CD2665 is an orally active and selective RAR-β,γ antagonist, with Kd values of 306 nM, 110 nM for RAR-β and RAR-γ, repectively.
性状
Solid
IC50 & Target[1][2]
Ki: 110 nM (RARγ), 306 nM (RARβ)
体外研究(In Vitro)
CD2665 (100 nM; 9 days; 3T3 cells) has significant effects on cell growth and differentiation.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay
Cell Line:
3T3 cells
Concentration:
100 nM
Incubation Time:
9 days
Result:
Abrogated the antiprolferative effects of ATRA , CD271 (adapalene, an RAR-β,γ agonist), and CD2043 (RAR-α,β,γ pan-agonist) returning cell numbers and percent LFCS to control level.
体内研究(In Vivo)
CD2665 (0.6 mg/kg; Subcutaneous injection; daily, for 22 days) completely inhibits the overexpression of RARβ mRNA in the brain of alcohol treated mice.
CD2665 is a selective retinoid antagonist and elicits the expected maturation delay and growth plate expansion.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Mice submitted to 10 months of ethanol consumption.
Dosage:
0.6 mg/kg
Administration:
Subcutaneous injection; daily, for 22 days.
Result:
Decreased brain RARβ mRNA levels (50% relative to control), without any change in RXR β/γ mRNA levels.
Animal Model:
Male and female mice (3 weeks).
Dosage:
1.6 mg/kg
Administration:
Oral gavage/intragastric; daily, for 31 days.
Result:
Growth plate closure had largely been prevented in LDE225/antagonist co-treated mice compared with those receiving LDE225 only.