产品介绍
Product Description
Application
TAK-475 has been used:
- as a farnesyl-diphosphate farnesyltransferase 1 (FDFT1) inhibitor to study its effects on cell signaling in pancreatic ductal adenocarcinoma cells
- as a squalene synthase (SQS) inhibitor to stabilize HMG-CoA reductase (HMGCR)-dCat-ELuc proteins
- as an SQS inhibitor to study its effects on the migration of prostate cancer cells
Biochem/physiol Actions
Squalene synthase inhibitor
TAK-475 (Lapaquistat acetate) is a potent and selective squalene synthase inhibitor. TAK-475 effectively lowers low-density lipoprotein cholesterol in human. Clinical development of TAK-475 was discontinued due to hepatotoxicity seen in two patients receiving a high dose.
技术参数
Specifications
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | −20°C |
| SMILES string | O=C1[C@@H](CC(N2CCC(CC(O)=O)CC2)=O)O[C@H](C3=CC=CC(OC)=C3OC)C4=C(C=CC(Cl)=C4)N1CC(C)(C)COC(C)=O |
| InChI | 1S/C33H41ClN2O9/c1-20(37)44-19-33(2,3)18-36-25-10-9-22(34)16-24(25)30(23-7-6-8-26(42-4)31(23)43-5)45-27(32(36)41)17-28(38)35-13-11-21(12-14-35)15-29(39)40/h6-10,16,21,27,30H,11-15,17-19H2,1-5H3,(H,39,40)/t27-,30-/m1/s1 |
| InChI key | CMLUGNQVANVZHY-POURPWNDSA-N |
