1196045-28-9
1196045-28-9 structure
- Name: ASP7657
- Chemical Name: ASP7657
- CAS Number: 1196045-28-9
- Molecular Formula: C28H26F3N3O3
- Molecular Weight: 509.529
- Catalog: Signaling Pathways GPCR/G Protein Prostaglandin Receptor
- Create Date: 2020-01-12 09:09:50
- Modify Date: 2024-04-03 22:51:43
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ASP7657 (ASP-7657) is a potent, selective, orally active prostaglandin EP4 receptor antagonist with Ki values of 6.02 nM and 2.21 nM for rat and human EP4 receptors, resepctively; potently inhibits the PGE2-induced cAMP increase in CHO cells expressing rat EP4 receptors and human lymphoblastoid T (Jurkat) cells, with IC50 values of 0.86 nM and 0.29 nM, respectively; does not inhibit the PGE2-induced intracellular calcium increase in HEK293 cells expressing rat EP1 and EP3 receptors, or cAMP increase in CHO cells expressing rat EP2 receptors; dose-dependently inhibits the PGE2-mediated inhibition of LPS-induced TNF-α release from rat whole blood culture, attenuates albuminuria in type 2 diabetic mice at dose of 0.1 mg/kg. Diabetes Phase 1 Discontinued
| Name | ASP7657 |
|---|
| Description | ASP7657 (ASP-7657) is a potent, selective, orally active prostaglandin EP4 receptor antagonist with Ki values of 6.02 nM and 2.21 nM for rat and human EP4 receptors, resepctively; potently inhibits the PGE2-induced cAMP increase in CHO cells expressing rat EP4 receptors and human lymphoblastoid T (Jurkat) cells, with IC50 values of 0.86 nM and 0.29 nM, respectively; does not inhibit the PGE2-induced intracellular calcium increase in HEK293 cells expressing rat EP1 and EP3 receptors, or cAMP increase in CHO cells expressing rat EP2 receptors; dose-dependently inhibits the PGE2-mediated inhibition of LPS-induced TNF-α release from rat whole blood culture, attenuates albuminuria in type 2 diabetic mice at dose of 0.1 mg/kg. Diabetes Phase 1 Discontinued |
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| References | References 1. Mizukami K, et al. Naunyn Schmiedebergs Arch Pharmacol. 2018 Aug 3. doi: 10.1007/s00210-018-1545-x. View Related Products by Target Prostaglandin Receptor Diabetes |
| Molecular Formula | C28H26F3N3O3 |
|---|---|
| Molecular Weight | 509.529 |