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Trifarotene (CD5789) 是一种有效的选择性 RARγ 激动剂,对 RARγ 的选择性是 RARα 和 RARβ 的 65 倍和 16 倍,EC50分别为7.7、500和125 nM。
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Trifarotene (CD5789) 是一种有效的选择性 RARγ 激动剂,对 RARγ 的选择性是 RARα 和 RARβ 的 65 倍和 16 倍,EC50分别为7.7、500和125 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 158 | 现货 | |
5 mg | ¥ 358 | 现货 | |
10 mg | ¥ 596 | 现货 | |
25 mg | ¥ 990 | 现货 | |
50 mg | ¥ 1,780 | 现货 | |
100 mg | ¥ 2,980 | 现货 | |
200 mg | ¥ 4,230 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 353 | 现货 |
产品描述 | Trifarotene (CD5789) is a potent and selective RARγ agonist with 65-fold and 16-fold selectivitiy for the RARγ (EC50=7.7 nM) over RARα (EC50=500 nM) and RARβ (EC50=125 nM). |
靶点活性 | RARβ:125 nM (EC50), RARγ:7.7 nM (EC50), RARα:500 nM (EC50) |
体外活性 | Administration of trifarotene involves in keratinization, desquamation, cornification and cell adhesion in reconstructed human epidermis (RHE) with the mean EC50 on the combined target genes of 0.0048%[2]. |
体内活性 | In rhino mice, administration of 0.001%-0.01% Trifarotene shows dose-dependent comedolytic activity. Being fully efficacious at 0.01% with reduction of 98%[2]. |
别名 | 曲法罗汀, CD5789 |
分子量 | 459.58 |
分子式 | C29H33NO4 |
CAS No. | 895542-09-3 |
Smiles | CC(C)(C)c1cc(ccc1N1CCCC1)-c1cc(ccc1OCCO)-c1ccc(cc1)C(O)=O |
密度 | 1.31g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 200 mg/mL (435.18 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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