of age)[1]
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Dosage:5 mg/kg; 30 mg/kg
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Administration:i.v.; bolus injection
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Result:Did not cause a statistically significant prolongation of bleeding time relative to controls.
Did not cause a statistically significant increase in bleeding volume relative to controls.
Chemical Information
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No. CAS 733805-92-0
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Appearance Solid
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Peso molecular 869.09
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Fòrmula C51H68N2O10
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Color White to off-white
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SMILES
O=C1C2=C(C3=C(C[C@H](O)[C@@](CC/C=C(C)/CC/C=C(C)/C)(C)O3)C(O)=C2)CN1[C@H](C(O)=O)CCCN4CC5=C(C=C(O)C6=C5O[C@](CC/C=C(C)/CC/C=C(C)/C)(C)[C@@H](O)C6)C4=O
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Synonyms
SMTP-7
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Pureza y Documentación
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Ficha de datos (286 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Orniplabin Related Classifications
HY-122311 Related Classifications
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