AMG131
Modify Date: 2024-01-14 16:41:28
AMG131 structure
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Common Name | AMG131 | ||
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| CAS Number | 315224-26-1 | Molecular Weight | 514.21 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C21H12Cl4N2O3S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of AMG131AMG131 (INT131), a potent and highly selective PPARγ partial agonist, binds to PPARγ and displaces Rosiglitazone with a Ki of ~10 nM. AMG131 can be used for research of type-2 diabetes mellitus (T2DM)[1][2]. |
| Name | N-(3,5-dichloro-4-quinolin-3-yloxyphenyl)-2,4-dihydroxybenzenesulfonamide |
|---|---|
| Synonym | More Synonyms |
| Description | AMG131 (INT131), a potent and highly selective PPARγ partial agonist, binds to PPARγ and displaces Rosiglitazone with a Ki of ~10 nM. AMG131 can be used for research of type-2 diabetes mellitus (T2DM)[1][2]. |
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| Related Catalog | |
| Target |
PPARγ |
| In Vitro | AMG131 (INT131) binds to PPARγ and displaces Rosiglitazone with a Ki of ~10 nM, demonstrating ~20-fold higher affinity than either Rosiglitazone or Pioglitazone, and with greater than 1000-fold selectivity for PPARγ over PPARα, PPARδ, or a set of other nuclear receptors. AMG131 is highly selective for PPARγ, with no binding to PPARα or δ at 10 μM, 1000 fold over the Ki for PPARγ[1]. |
| In Vivo | AMG131 (INT131; 80 mg/kg; 14-day oral treatment) increases in glucose tolerance in Zucker (fa/fa) rats following[2] Animal Model: Male Zucker fatty (fa/fa) rats ages 7-8 weeks[2] Dosage: 80 mg/kg Administration: Administered once daily by oral gavage for 14 days Result: Exhibited maximal efficacy comparable to that of Rosiglitazone with respect to plasma glucose clearance in an oral glucose tolerance test. Reduced baseline insulin levels, similar to Rosiglitazone, could improve insulin sensitivity in treated animals. |
| References |
| Molecular Formula | C21H12Cl4N2O3S |
|---|---|
| Molecular Weight | 514.21 |
| Exact Mass | 476.00000 |
| PSA | 117.13000 |
| LogP | 6.69970 |
| Storage condition | -20°C |
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AMG131 CAS#:315224-26-1 |
| Literature: WO2005/33074 A2, ; Page/Page column 33 ; WO 2005/033074 A2 |
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AMG131 CAS#:315224-26-1 |
| Literature: Bioorganic and Medicinal Chemistry, , vol. 21, # 4 p. 979 - 992 |
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AMG131 CAS#:315224-26-1 |
| Literature: Bioorganic and Medicinal Chemistry, , vol. 21, # 4 p. 979 - 992 |
| UNII-E7ILQ6U50J |
| AMG131 |
| T-131 cpd |
| INT-131 |
| T-131 |