MPT0G211|cas:2151853-97-1|西域试剂

MPT0G211,99.55%

产品编号：Bellancom-123976| CAS NO：2151853-97-1| 分子式：C₁₇H₁₅N₃O₂| 分子量：293.32

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货号	价格	库存与货期
Bellancom-123976	￥3000.00	杭州北京（现货）
Bellancom-123976	￥4800.00	杭州北京（现货）
Bellancom-123976	￥9500.00	杭州北京（现货）
Bellancom-123976	￥14500.00	杭州北京（现货）
Bellancom-123976	￥22500.00	杭州北京（现货）

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MPT0G211

产品介绍

MPT0G211 是一种高效、口服活性和选择性的 HDAC6 抑制剂 (IC₅₀=0.291 nM)。MPT0G211 对 HDAC6 的选择性是其他 HDAC 亚型的 1000 倍。MPT0G211 可以透过血脑屏障。MPT0G211 改善阿尔茨海默病模型中 tau 磷酸化和认知缺陷。MPT0G211 具有抗转移和神经保护作用。抗癌活性。

生物活性

MPT0G211 is a potent, orally active and selective HDAC6 inhibitor (IC₅₀=0.291 nM). MPT0G211 displays >1000-fold selective for HDAC6 over other HDAC isoforms. MPT0G211 can penetrate the blood-brain barrier. MPT0G211 ameliorates tau phosphorylation and cognitive deficits in an Alzheimer’s disease model. MPT0G211 has anti-metastatic and neuroprotective effects. Anticancer activities.

体外研究

MPT0G211 (0.1 μM; cells were transfected with pCAX APP 695 and pRK5-EGFP-Tau P301L for 24 h) significantly inhibits the phosphorylation of tau Ser396.
MPT0G211 inhibits HDAC6/Hsp90 binding and causes subsequent proteasomal degradation of polyubiquitinated proteins.
MPT0G211 significantly decreases the phosphorylation of tau by GSK3β inactivation.
MPT0G211 (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).
MPT0G211 inhibits MDA-MB-231 and MCF-7 cells growth (GI₅₀=16.19 and 5.6 μM, respectively).
In AML cells, MPT0G211 potentiated the cytotoxic effects of DOXO by impairing DNA repair machinery and activating Bcl-2-associated X protein (BCL-XL)-dependent cell apoptosis.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

MPT0G211 (50 mg/kg; p.o.; daily for 3 months) significantly ameliorates the spatial memory impairment.
MPT0G211 (25 mg/kg; i.p. ; qd; day 73 post-tumor injection) reduces numbers of nodules and lung weights.
MPT0G211 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Triple transgenic (3×Tg-AD) mice (harboring APP_Swe and tau_P301L mutant transgenes
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)
Dosage:	25 mg/kg
Administration:	I.p.; qd; day 73 post-tumor injection
Result:	Significantly reduced numbers of nodules and lung weights.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Triple transgenic (3×Tg-AD) mice (harboring APP_Swe and tau_P301L mutant transgenes
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)
Dosage:	25 mg/kg
Administration:	I.p.; qd; day 73 post-tumor injection
Result:	Significantly reduced numbers of nodules and lung weights.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (340.92 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.4092 mL	17.0462 mL	34.0925 mL
5 mM	0.6818 mL	3.4092 mL	6.8185 mL
10 mM	0.3409 mL	1.7046 mL	3.4092 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (8.52 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.52 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明