ASP7657 free base
Based on 1 Customer Validation
ASP7657 free base is an orally active EP4 receptor antagonist, with Kis of 2.21 and 6.02 nM for the human and rat EP4 receptors.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.3%
- CAS. Nr.: 1196045-28-9
- Formel: C28H26F3N3O3
- Molecular Weight:509.52
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
hEP4 2.21 nM (IC50) |
rat EP4 6.02 nM (IC50) |
In Vitro
ASP7657 free base inhibits the PGE2-induced cAMP increase in CHO cells (expressing rat EP4 receptors) and human lymphoblastoid T cells, with IC50 values of 0.86 nM and 0.29 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
ASP7657 free base (0.003-0.1 mg/kg, p.o.) inhibits LPS (1 μg/mL)-induced TNF-α release from rat whole blood[1].
ASP7657 free base (0.01 mg/kg, p.o.) attenuates urinary albumin excretion in type 2 diabetic mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:LPS (1 μg/mL)-induced rats[1]
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Dosage:0.003, 0.01, 0.03, 0.1 mg/kg
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Administration:p.o.
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Result:Antagonized the PGE2-mediated inhibition of LPS-induced TNF-α release from rat whole blood culture, in a dose-dependent way.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1196045-28-9
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Appearance Solid
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Molecular Weight 509.52
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Formel C28H26F3N3O3
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Color White to off-white
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SMILES
O=C([C@H]1CC[C@H](CNC(C2=CC(C(F)(F)F)=CC3=C2N(CC4=NC5=CC=CC=C5C=C4)C=C3)=O)CC1)O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Reinheit & Dokumentation
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Data Sheet (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
ASP7657 free base Related Classifications
HY-120598 Related Classifications
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