- ￥8480 - 14000
- TargetMol
- T61753
- 2026年07月07日
2 年钻石会员
企业认证
相关产品推荐更多 >
万千商家帮你免费找货
0 人在求购买到急需产品
- 详细信息
- 文献和实验
- 技术资料
- CAS号：
2151854-33-8
- 规格：
25mg/50mg/100mg
| 规格： | 25mg | 产品价格： | ￥8480.0 |
|---|---|---|---|
| 规格： | 50mg | 产品价格： | ￥11040.0 |
| 规格： | 100mg | 产品价格： | ￥14000.0 |
Product Introduction
Bioactivity
| 名称 | MPT0G211 mesylate |
| 描述 | MPT0G211 mesylate is a powerful and selective HDAC6 inhibitor (IC50 = 0.291 nM), with high oral bioavailability. It exhibits remarkable selectivity for HDAC6 over other HDAC isoforms (>1000-fold selectivity). Additionally, MPT0G211 mesylate can effectively cross the blood-brain barrier. In preclinical studies using an Alzheimer's disease model, MPT0G211 mesylate has shown promising results in reducing tau phosphorylation and cognitive deficits. Furthermore, this compound exhibits anti-metastatic and neuroprotective effects, making it a potential candidate for anticancer interventions. [1] [2] [3]. |
| 体外活性 | MPT0G211 mesylate (0.1 μM; Cells were transfected with pCAX APP 695 and pRK5-EGFP-Tau P301L for 24 h) significantly inhibited the phosphorylation of tau Ser396 [1]. MPT0G211 mesylate inhibits HDAC6/Hsp90 binding and causes subsequent proteasomal degradation of polyubiquitinated proteins [1]. MPT0G211 mesylate significantly decreases the phosphorylation of tau by GSK3β inactivation [1]. MPT0G211 mesylate (0.1 μM; 24 hours) significantly attenuates the phosphorylation of tau Ser396 and Ser404 in both cell lines (SH-SY5Y and Neuro-2a cells were transfected for 24 h with pCAX APP 695 and pRK5-EGFP-Tau P301L) [1]. MPT0G211 mesylate inhibits MDA-MB-231 and MCF-7 cells growth (GI 50 =16.19 and 5.6 μM, respectively) [2]. In AML cells, MPT0G211 mesylate potentiates the cytotoxic effects of DOXO by impairing DNA repair machinery and activating Bcl-2-associated X protein (BCL-XL)-dependent cell apoptosis [3]. |
| 体内活性 | MPT0G211 mesylate (50 mg/kg; p.o.; daily for 3 months) significantly ameliorates the spatial memory impairment [1]. MPT0G211 mesylate (25 mg/kg; i.p.; qd; day 73 post-tumor injection) reduces numbers of nodules and lung weights [2]. MPT0G211 mesylate treatment not only diminishes tau phosphorylation by inhibition GSK3β activity but also enhances the acetylation of Hsp90, which causes the downregulation of HDAC6/Hsp90 binding and facilitates proteasomal degradation of polyubiquitinated p-tau [1]. Animal Model: Triple transgenic (3×Tg-AD) mice (harboring APP Swe and tau P301L mutant transgenes [1] Dosage: 50 mg/kg Administration: P.o.; daily for 3 months Result: Significantly ameliorated the spatial memory impairment. Animal Model: Female SCID mice (bearing MDA-MB-231 cells) [2] Dosage: 25 mg/kg Administration: I.p.; qd; day 73 post-tumor injection Result: Significantly reduced numbers of nodules and lung weights. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 相关产品 | Valproic acid sodium salt | 4-Phenylbutyric acid | Valproic Acid | Sodium butanoate | Panobinostat | Manganese chloride (tetrahydrate) | Methoxyacetic acid | Theophylline | Acefylline | Curcumin | Theophylline monohydrate | Sodium 4-phenylbutyrate |
风险提示：丁香通仅作为第三方平台，为商家信息发布提供平台空间。用户咨询产品时请注意保护个人信息及财产安全，合理判断，谨慎选购商品，商家和用户对交易行为负责。对于医疗器械类产品，请先查证核实企业经营资质和医疗器械产品注册证情况。
文献和实验该产品被引用文献
官网有文献
技术资料暂无技术资料 索取技术资料
文献支持
化合物 MPT0G211 mesylate【2151854-33-8】
￥8480 - 14000
