價格 | ¥28500 | ¥59400 | ¥33100 |
包裝 | 25mg | 100mg | 50mg |
最小起訂量 | 1mg |
發(fā)貨地 | 上海 |
更新日期 | 2024-12-02 |
中文名稱:化合物 PXS-4787 | 英文名稱:PXS-4787 |
CAS:2409963-50-2 | 品牌: TargetMol |
產(chǎn)地: 美國 | 保存條件: Shipping with blue ice. |
產(chǎn)品類別: 抑制劑 | |
貨號: T60296 |
名稱 | PXS-4787 |
描述 | PXS-4787 is a potent and selective inhibitor of lysyl oxidase (LOX) with broad-spectrum activity. It effectively suppresses lysyl oxidase activity by acting on its mechanisms. The compound displays inhibitory effects with IC50 values of 2 μM (Bovine LOX), 3.2 μM (rh LOXL1), 0.6 μM (rh LOXL2), 1.4 μM (rh LOXL3), and 0.2 μM (rh LOXL4), respectively [1]. |
體外活性 | Lysyl oxidases stabilize collagen which is the main component of scar tissue, and drive scar stiffness and appearance [1]. PXS-4787 (0-10 μM; 15 min-4 h) dose- and time-dependently inhibits lysyl oxidase and displays comparable inhibitory activity across species [1]. PXS-4787 (0-100 μM; 72 h) is well tolerated by primary human dermal fibroblasts, (10 μM; 11 d) reduces collagen formation, deposition and crosslinking in primary human dermal fibroblasts cultured in vitro [1]. PXS-4787 (10 μM; 48 h) induces differential gene expression in fibroblasts and keratinocytes, including COL1A1, LOX, GAPDH, PGK1 [1]. Immunofluorescence [1] Cell Line: Primary human dermal fibroblasts cultured in vitro Concentration: 0, 1, 10 μM Incubation Time: 11 days Result: Significantly reduced in the 10 μM treatment group. RT-PCR [1] Cell Line: Cultured fibroblasts and keratinocytes (isolated from five different patients) Concentration: 10 μM Incubation Time: 48 hours Result: Resulted four genes with significant differential expression in fibroblasts and two differentially expressed genes in keratinocytes. |
體內(nèi)活性 | PXS-4787 (3%, oil in water cream; external application; once daily, for 28 days) lowers collagen deposition and cross-linkin in murine models of injury and fibrosis under topical application [1]. PXS-4787 (3%, oil in water cream; external application; once daily, for 12 weeks) also significantly improves scar appearance without reducing tissue strength in porcine injury models under topical application [1]. Animal Model: Porcine excision injury model (female Juvenile pigs, 18-20 kg) [1] Dosage: 3%, oil in water cream; 400 mg cream applied to 16 cm 2 Administration: External application; 1, 2 and 3 weeks post-injury; once dailly, for 12 weeks Result: Improved the appearance of scar in relevant in vivo models, indicative of a targetdriven, as opposed to compound-specific, effect. |
存儲條件 | Shipping with blue ice. |
成立日期 | 2013-04-18 (12年) | 注冊資本 | 589.8595萬人民幣 |
員工人數(shù) | 100-500人 | 年營業(yè)額 | ¥ 1億以上 |
主營行業(yè) | 中間體,天然產(chǎn)物,生物化工,化學(xué)試劑,生物技術(shù)服務(wù) | 經(jīng)營模式 | 貿(mào)易,工廠,試劑,定制,服務(wù) |
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