计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥99% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-20°C储存。超低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
IHMT-MST1-58 is a potent, selective mammalian and orally active STE20-like protein 1 kinase (MST1) inhibitor with IC 50 value of 23 nM. IHMT-MST1-58 can be used for the research of Type 1/2 diabetes
In Vitro
IHMT-MST1-58 (compound 19) shows good activity against MST1 with an IC 50 value of 23 nM. IHMT-MST1-58 (1 μM) displays strong inhibitory activity against MST1 (IC 50 = 23 nM), weak activity against MST2 (IC 50 = 652 nM), but no activity against NEK3 even at 10 μM (IC 50 > 10 μM). IHMT-MST1-58 (1 μM) shows strong binding affinity to MST1 and weak binding affinity to MST2 with K d values of 240 nM and 2.7 μM. IHMT-MST1-58 (0.1-10 μM; 1-2 h) inhibits the phosphorylation of MST1 in vitro. IHMT-MST1-58 (0.03, 0.1 and 0.3 μM; 48 h) exhibits a significant protective effect of β cells from the damage caused by inflammatory cytokines. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: HepG2 liver cells, RAW264.7, RPE1 and HL7702 cells; INS-1 and RIN-m5F cell lines Concentration: 0-10 μM Incubation Time: 2 h (HepG2 liver cells, RAW264.7, RPE1, and HL7702 cells) Result: Inhibited the H2O2-stimulated MOB1 phosphorylation and MST1/2 autophosphorylation in a dose-dependent manner in all four cell lines. Inhibited the phosphorylation of LATS1 (T1079) and YAP (S127) in HepG2 cells. Showed strong inhibition of MST1 phosphorylation and its downstream MOB1 autophosphorylation in a dose-dependent manner in both cell lines.
In Vivo
IHMT-MST1-58 (compound 19) (p.o, 50 mg/kg/day, QD) combination with metformin led to the decline of fasting blood glucose, show protective effect of β cells and decrease the hemoglobin A1c level in the STZ-induced T1D/T2D mouse models . Pharmacokinetic Parameters of IHMT-MST1-58 in different species (i.v. or p.o; 1 mg/kg, 5 mg/kg and 10 mg/kg) . mice rats beagle dogs parameter i.v.(1 mg/kg) p.o.(10 mg/kg) i.v.(1 mg/kg) p.o.(10 mg/kg) i.v.(1 mg/kg) p.o.(10 mg/kg) AUC 0-t (ng/mL*h) 501.1 5583 2553±155.1 4858±2648 764.5±82.9 4939±1067 t 1/2 (h) 1.7 1.81 3.51±0.34 3.03±0.2 6.47±0.71 5.79±1.09 C max /F (ng/mL) 1240 1922 944.0±219.1 1717±276 466.7±45.2 1113±417 F(%) - 110.8 - 73.3±40.1 - 106.5±20.9 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: mice Dosage: 50 mg/kg Administration: oral, single Result: parameter plasma pancreas C max (ng/mL) 3990±390 12216±1509 AUC 0-t (ng/mL*h) 13621±2127 51394±10098 Cl(mL/h/kg) 3734±641 996±189 Animal Model: T1D mouse models and T2D mouse models Dosage: 50 mg/kg Administration: p.o, 50 mg/kg/day, QD Result: Decreased the FBG level, improved the food intake and water consumption, had low HbA1c and a good antidiabetic effect, improved the histological structure of the islet. Animal Model: mice, Sprague Dawley rats, and beagle dogs Dosage: 1 mg/kg, 5 mg/kg and 10 mg/kg Administration: intravenous injection and oral administration Result: Displayed acceptable pharmacokinetic properties in different species.
Form:Solid
IC50& Target:MST1 23 nM (IC 50 )
规格
规格或纯度
≥99%
英文名称
IHMT-MST1-58
生化机理
IHMT-MST1-58 是一种强效、选择性哺乳动物口服活性 STE20 样蛋白 1 激酶（MST1）抑制剂，IC 50 值为 23 nM。IHMT-MST1-58 可用于 1/2 型糖尿病的研究。
储存条件
-20°C储存
运输条件
超低温运输
作用类型
抑制剂
纯度
≥99%
名称和识别符
分子类型
小分子
分子量
438.50
技术文档
高级数据
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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溶液计算器
常见问题
本产品的纯度是多少？
本产品的化学纯度（含量）为 ≥99%。批次的具体数值以分析证书（COA）为准。
本产品应如何储存？
请于?20 °C条件下保存。需冷冻保存以维持规定的有效期。
本产品如何运输？
本产品采用保温箱配冰袋运输。收货后请立即拆包，并按上述储存条件保存。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 2414484-25-4，分子式为 C21H22N6O3S，分子量为 438.50 g/mol。
如何获取批次专用COA？
每个订单都会随附分析证书（COA），您也可以从账户订单历史中下载。如需订购前的COA，请联系您的客户代表，或使用PDP上的"申请COA"按钮——我们将提供代表性批次的COA。
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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