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Biochem/physiol Actions
Inverse agonist of PPARγ that promoted osteogenic differentiation of isolated bone marrow-derived mesenchymal stem cells
SR2595 is an inverse agonist of PPARG (PPARγ) with an IC50 value of 30 nM. It was found to promote osteogenic differentiation of isolated bone marrow-derived mesenchymal stem cells accompanied by increased expression of bone morphogenetic proteins BMP2 and BMP6. SR2595 showed good pharmacokinetics and can be administered orally. It caused no significant change in insulin sensitivity, fasting insulin levels, food consumption or body weight when administered orally to mice.
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to faint brown |
| solubility | DMSO: 2 mg/mL, clear |
| shipped in | wet ice |
| storage temp. | −20°C |
| SMILES string | O=C(C(C=C1)=CC2=C1N(C(C)=C2C)CC(C=C3)=CC=C3C4=C(C(O)=O)C=CC=C4)N[C@H](C(C=C5)=CC=C5C(C)(C)C)C |
| InChI | 1S/C37H38N2O3/c1-23-25(3)39(22-26-11-13-28(14-12-26)31-9-7-8-10-32(31)36(41)42)34-20-17-29(21-33(23)34)35(40)38-24(2)27-15-18-30(19-16-27)37(4,5)6/h7-21,24H,22H2,1-6H3,(H,38,40)(H,41,42)/t24-/m0/s1 |
| InChI key | WKDKAVKAQXVFJV-DEOSSOPVSA-N |
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