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抑制剂描述:

产品名称:Smoothened Agonist (SAG)

产品别名:见爱必信官网

英文别名:Smoothened Agonist (SAG)

靶点:Smo

CAS:912545-86-9

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

SAG is a potent Smoothened (Smo) receptor agonist (Kd = 59 nM); potently activates the Hedgehog signaling pathway in Shh-light 2 cells (EC50 ~ 3 nM).

溶解性:Ethanol :40 mg/mL (75.97 mM)
DMSO :100 mg/mL (189.92 mM)
Water :100 mg/mL (189.92 mM)

体外研究:

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. SAG and purmorphamine verride the inhibitory effect of robotnikinin since Smo functions downstream of Shh/Ptc1.

体内研究:In CD-1 mice, SAG (1.0 mM) or NELL-1 (600 μg/ml) alone results in increased bone formation at 4 and 8 weeks, but significantly greater bone formation with both components combined (SAG + NELL-1). The combination of the two compounds exhibits a significant increase in new bone formation, accompanied by increased defect vascularization. SAG (15, 17, or 20 mg/kg, i.p.) induces pre-axial polydactyly prevalently. The highest SAG dose is 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.

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