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Smoothened Agonist(SAG)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Smoothened Agonist(SAG)图片
CAS NO:912545-86-9
规格:≥98%
包装与价格:
包装价格(元)
1mg电议
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)490.06
FormulaC28H28ClN3OS
CAS No.912545-86-9
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 71 mg/mL (134.8 mM)
Water: N/A
Ethanol: 40 mg/mL (75.9 mM)
Other info

Chemical Name: 3-chloro-N-((1r,4r)-4-(methylamino)cyclohexyl)-N-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide

SMILES Code: O=C(C1=C(Cl)C2=CC=CC=C2S1)N([C@H]3CC[C@H](NC)CC3)CC4=CC=CC(C5=CC=NC=C5)=C4

Exact Mass: 489.16416

Synonyms

SAG free base; SAG; SAG (cyclopamine antagonist);SAG (Smo agonist)

实验参考方法
In Vitro

In vitro activity: SAG regulates Smo activity by binding directly to the Smo heptahelical bundle. SAG induces Smo-dependent signaling through Gli in a GRK2-dependent way. SAG also (1 nM) induces proliferation of neuronal and glial precursors without affecting the differentiation pattern of newly produced cells.


Cell Assay: SAG acts downstream of Ptch1 in the Hh pathway and counteracts cyclopamine inhibition of Smo. SAG induces firefly luciferase expression in Shh-LIGHT2 cells with an EC50 of 3 nM and then inhibits expression at higher concentrations. In Smo-expressing Cos-1 cells, SAG yields an apparent dissociation constant (KD) of 59 nM for the SAG/Smo complex.

In VivoIn the adult rat hippocampus, the intracerebroventricular administration of SAG (2.5 nM) significantly increases the number of newly generated cells and extends survival of hippocampal cells. In mice, SAG (20 μg/g, i.p.) effectively prevents GC-induced neonatal cerebellar developmental abnormalities.
Animal modelRats and mice
Formulation & DosageRats: 2.5 nM, intracerebroventricular administration; Mice: 20 μg/g, i.p.
References

Proc Natl Acad Sci U S A. 2002 Oct 29;99(22):14071-6; Neurosci Lett. 2010 Sep 27;482(2):81-5.