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CAS No.: 2095432-58-7

SAG HCl Catalog No. CSN19210

Synonyms: Smoothened Agonist HCl;SAG;SAG (Smo agonist)

SAG HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述The Hh signaling pathway can be activated after the inhibition of Smoothened (Smo) by Ptch is relieved through the binding of ligand to Ptch. SAG is an Hh pathway agonist with EC50 value of ~3nM for induction of this pathway activation in a mouse cultured cell assay (Shh-LIGHT2; ref. 24), which target directly on Smo and can work in an Hh protein-independent manner. This activation by SAG could be inhibited by Ptch1 in a dose-dependent manner, as well as be counteracted by the smo antagonists SANT1-4 (20-200nM) . Through activation of Hh pathway by 0.5-5nM SAG, increased expression of Gli1 mRNA in the cortical/hippocampal cell culture could be observed. Incubation with 0.5nM and 1nM SAG (but no effect at 5nM) for 48h could lead to increased cell proliferation in this culture. Consistent with this, intracerebral injection with SAG at dose of both 2.5nM and 2.5μM significantly increased the number of newly generated cells in the adult rat hippocampus. Combined treatment of 0.4mM SAG with sonic hedgehog (200 ng/mL) could enhance neuronal differentiation of iPSCs into dopaminergic neurons.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
HUVEC	-	Cytotoxicity assay	24 h	Cytotoxicity against HUVEC after 24 hrs by WST-1 assay, IC50=22 μM	22985958
mouse Shh-Light II cell	-	Function assay	48 hrs	Activation of Shh pathway in mouse Shh-Light II cells assessed as induction of gli1 expression after 48 hrs by renilla luminescence assay, EC50=0.0088 μM	22985958

动物研究
剂量
Mice: 15 mg/kg - 20 mg/kg^[3] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 15 mg/kg - 20 mg/kg^[3] (i.p.)
给药途径	i.p.

[1] Meloni AR, Fralish GB, et al. Smoothened signal transduction is promoted by G protein-coupled receptor kinase 2. Mol Cell Biol. 2006 Oct;26(20):7550-60.
[2] Chen JK, Taipale J, et al. Small molecule modulation of Smoothened activity. Proc Natl Acad Sci U S A. 2002 Oct 29;99(22):14071-6.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8993 mL
- 9.4963 mL
- 18.9926 mL
- 5 mM
- 0.3799 mL
- 1.8993 mL
- 3.7985 mL
- 10 mM
- 0.1899 mL
- 0.9496 mL
- 1.8993 mL

技术信息

CAS号

2095432-58-7

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H29Cl2N3OS

运输

蓝冰

分子量

526.52

别名

Smoothened Agonist HCl;SAG;SAG (Smo agonist)

溶解度

DMSO	210.0 mg/mL (398.8 mM)
Water	125.0 mg/mL (237.4 mM)

动物实验配方

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