SAG 是一种有效的Smoothened (Smo)受体激动剂 (EC50=3 nM;Kd=59 nM)。SAG 可激活 Hedgehog 信号通路并抵消 Cyclopamine (HY-17024) 对 Smo 的抑制作用。
生物活性 | SAG is a potentSmoothened (Smo) receptoragonist (EC50=3 nM;Kd=59 nM). SAG activates theHedgehogsignaling pathway and counteracts Cyclopamine (HY-17024) inhibition ofSmo[1][2][3]. |
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体外研究 (In Vitro) | SAG (0.1 nM-100 μM; 30 h) induces firefly luciferase expression in Shh-LIGHT2 cells with an EC50of 3 nM and then inhibits expression at higher concentrations[1]. SAG (1-1000 nM; 1 h) competes for the binding of BODIPY-cyclopamine to Smo-expressing Cos-1 cells, yielding an apparent dissociation constant (Kd) of 59 nM for the SAG/Smo complex[1]. SAG (100 nM) inhibits the inhibitory effect of ShhN-induced pathway activation by Robotnikinin[2]. SAG (250 nM; 48 h) significantly increases SMO mRNA and protein expression in MDAMB231 cells[3]. SAG (250 nM; 24 and 48 h) increases CAXII mRNA expression in MDAMB231 cells at 24h in normoxic and hypoxic conditions in MDAMB231 cells[3]. SAG (250 nM; 24 h) increases MDAMB231 cells migration[3].
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体内研究 (In Vivo) | SAG (1.0 mM) induces more osteogenesis mainly at the defect borders and a significant increase in BV/TV at the eight week timepoint in CD-1 mice[4]. SAG (15-20 mg/kg; i.p.) induces pre-axial polydactyly prevalently in a dose-dependent manner in mice[5].
Animal Model: | Pregnant C57BL/6J mice[5] | Dosage: | 15, 17, 20 mg/kg | Administration: | A single i.p. | Result: | Effective in ca. 80% of the embryos and increased Gli1 and Gli2 mRNA expression in the limb bud, with Gli1 mRNA being the most upregulated at the dose of 20 mg/kg. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
溶解性数据 | In Vitro: DMSO : ≥ 38 mg/mL(77.54 mM) H2O :< 0.1 mg/mL (ultrasonic;warming;heat to 60℃)(insoluble) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 2.0406 mL | 10.2028 mL | 20.4057 mL | 5 mM | 0.4081 mL | 2.0406 mL | 4.0811 mL | 10 mM | 0.2041 mL | 1.0203 mL | 2.0406 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 (protect from light)。-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: ≥ 10 mg/mL (20.41 mM); Clear solution
此方案可获得 ≥ 10 mg/mL (20.41 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 100.0 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: ≥ 10 mg/mL (20.41 mM); Clear solution
此方案可获得 ≥ 10 mg/mL (20.41 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 100.0 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: ≥ 10 mg/mL (20.41 mM); Clear solution
此方案可获得 ≥ 10 mg/mL (20.41 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 100.0 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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