DY131 (GSK 9089) 是一种有效的选择性的ERRγ和ERRβ激动剂,对 ERRα,ERα 和 ERβ 无效。DY131 还抑制Smo信号传导。
生物活性 | DY131 (GSK 9089) is a potent and selectiveERRγandERRβagonist. DY131displays inactive againstERRα,ERαandERβ[1][2]. DY131 also inhibitsSmosignaling[3]. |
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体外研究 (In Vitro) | DY131 (0.1-30 μM; 5 days) treatment suppresses cell proliferation and reduces BrdUrd-positive cells in both LNCaP-ERRγ and LNCaP cells in a dose-dependent manner, with higher suppression in LNCaP-ERRγ clone[1]. DY131inhibits Shh induced accumulation of Smo::EGFP with an IC50of 0.8 μM. DY131 suppresses SAG (100 nM) induced accumulation of Smo::EGFP in the primary cilium and Gli transcription activity with an IC50of ~2 μM[3]. DY131 dramatically decreases phosphorylated histone H3 (pH3) marked proliferation of CGNPs induced by Shh[3]. A selective ERRγ agonist, DY131, inhibits the growth of the ERα-positive endometrial cancer cells but promoted that of the ERα-negative cancer cells[4].
Cell Proliferation Assay[1] Cell Line: | LNCaP-ERRγ and LNCaP cells | Concentration: | 0.1 μM, 1 μM, 10 μM, 30 μM | Incubation Time: | 5 days | Result: | Suppressed cell proliferation and reduced BrdUrd-positive cells in both LNCaP-ERRγ and LNCaP cells in a dose-dependent manner. |
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体内研究 (In Vivo) | DY131 (5 μg/kg; subcutaneous injection; every second day; for 12 days) treatment increases P450 side-chain cleavage (P450scc), StAR and HMGCoA reductase (HMGCR) while decreases hormone sensitive lipase (HSL) expressions[5].
Animal Model: | Mature male mice (C57BL/6) (8-10 week-old; ~24.3 g)[5] | Dosage: | 5 μg/kg | Administration: | Subcutaneous injection; every second day; for 12 days | Result: | Increased P450scc, StAR and HMGCR while decreased HSL expressions. |
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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 | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 50 mg/mL(160.58 mM;Need ultrasonic) 配制储备液 1 mM | 3.2115 mL | 16.0576 mL | 32.1151 mL | 5 mM | 0.6423 mL | 3.2115 mL | 6.4230 mL | 10 mM | 0.3212 mL | 1.6058 mL | 3.2115 mL |
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以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (8.03 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.03 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (8.03 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.03 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (8.03 mM); Suspended solution
此方案可获得 ≥ 2.5 mg/mL (8.03 mM,饱和度未知) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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