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.
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- Purity : 99.3%
- CAS No.: 1196045-28-9
- 화학식: C28H26F3N3O3
- 분자량:509.52
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
제품 설명
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
|
|---|---|---|---|---|
| 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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분자량 509.52
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
순도&문서
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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)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)