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MW-150, 丝裂原活化蛋白激酶 14 抑制剂

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货号 (SKU) 包装规格 是否现货 价格 数量
M412289-1mg
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M412289-5mg
 5mg 现货 Stock Image
M412289-10mg
 10mg 现货 Stock Image
M412289-25mg
 25mg 现货 Stock Image
M412289-50mg
 50mg 现货 Stock Image
M412289-100mg
 100mg 现货 Stock Image
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Autophagy (2848) MAPK/ERK Pathway (548) mitogen-activated protein kinase 14 Inhibitor (27) p38 MAPK (137)
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基本描述

英文别名 6-(4-Methyl-piperazin-1-yl)-(2-naphthalen-2-yl)-4-pyridin-4-ylpyridazine | 6-(4-methyl-1-piperazinyl)-3-(2-naphthalenyl)-4-(4-pyridinyl)-pyridazine | 6-(4-Methylpiperazin-1-Yl)-3-(Naphthalen-2-Yl)-4-(Pyridin-4-Yl)pyridazine | MS-26255 | MW 150 | BDBM50537
规格或纯度 Moligand™, ≥98%
英文名称 MW-150
生化机理 MW150 (MW01-18-150SRM) 是一种具有选择性、中枢神经系统穿透性和口服活性的 p38α MAPK 抑制剂，其 Ki 值为 101 nM。MW-150 可抑制活化胶质细胞中内源性 p38α MAPK 磷酸化内源性底物 MK2 的能力。
储存温度 -20°C储存
运输条件 超低温冰袋运输
作用类型 抑制剂
作用机制 丝裂原活化蛋白激酶 14 抑制剂
产品介绍


Information

MW150 (MW01-18-150SRM) is a selective, CNS-penetrant and orally active inhibitor of p38α MAPK with Ki of 101 nM. MW-150 inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia.
纯度 ≥98%

关联靶点（人）

MAPK14 Tchem 丝裂原活化蛋白激酶 14(Mitogen-activated protein kinase 14) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
NR3C1 Tclin Glucocorticoid receptor (14987 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRB2 Tclin Beta-2 adrenergic receptor (11824 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRB1 Tclin Beta-1 adrenergic receptor (6630 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR1A Tclin Serotonin 1a (5-HT1a) receptor (14969 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRA2A Tclin Alpha-2a adrenergic receptor (9450 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AR Tclin Androgen Receptor (11781 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHRM1 Tclin Muscarinic acetylcholine receptor M1 (12690 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DRD2 Tclin Dopamine D2 receptor (23596 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MAOA Tclin Monoamine oxidase A (11911 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CNR1 Tclin Cannabinoid CB1 receptor (20913 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
DRD1 Tclin Dopamine D1 receptor (9720 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ACHE Tclin Acetylcholinesterase (18204 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PTGS1 Tclin Cyclooxygenase-1 (9233 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC6A2 Tclin Norepinephrine transporter (10102 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HRH2 Tclin Histamine H2 receptor (5428 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MAOB Tclin Monoamine oxidase B (8835 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR1B Tclin Serotonin 1b (5-HT1b) receptor (2801 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR2A Tclin Serotonin 2a (5-HT2a) receptor (14758 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC6A4 Tclin Serotonin transporter (12625 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ADRA1A Tclin Alpha-1a adrenergic receptor (8359 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PTGS2 Tclin Cyclooxygenase-2 (13999 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HRH1 Tclin Histamine H1 receptor (7573 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OPRM1 Tclin Mu opioid receptor (19785 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
AVPR1A Tclin Vasopressin V1a receptor (5412 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OPRD1 Tclin Delta opioid receptor (15096 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
OPRK1 Tclin Kappa opioid receptor (16155 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR3A Tclin Serotonin 3a (5-HT3a) receptor (3366 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SLC6A3 Tclin Dopamine transporter (10535 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
PDE3A Tclin Phosphodiesterase 3A (3309 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHRM3 Tclin Muscarinic acetylcholine receptor M3 (7750 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTR2B Tclin Serotonin 2b (5-HT2b) receptor (10323 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CNR2 Tchem Cannabinoid CB2 receptor (16942 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MAPK11 Tchem MAP kinase p38 beta (2785 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP2C8 Tchem Cytochrome P450 2C8 (1492 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
MAPK14 Tchem MAP kinase p38 alpha (12866 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 活性数据)
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)
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)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP2C9 Tchem Cytochrome P450 2C9 (32119 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP2C19 Tchem Cytochrome P450 2C19 (29246 活性数据)
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)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CYP2B6 Tchem Cytochrome P450 2B6 (1338 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ABCG2 Tchem ATP-binding cassette sub-family G member 2 (4927 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
CHRNB2 Tclin Neuronal acetylcholine receptor; alpha4/beta2 (3972 活性数据)
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）

