SAG dihydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SAG dihydrochloride 是一种有效的 Smoothened (Smo) 受体激动剂 (EC50=3 nM; Kd=59 nM)。SAG dihydrochloride 可激活 Hedgehog 信号通路并抵消 Cyclopamine (HY-17024) 对 Smo 的抑制作用。

SAG dihydrochloride is a potent Smoothened (Smo) receptor agonist (EC50=3 nM; Kd=59 nM). SAG dihydrochloride activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of Smo.

SAG (0.1 nM-100 μM; 30 h) induces firefly luciferase expression in Shh-LIGHT2 cells with an EC50 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 (Kd) 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.

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.

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GPCR/G Protein

Hedgehog (Hh)

Hedgehog/Smoothened

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2702366-44-5

562.98

C28H30Cl3N3OS

>98% (HPLC)

In Vitro:?H2O 中的溶解度 : 100 mg/mL (177.63 mM; 超声助溶) DMSO 中的溶解度 : 33.33 mg/mL (59.20 mM; 超声助溶 )

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

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(-20℃)

With Ice Pack

≥ 2 years