AMG131
CAS No. : 315224-26-1
(Synonyms: INT131)
| Size | Price | Stock |
|---|---|---|
| 5mg | $90 | In-stock |
| 10mg | $150 | In-stock |
| 25mg | $320 | In-stock |
| 50mg | $520 | In-stock |
| 100mg | $830 | In-stock |
| 200 mg | Get quote | |
| 500 mg | Get quote | |
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| Cat. No. : | HY-117103 |
| M.Wt: | 514.21 |
| Formula: | C21H12Cl4N2O3S |
| Purity: | >98 % |
| Solubility: | DMSO : 250 mg/mL (ultrasonic) |
AMG131 (INT131) is a potent non-thiazolidinedione (TZD) selective peroxisome proliferator-activated receptor γ modulator (SPPARM). AMG131 binds to PPARγ within the same binding pocket as the TZDs, but occupies a unique space in the pocket and contacts the receptor at distinct points from the TZDs. AMG131 is promising for research of type-2 diabetes mellitus[1][2][3]. IC50 & Target:Ki: ~10 nM (PPARγ)[1][2] 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]
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