rel-3-Chloro-N-((1r,4r)-4-(methylamino)cyclohexyl)-N-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide hydrochloride
SAG hydrochloride
CAS: 2095432-58-7
Molecular Formula: C28H29Cl2N3OS
rel-3-Chloro-N-((1r,4r)-4-(methylamino)cyclohexyl)-N-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide hydrochloride - Names and Identifiers
| Name | SAG hydrochloride |
| Synonyms | SAG.2HCl SAG hydrochloride rel-3-Chloro-N-((1r,4r)-4-(methylamino)cyclohexyl)-N-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide hydrochloride |
| CAS | 2095432-58-7 |
rel-3-Chloro-N-((1r,4r)-4-(methylamino)cyclohexyl)-N-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide hydrochloride - Physico-chemical Properties
| Molecular Formula | C28H29Cl2N3OS |
| Molar Mass | 526.52 |
| Solubility | Soluble in DMSO |
| Storage Condition | -20℃ |
| Use | Smoothened Agonist (SAG) HCl is a cell permeability Smoothened (Smo) agonist whose EC50 in Shh-LIGHT2 cells is about 3 nM. |
| In vitro study | SAG regulates Smo activity by binding directly to the Smo helix bundle. SAG induces Smo-dependent signaling through Gli in a grk2-dependent manner. SAG(1 nM) also induced the proliferation of neuronal and glial precursor cells without affecting the differentiation pattern of the new cells. |
| In vivo study | In adult rat hippocampus, intraventricular administration of SAG (2.5 nM) significantly increased the number of newborn cells and prolonged the survival time of hippocampal cells. In mice, SAG (20 μg/g, I. p.) effectively prevents GC-induced neonatal cerebellar dysplasia. |
rel-3-Chloro-N-((1r,4r)-4-(methylamino)cyclohexyl)-N-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide hydrochloride - Reference
| Reference Show more | 1: Geyer N, Ridzewski R, Bauer J, Kuzyakova M, Dittmann K, Dullin C, Rosenberger A, Schildhaus HU, Uhmann A, Fulda S, Hahn H. Different Response of Ptch Mutant and Ptch Wildtype Rhabdomyosarcoma Toward SMO and PI3K Inhibitors. Front Oncol. 2018 Sep 25;8:396. doi: 10.3389/fonc.2018.00396. eCollection 2018. PubMed PMID: 30319965; PubMed Central PMCID: PMC6168716. 2: Guerrini G, Criscuoli M, Filippi I, Naldini A, Carraro F. Inhibition of smoothened in breast cancer cells reduces CAXII expression and cell migration. J Cell Physiol. 2018 Dec;233(12):9799-9811. doi: 10.1002/jcp.26947. Epub 2018 Aug 21. PubMed PMID: 30132883. 3: Gigante ED, Long AB, Ben-Ami J, Caspary T. Hypomorphic Smo mutant with inefficient ciliary enrichment disrupts the highest level of vertebrate Hedgehog response. Dev Biol. 2018 May 15;437(2):152-162. doi: 10.1016/j.ydbio.2018.03.019. Epub 2018 Mar 20. PubMed PMID: 29571613; PubMed Central PMCID: PMC5903954. 4: Zhang F, Hao M, Jin H, Yao Z, Lian N, Wu L, Shao J, Chen A, Zheng S. Canonical hedgehog signalling regulates hepatic stellate cell-mediated angiogenesis in liver fibrosis. Br J Pharmacol. 2017 Mar;174(5):409-423. doi: 10.1111/bph.13701. Epub 2017 Jan 31. PubMed PMID: 28052321; PubMed Central PMCID: PMC5301045. |
rel-3-Chloro-N-((1r,4r)-4-(methylamino)cyclohexyl)-N-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide hydrochloride - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.899 ml | 9.496 ml | 18.993 ml |
| 5 mM | 0.38 ml | 1.899 ml | 3.799 ml |
| 10 mM | 0.19 ml | 0.95 ml | 1.899 ml |
| 5 mM | 0.038 ml | 0.19 ml | 0.38 ml |
Last Update：2024-01-02 23:10:35
rel-3-Chloro-N-((1r,4r)-4-(methylamino)cyclohexyl)-N-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide hydrochloride - Reference Information
| biological activity | , its EC50 in Shh-LIGHT2 cells was approximately 3 nM.|
| Target | Value |
| Smoothened (mouse cultured cell assay) | 3 nM(EC50) |
Last Update：2024-04-09 21:32:11
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