MRK-560|cas:677772-84-8|西域试剂

MRK-560,99.0%

产品编号：Bellancom-14174| CAS NO：677772-84-8| 分子式：C₁₉H₁₇ClF₅NO₄S₂| 分子量：517.92

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货号	价格	库存与货期
Bellancom-14174	￥1600.00	杭州北京（现货）
Bellancom-14174	￥2500.00	杭州北京（现货）
Bellancom-14174	￥8800.00	杭州北京（现货）
Bellancom-14174	￥14000.00	杭州北京（现货）

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MRK-560

产品介绍

MRK-560 是一种口服有效的，可渗透血脑屏障的 γ-Secretase 抑制剂，能有效减少大鼠脑和脑脊液中 Aβ 肽。MRK-560 能通过选择性地抑制 PSEN1 来阻碍 NOTCH1 的突变进程。MRK-560 可用于阿尔兹海默病和 T 细胞急性淋巴细胞白血病的研究。

生物活性

MRK-560 is an orally active, brain barrier-penetrating γ-Secretase inhibitor, can potently reduces Aβ peptide in rat brain and cerebrospinal fluid. MRK-560 also decreases mutant NOTCH1 processing by selectively inhibiting PSEN1. MRK-560 can be used in studies of Alzheimer's disease and T-cell acute lymphoblastic leukaemia (T-ALL).

体外研究

MRK-560 (30, 100, 300, 1000 nM; 15days) blocks mutant NOTCH1 receptor signaling in human T-ALL cell lines.

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

Cell Proliferation Assay

Cell Line:	HPB-ALL, DND-41, and Jurkat cells
Concentration:	30, 100, 300, 1000 nM
Incubation Time:	15 days
Result:	Reduced NICD1 generation in cells and resulted in a dose-dependent decrease of proliferation in HPB-ALL and DND-41, which depend on NOTCH signaling for their survival.

体内研究
(In Vivo)

MRK-560 (15.54 mg/kg; S.C.; single daily for 14 days) shows strong antileukemic effects on T-ALL model.
MRK-560 (1, 3, 10, 30, 100 mg/kg; p.o.; single) shows good blood-brain barrier permeability in a dose-dependent manner in rats.

MRK-560 (1, 3, 10, 30, 100 mg/kg; p.o.; single) inhibits the production of Aβ levels in brain and cerebrospinal fluid.
MRK-560 (1 mg/kg; p.o.; single) shows a good bioavailability of 70 to 90%, and T_max is 12 h.
MRK-560 (1 mg/kg; i.v.; single) is suitable for once-a-day dosing (with a low plasma clearance and a half-life of more than 15 h).

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

Animal Model:	Tg (HLA-DRB1) 31Dmz/Szj (NSG) mice (T-ALL (T cell acute lymphoblastic leukemia) model).
Dosage:	15.54 mg/kg
Administration:	Subcutaneous injection; single daily for 14 days.
Result:	Resulted in strong antileukemic effects and improved median survival to 30 days compared to 18 days in vehicle-treated mice.

Animal Model:	Male Sprague-Dawley rats (250-300 g).
Dosage:	1, 3, 10, 30, 100 mg/kg
Administration:	Oral administration; single (experiment is performed 8 h later)
Result:	Increased the plasma and brain concentrations in a dose-dependent manner. Reduced (dose-dependent) both brain and CSF Aβ levels, with essentially complete inhibition of the production of both peptides being observed at a dose of 100 mg/kg.

Animal Model:	Male Sprague-Dawley rats (250-300 g).
Dosage:	1 mg/kg
Administration:	Intravenously and orally administration; single.
Result:	Showed T_max after the oral dose was 12 h,and bioavailability was 70 to 90%. Revealed a low plasma clearance of less than 5 mL/min/kg with a volume of distribution of approximately 6 L/kg, which translated to a long half-life of more than 15 h.

体内研究

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

Animal Model:	Tg (HLA-DRB1) 31Dmz/Szj (NSG) mice (T-ALL (T cell acute lymphoblastic leukemia) model).
Dosage:	15.54 mg/kg
Administration:	Subcutaneous injection; single daily for 14 days.
Result:	Resulted in strong antileukemic effects and improved median survival to 30 days compared to 18 days in vehicle-treated mice.

Animal Model:	Male Sprague-Dawley rats (250-300 g).
Dosage:	1, 3, 10, 30, 100 mg/kg
Administration:	Oral administration; single (experiment is performed 8 h later)
Result:	Increased the plasma and brain concentrations in a dose-dependent manner. Reduced (dose-dependent) both brain and CSF Aβ levels, with essentially complete inhibition of the production of both peptides being observed at a dose of 100 mg/kg.

Animal Model:	Male Sprague-Dawley rats (250-300 g).
Dosage:	1 mg/kg
Administration:	Intravenously and orally administration; single.
Result:	Showed T_max after the oral dose was 12 h,and bioavailability was 70 to 90%. Revealed a low plasma clearance of less than 5 mL/min/kg with a volume of distribution of approximately 6 L/kg, which translated to a long half-life of more than 15 h.

体内研究

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

Animal Model:	Tg (HLA-DRB1) 31Dmz/Szj (NSG) mice (T-ALL (T cell acute lymphoblastic leukemia) model).
Dosage:	15.54 mg/kg
Administration:	Subcutaneous injection; single daily for 14 days.
Result:	Resulted in strong antileukemic effects and improved median survival to 30 days compared to 18 days in vehicle-treated mice.

Animal Model:	Male Sprague-Dawley rats (250-300 g).
Dosage:	1, 3, 10, 30, 100 mg/kg
Administration:	Oral administration; single (experiment is performed 8 h later)
Result:	Increased the plasma and brain concentrations in a dose-dependent manner. Reduced (dose-dependent) both brain and CSF Aβ levels, with essentially complete inhibition of the production of both peptides being observed at a dose of 100 mg/kg.

Animal Model:	Male Sprague-Dawley rats (250-300 g).
Dosage:	1 mg/kg
Administration:	Intravenously and orally administration; single.
Result:	Showed T_max after the oral dose was 12 h,and bioavailability was 70 to 90%. Revealed a low plasma clearance of less than 5 mL/min/kg with a volume of distribution of approximately 6 L/kg, which translated to a long half-life of more than 15 h.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (193.08 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9308 mL	9.6540 mL	19.3080 mL
5 mM	0.3862 mL	1.9308 mL	3.8616 mL
10 mM	0.1931 mL	0.9654 mL	1.9308 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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式