大连美仑生物技术有限公司

Apoptosis Bcl-2 Bcl-6 Caspase Ferroptosis Mdm2 p53 RIP kinase Survivin TNF-alpha Cuproptosis IAP Metabolic Enzyme/Protease PDHK ROS Kinase Phosphatase MDM-2/p53 Kinesin PKC HSP Autophagy TNF Receptor FKBP Bcl-2 Family Pyroptosis DAPK PKD EBV Glutathione Peroxidase Transferrin Receptor c-Myc Necroptosis ASK1 Thymidylate Synthase

Autophagy

Autophagy LRRK2 Estrogen/progestogen PINK1/Parkin Dynamin Anti-infection Oxidative Phosphorylation Akt AMPK JAK Toll-like Receptor (TLR) ULK p62 Atg8/LC3 Atg7 Atg4 AUTACs

Epigenetics

DNA Methyltransferase DNMT Epigenetic Reader Domain Histone Acetyltransferase Histone demethylases Histone Methyltransferase PKC AMPK HDAC JAK MicroRNA Protein Arginine Deiminase Phosphodiesterase (PDE)

GPCR/G Protein

Adenosine Receptor Angiotensin Receptor Cannabinoid Receptor CaSR E1 Activating CRFR E2 conjugating E3 Ligase Endothelin Receptor GHSR Glucagon Receptor GLP-1R GPCR19(TGR5) GPR GPR119 GPR40(FFAR1) Imidazoline Receptor Leukotriene Receptor LPA Receptor OX Receptor Protease-activated Receptor Rac Prostaglandin Receptor Oxytocin Receptor Ras Rho S1P Receptor Sigma Receptor 5-HT Receptor Neurokinin Receptor mAChR GCGR LPL Receptor Dopamine Receptor Guanylate Cyclase Histamine Receptor CXCR CCR GPR35 P2Y Receptor Opioid Receptor GPR68 mGluR Formyl Peptide Receptor (FPR) Platelet-activating Factor Rec GnRH Receptor Protease Activated Receptor (P Vasopressin Receptor Chemerin Receptor Melatonin Receptor MCHR1 (GPR24) Orexin Receptor (OX Receptor) RGS Protein CGRP Receptor Free Fatty Acid Receptor

Immunology/Inflammation

AhR CCR COX Complement 5(C5) CXCR Histamine Receptor IL Receptor Immunology IL-5 NOD1 IL-12 PD-1 IL-17 PDL-1 reactive oxygen species (ROS) NLRP3 TLR STING Toll-like Receptor (TLR) Bcr-Abl Salt-inducible Kinase (SIK) Glucocorticoid Receptor IRAK SphK Interleukin Related PGE synthase Macrophage migration inhibitor Complement System MyD88 FLAP Thrombopoietin Receptor Arginase NO Synthase AP-1 Nuclear Factor of activated T IFNAR CD276/B7-H3 CD3 CD38 CD28 CD22 CD20 CD19 Aryl Hydrocarbon Receptor PD-1/PD-L1 NOD-like Receptor (NLR) Mesothelin Mucin NTPDase PSMA SOD DOCK CD74 CD6 CD73 CTLA-4 CX3CR1 Cyclic GMP-AMP Synthase FAP Galectin Cyclophilin P-selectin CD2 CD47 Tim3 TROP2 Glycoprotein VI Kallikrein LAG-3 VAP-1 BCL6

