AGN 194310 (VTP-194310) 是一种高亲和力的、有效的、具有选择性的视黄酸受体 (RARs) 的泛拮抗剂，对RARα，RARβ，RARγ的Kd值分别为 3 nM，2 nM，5 nM。
| 生物活性 | AGN 194310 (VTP-194310) is a high affinity, potent and selectiveretinioic acid receptors (RARs)pan-antagonist withKdvalues of 3 nM, 2 nM, 5 nM forRARα,RARβ,RARγ, respectively[1][2]. |
体外研究
(In Vitro) | AGN194310 potently inhibits colony formation by all three lines, with IC50 values of 16 nM for LNCaP cells; 18 nM for PC3 cells; and 34 nM for DU-145 cells[2].
AGN 194310 (50 nM, 100 nM; LNCaP, PC-3 and DU-145 cells) inhibits colony formation at concentrations of 50 nM and 100 nM alone and in combination with TTNPB[2].
AGN 194310 (1 μM; 72 hours; LNCaP cells) treatment results in 80% apoptosis[2].
Cell Viability Assay[2] | Cell Line: | LNCaP, PC-3 and DU-145 cells. | | Concentration: | 50 nM, 100 nM | | Incubation Time: | | | Result: | When used together with 100 nM TTNPB, there was almost complete reversal of the growth inhibitory effect of 50 nM and partial reversal of the effect of 100 nM. |
Apoptosis Analysis[2] | Cell Line: | LNCaP cells | | Concentration: | 1 μM | | Incubation Time: | 72 hours | | Result: | Induced apoptosis in LNCaP cells. |
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体内研究
(In Vivo) | AGN 194310 (0.5 mg/kg/day; oral gavage; every day; for 10 days; female C57Bl/6J mice) treatment increases the number of granulocytes across haemopoietic compartments. A significant increase in the frequency of granulocyte-progenitor cells is observed in the bone marrow of mice after treatment with AGN194310[3].
| Animal Model: | Female C57Bl/6J mice (Five-week-old (34-37 days))[3] | | Dosage: | 0.5 mg/kg/day | | Administration: | Oral gavage; every day; for 10 days | | Result: | The number of granulocytes was significantly increased across haemopoietic compartments. Progenitor cells containing granulocytes also increased significantly. |
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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(117.77 mM;ultrasonic and warming and heat to 60℃) H2O :< 0.1 mg/mL(insoluble) 配制储备液 | 1 mM | 2.3554 mL | 11.7772 mL | 23.5544 mL | | 5 mM | 0.4711 mL | 2.3554 mL | 4.7109 mL | | 10 mM | 0.2355 mL | 1.1777 mL | 2.3554 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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: ≥ 1 mg/mL (2.36 mM); Clear solution
此方案可获得 ≥ 1 mg/mL (2.36 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 10.0 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%corn oil Solubility: ≥ 1 mg/mL (2.36 mM); Clear solution
此方案可获得 ≥ 1 mg/mL (2.36 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 10.0 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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