2. GPCR/G Protein
  3. Prostaglandin Receptor
  4. ASP7657 free base

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.

For research use only. We do not sell to patients.

ASP7657 free base Chemical Structure

ASP7657 free base Chemical Structure

CAS No. : 1196045-28-9

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Based on 1 publication(s) in Google Scholar

ASP7657 free base Related Antibodies

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Description

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[1].

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.

ASP7657 free base Related Antibodies
In Vivo

ASP7657 free base (0.1 mg/kg, p.o., rats) shows a t1/2 of 1.38 h, Cmax of 22.4 ng/mL, and oral bioavailability of 46.2%[1].
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.

Animal Model: LPS (1 μg/mL)-induced rats[1]
Dosage: 0.003, 0.01, 0.03, 0.1 mg/kg
Administration: p.o.
Result: Antagonized the PGE2-mediated inhibition of LPS-induced TNF-α release from rat whole blood culture, in a dose-dependent way.
Clinical Trial
Molecular Weight

509.52

Formula

C28H26F3N3O3
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ASP7657 free base Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ASP76571196045-28-9ASP 7657ASP-7657Prostaglandin ReceptorTNF-αLPSPGE2type 2 diabetesprostaglandinInhibitorinhibitorinhibit

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