Integrin

JAK-STAT/IL6

JAK STAT IL-6 Pim EGFR

MAPK

ErbB2 ERK JNK MEK p38 MAPK Mixed Lineage Kinase Raf

Membrane Transporter/Ion Chann

Amino acid transporter antagon ATPase Calcium Channel CFTR Chloride channel CRM1 GABA Receptor GluR iGluR NMDAR P-gp Potassium Channel Proton Pump SGLT Sodium Channel TRPV P-glycoprotein Na+/K+ ATPase Piezo Channel Fat Mass and Obesity-associate TRP Channel BCRP nAChR CRAC Channel Apical Sodium-Dependent Bile A P2X Receptor Monocarboxylate Transporter Na+/HCO3- Cotransporter GlyT OAT NKCC Monoamine Transporter HCN Channel EAAT Ferroportin GLUT Na+/H+ Exchanger (NHE) Na+/Ca2+ Exchanger FATP ATP Synthase ASCT VDAC Urea Transporter URAT1 Aquaporin Calmodulin

Metabolic Enzyme/Protease

5-alpha Reductase Aminopeptidase ATP-citrate lyase in Carbonic Anhydrase CETP DGAT DPP-4 Factor Xa FOX FXR Glucokinase(GK) GSNOR HCV Protease HIF HMG-CoA Reductase HSP IDO Lactate Dehydrogenase Integrase MMP NAMPT P450 PAI-1 PDE PGC-1α Phospholipase Procollagen C Protein Proteases PKM Proteasome RAR/RXR Retinoid Receptor Serine Protease Thrombin Transferase Xanthine Oxidase p38-MAPK Stearoyl-CoA Desaturase (SCD) Mitochondrial Metabolism (MPC) Tyrosinase Endogenous Metabolite Phosphatase Pyruvate Kinase PDI Phosphodiesterase (PDE) HIF/HIF Prolyl-Hydroxylase Hexokinase Ser/Thr Protease Carboxylesterase Cathepsin Cytochrome P450 Drug Metabolite E1/E2/E3 Enzyme Angiotensin-converting Enzyme HMG-CoA Reductase (HMGCR) Aldose Reductase Oxidative Phosphorylation NADPH Oxidase Lipoxygenase DAGL MAGL MALT1 Adenosine Kinase COMT Glutathione S-transferase Adenosine Deaminase Acyltransferase Enolase Aldehyde Dehydrogenase (ALDH) Farnesyl Transferase Glucosidase PDHK Fatty Acid Synthase (FASN) Dipeptidyl Peptidase Methylenetetrahydrofolate Dehy Dihydroorotate Dehydrogenase Renin FAAH SGK Dopamine β-hydroxylase HIV Integrase Adiponectin Receptor ROR LXR Mineralocorticoid Receptor REV-ERB Amine N-methyltransferase

Neuronal Signaling

5-HT Receptor AChR BACE Beta Amyloid Beta-secretase CaMK CGRP Receptor Dopamine Receptor FAAH Gamma-secretase GlyT iGluR MAO mAChR Opioid Receptor Serotonin Transporter Legumain γ-secretase Notch Monoamine Oxidase Trk Receptor Cholinesterase (ChE) Imidazoline Receptor Amyloid-β Dopamine Transporter Sigma Receptor Glucosylceramide Synthase (GCS

NF-κB

NF-κB Nrf2 IκB/IKK Reactive Oxygen Species Keap1-Nrf2 IKK RANKL/RANK

Others

Androgen Receptor Aromatase CD20 CD52 c-Myc CPT1 c-RET CTLA-4 Decarboxylase Dehydrogenase FPR GLUT Glutaminase HIV ProteaseAnti-infection HSP90 Hydroxylase IAP IgE IRE1 LDL Lipase Lipoxygenase Lysyl Hydroxylase MT Receptor NADPH oxidase others P2 Receptor PAFR PCSK9 RAAS RANK Ligand Reverse Transcriptase S6 Kinase Thioredoxin Tie-2 SARM Vasopressin Receptor VDA Vitamin D Related CDA TrxR PDE IDO

PI3K/Akt/mTOR

Akt MELK mTOR GSK-3 PDK-1 PI3K PIKfyve PTEN RSK AMPK PI4K PIN1

Protein Tyrosine Kinase/PTK

ACK ALK Axl Bcr-Abl BTK cAMP(PKA) c-Kit c-Met CSF-1R DYRK EGFR Ephrin receptor FAK FGFR FLT3 HER2 IGF-1R MET Insulin Receptor PDGFR PKA ROS Src Syk Trk receptor VEGFR

