DY131 GSK 9089|cas:95167-41-2|西域试剂

DY131 GSK 9089,99.88%

产品编号：Bellancom-15483| CAS NO：95167-41-2| 分子式：C₁₈H₂₁N₃O₂| 分子量：311.38

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货号	价格	库存与货期
Bellancom-15483	￥600.00	杭州北京（现货）
Bellancom-15483	￥1000.00	杭州北京（现货）
Bellancom-15483	￥3500.00	杭州北京（现货）
Bellancom-15483	￥5500.00	杭州北京（现货）

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DY131 GSK 9089

产品介绍

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 selective ERRγ and ERRβ agonist. DY131displays inactive against ERRα, ERα and ERβ. DY131 also inhibits Smo signaling.

体外研究

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.
DY131inhibits Shh induced accumulation of Smo::EGFP with an IC₅₀ of 0.8 μM. DY131 suppresses SAG (100 nM) induced accumulation of Smo::EGFP in the primary cilium and Gli transcription activity with an IC₅₀ of ~2 μM.
DY131 dramatically decreases phosphorylated histone H3 (pH3) marked proliferation of CGNPs induced by Shh.
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].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

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.

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].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (160.58 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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

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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
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。