| CAS NO: | 912545-86-9 |
| 规格: | ≥98% |
| 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 |
| Molecular Weight (MW) | 490.06 |
|---|---|
| Formula | C28H28ClN3OS |
| 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) |
| 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 Vivo | In 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 model | Rats and mice |
| Formulation & Dosage | Rats: 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. |
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