CD2665 是一种能口服的选择性RAR-β,γ拮抗剂，对 RAR-β 和 RAR-γ 作用的Kd值分别为 306 nM，110 nM。CD2665 与 RAR-α 处无结合。
| 生物活性 | CD2665 is an orally active and selectiveRAR-β,γantagonist, withKdvalues of 306 nM, 110 nM for RAR-β and RAR-γ, repectively[1][3]. |
| IC50& Target | Ki: 110 nM (RARγ), 306 nM (RARβ)[1] |
体外研究
(In Vitro) | CD2665 (100 nM; 9 days; 3T3 cells) has significant effects on cell growth and differentiation[1].
Cell Proliferation Assay[1] | 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. |
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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[2].
CD2665 is a selective retinoid antagonist and elicits the expected maturation delay and growth plate expansion[3].
| Animal Model: | Mice submitted to 10 months of ethanol consumption[2]. | | 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)[3]. | | 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. |
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| 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 |
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