| 产品描述: | BMS 195614是一种选择性的RARα拮抗剂。BMS 195614可以与RARα亚基结合。 |
| 靶点: |
RetinoidReceptor |
| 体外研究: |
BMS 195614 reversed the induction effect of selective RARα agonists, AM580, AM80 and BMS 194753 on differentiation of the acute promyelocytic leukemia cell lines, NB4 and HL60. Treatment with retinoic acid (RA) (1 uM) for 72 hrs significantly reduced T47D breast cancer cells migration. But RA in combination with BMS 195614 did not affect the cell movement. In cells of a bovine stromal-vascular fraction from intramuscular fat, BMS 195614 significantly diminished the anti-adipogenic effect of ATRA. |
| 体内研究: |
BMS 195614 displayed poor in vivo activity in mice when administered orally. Treatment with BMS 195614 at oral doses for 1 month showed no inhibition to spermatogenesis. Oral administration of BMS 195614 did not suppress spermatogenesis in mice. |
| 参考文献: |
1. F. Christopher Zusi, Matthew V. Lorenzi and Valerie Vivat-Hannah. Selective retinoids and rexinoids in cancer therapy and chemoprevention. Drug Discovery Today, 2002, 7(23):1165-1174. 2. Flamini Marina Ines, Gauna Gisel Valeria, Sottile Mayra Lis, et al. Retinoic acid reduces migration of human breast cancer cells: role of retinoic acid receptor β. J. Cell. Mol. Med., 2014, 18(6): 1113-1123. 3. Nikolas Gunkel, Thorsten Meyer and John Michael Graettinger; N/A. Method of Modulating the Degree of Adipose Tissue Deposited Intramuscularly. US patent 20140094512A1. 2014 Apr. 3. 4. Sanny S. W. Chung, Rebecca A. D. Cuellar, Xiangyuan Wang, et al. Pharmacological Activity of Retinoic Acid Receptor Alpha-Selective Antagonists in Vitro and in Vivo. ACS Med. Chem. Lett., 2013, 4: 446-450. 5. Fern E. Murdoch and Erwin Goldberg. Male contraception: Another holy grail. Bioorg. Med. Chem. Lett., 2014, 24:419-424. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.23 ml |
11.148 ml |
22.296 ml |
| 5 mM |
0.446 ml |
2.23 ml |
4.459 ml |
| 10 mM |
0.223 ml |
1.115 ml |
2.23 ml |
| 50 mM |
0.045 ml |
0.223 ml |
0.446 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |