DL5055 is a Potent and Selective CAR activator ( Constitutive Androstane Receptor Activator). DL5055 Facilitates Cyclophosphamide-Based Chemotherapies. DL5055 activates hCAR with an EC50 of 0.35 μM and EMAX of 4.3, and does not activate hPXR and other related nuclear receptors. It induced the expression of CYP2B6 and caused the translocation of hCAR from the cytoplasm to the nucleus in human primary hepatocytes. DL5055 also induces the expression of Cyp2b10 (the mouse analog of human CYP2B6) in hCAR-transgenic mice. In addition, it significantly enhances the efficacy of CPA-based chemotherapy regimen, CHOP, in a coculture system and a mouse xenograft model in vivo.
MedKoo Cat#: 128697
Name: DL5055
CAS#: N/A
Chemical Formula: C25H19N3O2
Exact Mass: 393.1477
Molecular Weight: 393.45
Elemental Analysis: C, 76.32; H, 4.87; N, 10.68; O, 8.13
The following data is based on the product molecular weight 393.45 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
