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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.3%
- CAS No.: 1196045-28-9
- Formule: C28H26F3N3O3
- Masse moléculaire:509.52
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
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.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1196045-28-9
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Appearance Solid
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Masse moléculaire 509.52
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Pureté et documentation
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Fiche technique (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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Instruction de manipulation (2659 KB)
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ASP7657 free base Related Classifications
HY-120598 Related Classifications
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