BMS 195614 (Synonyms:BMS 195614/BMS 614)
目录号 : KCM12108 CAS No. : 182135-66-6 纯度 : ≥98%
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.
规格 价格 是否有货 数量
1mg
In-stock
5mg
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10mg
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25mg
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10 mM * 1 mL in DMSO
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生物活性

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.

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)

配制储备液
                                           
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
                                                                                                                    
1 mM 2.2296 mL 11.1480 mL 22.2960 mL
5 mM 0.4459 mL 2.2296 mL 4.4592 mL
10 mM 0.2230 mL 1.1148 mL 2.2296 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

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