Cckar Cholecystokinin A receptor (90 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Pde4d Phosphodiesterase 4D (4 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Abcb1b P-glycoprotein 1 (174 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Mus musculus (284745 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Gabrp GABA-A receptor; anion channel (5731 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Grin1 Glutamate NMDA receptor (6467 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Cacna1c Voltage-gated L-type calcium channel (1164 活性数据)
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

PubChem SID 504772473
分子类型 小分子
IIUPAC Name 6-(4-methylpiperazin-1-yl)-3-naphthalen-2-yl-4-pyridin-4-ylpyridazine
INCHI 1S/C24H23N5/c1-28-12-14-29(15-13-28)23-17-22(19-8-10-25-11-9-19)24(27-26-23)21-7-6-18-4-2-3-5-20(18)16-21/h2-11,16-17H,12-15H2,1H3
InChi Key CIIVUDIZZJLXCN-UHFFFAOYSA-N
Smiles CN1CCN(CC1)C2=NN=C(C(=C2)C3=CC=NC=C3)C4=CC5=CC=CC=C5C=C4
Isomeric SMILES CN1CCN(CC1)C2=NN=C(C(=C2)C3=CC=NC=C3)C4=CC5=CC=CC=C5C=C4
分子量 381.47
Reaxy-Rn 27471330
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=27471330&ln=

化学和物理性质

分子量 381.500 g/mol
XLogP3 3.600
氢键供体数Hydrogen Bond Donor Count 0
氢键受体数Hydrogen Bond Acceptor Count 5
可旋转键计数Rotatable Bond Count 3
精确质量Exact Mass 381.195 Da
单同位素质量Monoisotopic Mass 381.195 Da
拓扑极表面积Topological Polar Surface Area 45.200 Ų
重原子数Heavy Atom Count 29
形式电荷Formal Charge 0
复杂度Complexity 513.000
同位素原子数Isotope Atom Count 0
定义的原子立体中心计数Defined Atom Stereocenter Count 0
未定义的原子立体中心计数Undefined Atom Stereocenter Count 0
定义的键立体中心计数Defined Bond Stereocenter Count 0
未定义的键立体中心计数Undefined Bond Stereocenter Count 0
所有立体化学键的总数The total count of all stereochemical bonds 0
共价键合单元计数Covalently-Bonded Unit Count 1

质检证书（CoA,COO,BSE/TSE 和分析图谱)

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找到8个结果

批号(Lot Number) 证书类型 货号
K2328294 分析证书 M412289
K2328297 分析证书 M412289
K2328302 分析证书 M412289
K2328290 分析证书 M412289
K2328291 分析证书 M412289
K2328293 分析证书 M412289
K2328295 分析证书 M412289
K2328296 分析证书 M412289

引用文献

1. Watterson DM, Grum-Tokars VL, Roy SM, Schavocky JP, Bradaric BD, Bachstetter AD, Xing B, Dimayuga E, Saeed F, Zhang H et al..  (2013)  Development of Novel In Vivo Chemical Probes to Address CNS Protein Kinase Involvement in Synaptic Dysfunction..  PLoS ONE,  8  (6): (e66226).  [PMID:23840427]
2. Zhou Z, Bachstetter AD, Späni CB, Roy SM, Watterson DM, Van Eldik LJ.  (2017)  Retention of normal glia function by an isoform-selective protein kinase inhibitor drug candidate that modulates cytokine production and cognitive outcomes..  J Neuroinflammation,  14  (1): (75).  [PMID:28381303]
3. Roy SM, Grum-Tokars VL, Schavocky JP, Saeed F, Staniszewski A, Teich AF, Arancio O, Bachstetter AD, Webster SJ, Van Eldik LJ et al..  (2015)  Targeting human central nervous system protein kinases: An isoform selective p38αMAPK inhibitor that attenuates disease progression in Alzheimer's disease mouse models..  ACS Chem Neurosci,  6  (4): (666-80).  [PMID:25676389]
4. Roy SM, Minasov G, Arancio O, Chico LW, Van Eldik LJ, Anderson WF, Pelletier JC, Watterson DM.  (2019)  A Selective and Brain Penetrant p38αMAPK Inhibitor Candidate for Neurologic and Neuropsychiatric Disorders That Attenuates Neuroinflammation and Cognitive Dysfunction..  J Med Chem,  62  (11): (5298-5311).  [PMID:30978288]

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