SUN11602
作者：齊岳
發布時間：2023-08-28
09:00:55
點擊數：
產品名稱：SUN11602
產品描述：
| 產品描述 | SUN11602, an aniline compound, mimics the neuroprotective mechanisms of basic fibroblast growth factor. It mimics the neuroprotective effects of bFGF and prevents glutamate-induced neuronal death. It also increases levels of CALB1 gene expression in cerebrocortical neurons and triggers phosphorylation of FGFR and ERK1/2. |
| 體外活性 | Physiological actions of SUN11602 mimic several phenomena of the neuroprotection that is induced by bFGF. SUN11602 plays a pivotal role in allowing primary cultured neurons to survive in adverse environments of glutamate toxicity and activating intracellular key molecules that are involved in the neuroprotective mechanisms. These actions are quite similar to those of bFGF. Such neuroprotective mechanisms are specific and distinctive to SUN11602 and bFGF and differs clearly from those of the other growth factors that are investigated. But unlike bFGF, SUN11602 can either directly or indirectly trigger the phosphorylation of the cytosolic domain of the FGFR without binding to the extracellular domain of the FGFR-1[1]. SUN11602 demonstrates no cell proliferative activity of somatic cells, unlike bFGF. SUN11602 significantly affects neuronal survival in adverse conditions through a FGFR1-mitogen-activated protein kinase/extracellular signal-regulated kinase-1/2 kinase (FGFR-1–MEK/ERK) signaling pathway[2]. |
| 體內活性 | In WT mice, SUN11602 and bFGF increase the levels of newly synthesized Calb in cerebrocortical neurons and suppress the glutamate-induced rise in intracellular Ca2+. This Ca2+-capturing ability of Calb allows the neurons to survive severe toxic conditions of glutamate. In contrast, Calb levels remain unchanged in Calb-/- mice after exposure to SUN11602 or bFGF, and due to a loss of function of the gene, these neurons are no longer resistant to toxic conditions of glutamate[1]. Neuroprotective activities of SUN11602 and FGF-2 are due to exogenously induced hyperexpression of CalB in hippocampal neurons. The pharmacokinetic properties of SUN11602 appear to hold promise in terms of bioavailability (>65%) after oral administration in rodents (rats and mice) and dogs (beagles)[2]. |
| 細胞實驗 | Actinomycin D or cycloheximide is first added to the cultures, and, 2 h later, SUN11602 or bFGF is added. After a 24 h incubation, neurons in the cultures are exposed to 150 μM glutamate for another 24 h, and cell viability is determined by a (3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H tetrazolium bromide (MTT) assay.(Only for Reference) |
| 別名 | SUN 11602 |
| 分子量 | 451.615 |
| 分子式 | C26H37N5O2 |
| CAS No. | 704869-38-5 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
Ethanol: 9 mg/mL (20 mM)
DMSO: 22.6 mg/mL (50 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齊岳生物科技有限公司是集化學科研和定制與一體的高科技化學公司。業務范圍包括化學試劑和產品的研發、生產、銷售等。涉及產品為通用試劑的分銷、非通用試劑的定制與研發，涵蓋生物科技、化學品、中間體和化工材料等領域。
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