SAG

生物活性靶点体外研究体内研究 SAG 试剂级价格

SAG

CAS号:912545-86-9
英文名:SAG
中文名:SAG
CBNumber:CB91565561
分子式:C28H28ClN3OS
分子量:490.06
MOL File:912545-86-9.mol

SAG化学性质

沸点 :688.6±55.0 °C(Predicted)
密度 :1.30±0.1 g/cm3(Predicted)
储存条件 :Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
溶解度 :Soluble in DMSO (up to 20 mg/ml), in DMF (up to 20 mg/ml) or in Ethanol (up to 20 mg/ml).
酸度系数(pKa) :10?+-.0.40(Predicted)
形态 :lyophilized solid
颜色 :white to beige
敏感性 :Light Sensitive
稳定性 :Light Sensitive

安全信息

危险品运输编号 :UN 2811 6.1 / PGIII
海关编码 :2934999090

SAG性质、用途与生产工艺

生物活性 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。
靶点

EC50: 3 nM (Smo)
体外研究

SAG (0.1 nM-100 μM; 30 h) induces firefly luciferase expression in Shh-LIGHT2 cells with an EC ₅₀ of 3 nM and then inhibits expression at higher concentrations.
SAG (1-1000 nM; 1 h) competes for the binding of BODIPY-cyclopamine to Smo-expressing Cos-1 cells, yielding an apparent dissociation constant (K _d ) of 59 nM for the SAG/Smo complex.
SAG (100 nM) inhibits the inhibitory effect of ShhN-induced pathway activation by Robotnikinin.
SAG (250 nM; 48 h) significantly increases SMO mRNA and protein expression in MDAMB231 cells.
SAG (250 nM; 24 and 48 h) increases CAXII mRNA expression in MDAMB231 cells at 24h in normoxic and hypoxic conditions in MDAMB231 cells.
SAG (250 nM; 24 h) increases MDAMB231 cells migration.

体内研究

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.
SAG (15-20 mg/kg; i.p.) induces pre-axial polydactyly prevalently in a dose-dependent manner in mice.

Animal Model:	Pregnant C57BL/6J mice
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.