SAR502250

COA

级别和纯度:

≥99%

CAS编号: 503860-57-9
分子式: C₁₉H₁₈FN₅O₂
分子量: 367.38
PubChem编号: 56589672

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货号 (SKU)	包装规格	是否现货
S648489-5mg	5mg	期货
S648489-10mg	10mg	期货
S648489-25mg	25mg	期货
S648489-50mg	50mg	期货
S648489-100mg	100mg	期货

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GSK-3 (105) PI3K/Akt/mTOR (764) Stem Cell/Wnt (1018)

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基本描述

规格或纯度	≥99%
英文名称	SAR502250
生化机理	SAR502250 是一种强效、选择性、ATP 竞争性、口服活性和脑穿透性 GSK3 抑制剂，对人 GSK-3β 的 IC 50 为 12 nM。SAR502250 具有类似抗抑郁剂的活性。SAR502250 可用于阿尔茨海默病的研究。
储存温度	-20°C储存
运输条件	超低温冰袋运输
产品介绍	SAR502250 is a potent, selective, ATP competitive, orally active and brain-penetrant inhibitor of GSK3 , with an IC 50 of 12 nM for human GSK-3β . SAR502250 displays antidepressant-like activity. SAR502250 can be used for the research of Alzheimer’s disease (AD) In Vitro SAR502250 (0.01-1 μM; 36 h) attenuates the Aβ 25-35 -induced cell death in rat embryonic hippocampal neurons. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo SAR502250 (1-100 mg/kg; a single p.o,) attenuates tau hyperphosphorylation in the cortex and spinal cord of transgenic mice expressing P301L tau. SAR502250 (10-30 mg/kg; p.o. once daily for 7 weeks) improves the cognitive deficit in transgenic APP(SW)/Tau(VLW) mice after infusion of Aβ 25-35. SAR502250 (10-30 mg/kg; a single p.o.) significantly increases the percentage of lever-presses in the inter-response time (IRT) bin (49-96 s), with a significant augmentation of the percentage of reinforced responses. SAR502250 (30 mg/kg; i.p. once daily for 28 d) ameliorates chronic stress-induced degradation of the physical state of the mice coat. SAR502250 (10-60 mg/kg; a single p.o.) decreases hyperactivity produced by psychostimulantsin mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female P301L human tau transgenic mice (three-month-old; 32 g)Dosage: 1, 3, 10, 30, 100 mg/kg Administration: A single p.o. Result: Attenuated dose-dependently tau phosphorylation in the cortex and spinal cord, with ED 50 s of 12.5 and 11.5 mg/kg, respectively. Form:Solid IC50& Target:hGSK-3β 12 nM (IC 50 )
纯度	≥99%

关联靶点（人）

GSK3B Tclin 糖原合酶激酶-3β(Glycogen synthase kinase-3 beta) (2 活性数据)

点击查看靶蛋白信息： GSK3B

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

GSK3B Tclin Glycogen synthase kinase-3 beta (11785 活性数据)

点击查看靶蛋白信息： GSK3B

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

CYP2D6 Tclin Cytochrome P450 2D6 (33882 活性数据)

点击查看靶蛋白信息： CYP2D6

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

CSNK1A1 Tchem Casein kinase I alpha (2581 活性数据)

点击查看靶蛋白信息： CSNK1A1

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

CYP1A2 Tchem Cytochrome P450 1A2 (26471 活性数据)

点击查看靶蛋白信息： CYP1A2

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

CYP3A4 Tclin Cytochrome P450 3A4 (53859 活性数据)

点击查看靶蛋白信息： CYP3A4

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

Caco-2 (12174 活性数据)

点击查看此靶标相关信息

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

GSK3A Tclin Glycogen synthase kinase-3 (736 活性数据)

点击查看靶蛋白信息： GSK3A

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

关联靶点（其它种属）

Mus musculus (284745 活性数据)

点击查看此靶标相关信息

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

Rattus norvegicus (775804 活性数据)

点击查看此靶标相关信息

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

Liver microsome (341 活性数据)

点击查看此靶标相关信息

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

作用机制

作用机制	Action Type	target ID	Target Name	Target Type	Target Organism	Binding Site Name	参考文献

名称和识别符

分子类型	小分子
IIUPAC Name	2-[(2S)-2-(4-fluorophenyl)morpholin-4-yl]-3-methyl-6-pyrimidin-4-ylpyrimidin-4-one
INCHI	1S/C19H18FN5O2/c1-24-18(26)10-16(15-6-7-21-12-22-15)23-19(24)25-8-9-27-17(11-25)13-2-4-14(20)5-3-13/h2-7,10,12,17H,8-9,11H2,1H3/t17-/m1/s1
InChi Key	NKUNFNVAHJNALA-QGZVFWFLSA-N
Smiles	CN1C(=O)C=C(N=C1N2CCOC(C2)C3=CC=C(C=C3)F)C4=NC=NC=C4
Isomeric SMILES	CN1C(=O)C=C(N=C1N2CCO[C@H](C2)C3=CC=C(C=C3)F)C4=NC=NC=C4
PubChem CID	56589672
分子量	367.38

化学和物理性质

溶解性	DMSO : 100 mg/mL (272.20 mM; Need ultrasonic)

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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