BMS 195614 is a neutral retinoic acid receptor (RAR) α-selective antagonist (K = 2.5 nM). It antagonizes agonist-induced coactivator recruitment and moderately decreases SMRT binding to RAR but does not significantly affect nuclear receptor corepressor binding.
BMS 195614 is an orally active neutral RARα-selective antagonist with a Ki of 2.5 nM. BMS 195614 restores the expression of Bcl2.BMS 195614 inhibits the transactivation of NF-κB, AP-1 and PPAR.BMS 195614 downregulates the expression of IL-6 and VEGF. BMS-195614 reduces blue light-induced phototoxicity and inhibits cell migration. BMS-195614 modulates inflammation and angiogenesis.
IC50&Target
BCL2 IL-6
体外研究
BMS 195614 (10-20 μM) can reduce blue light induced phototoxicity and regulate inflammation and angiogenesis in the presence of A2E in RPE cells.
BMS 195614 (6 μM, 24 h) can reverse the anti-inflammatory effects of Vitamin A and RA on LPS activated BV-2 cells releasing IL-6.
BMS 195614 (1 μM, 24 h) can inhibit the migration of MC3T3E1 osteoblast like cells induced by Retinoic acid.
Real Time qPCR
Cell Line:
RPE cells
Concentration:
10 µM
Incubation Time:
Result:
Inhibited NF-κB transactivation, the transactivation of AP-1, the expression of IL-6 and VEGF mRNA.
体内研究
BMS 195614 (2-10 mg/kg, orally, 7 days) showed no or only slight inhibition on overall spermatogenesis in mice.
分子式
C29H24N2O3
分子量
448.51
CAS号
182135-66-6
中文名称
BMS 195614/BMS 614
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO: 30 mg/mL (66.89 mM; Need ultrasonic and warming)