Stem Cell /Wnt

c-Jun Hedgehog/Smoothened Hippo pathway Met stemness kinase OCT Wnt/β-catenin Adenylate Cyclase YAP PKA TGF-beta/Smad Gli Wnt sFRP-1 Smo Organoid Hedgehog Porcupine PKG Hippo (MST) Oct3/4 β-catenin BMI1

TGF-beta/Smad

TGF-beta/Smad TGF-β Receptor PKC PKA

Cell Cycle/DNA Damage

Antifolate APC ATM/ATR Aurora Kinase BMI-1 Casein Kinase CDK CD38 Chk DHFR DNA alkylator DNA-PK DNA/RNA Synthesis DUB Dynamin HDAC HSP Kinesin Microtubule Associated p97 MTH1 PAK PERK PLK PPAR PARP ROCK Sirtuin RAD51 Telomerase TOPK Topoisomerase Wee1 Deubiquitinase NEKs OGG Polo-like Kinase (PLK) Microtubule/Tubulin Mps1 MASTL Haspin Kinase SRPK DNA Alkylator/Crosslinker ATF6 Checkpoint Kinase (Chk) G-quadruplex Nucleoside Antimetabolite/Anal Eukaryotic Initiation Factor ( CRISPR/Cas9 IRE1 MARK Epoxide Hydrolase

Protein Tyrosine Kinase/RTK

TAM Receptor ROS Kinase JAK Src VEGFR c-Met Syk ALK FAK IGF-1R FLT3 c-Met/HGFR PDGFR Bcr-Abl c-Fms Ephrin receptor FLT3 BTK Itk Anaplastic lymphoma kinase (AL Ack1 RET c-Kit FGFR EGFR Insulin Receptor Discoidin Domain Receptor BRK BMX Kinase SHP2 DYRK Tie Pyk2 GDNF Receptor

Epigenetics Histone

Methyltransferase

Anti-infection

HSV Flavivirus others Fungal Parasite HBV Bacterial Dengue virus HIV Filovirus Antibiotic VSV SARS-CoV Beta-lactamase HCV CMV Reverse Transcriptase Influenza Virus Arenavirus HIV Protease

MAPK/ERK Pathway

ERK p38 MAPK MEK MAP3K Ribosomal S6 Kinase (RSK) Raf JNK MAP4K KLF Mixed Lineage Kinase MNK

Vitamin D Related/Nuclear Rece

Estrogen Receptor/ERR Progesterone Receptor VD/VDR Androgen Receptor Thyroid Hormone Receptor Nuclear Hormone Receptor 4A/NR Constitutive Androstane Recept

Cytoskeleton

MARCKS Integrin Gap Junction Protein Myosin Polo-like Kinase (PLK) Annexin A Dynamin Arp2/3 Complex

Antibodydrug Conjugate/ADC Rel

ADC Cytotoxin Antibody-Drug Conjugates (ADCs Drug-Linker Conjugates for ADC

PROTAC

Molecular Glues PROTACs Ligands for Target Protein for PROTAC Linkers Ligands for E3 Ligase E3 Ligase Ligand-Linker Conjug PROTAC-Linker Conjugates for P Target Protein Ligand-Linker C SNIPERs LYTACs AUTOTACs

通用试剂类

氨基酸

氨基酸犬尿氨酸系列

胆酸系列

蛋白及衍生物

合成多肽

核酸及其衍生物

抗生素及抗病毒

抗生素及抗病毒抗真菌抗生素抗细菌抗生素抗肿瘤抗生素抗病毒化合物

酶辅酶

染色剂指示剂

生物缓冲剂

碳水化合物

碳水化合物多糖寡糖去垢剂

通用试剂

微生物检测

微生物培养基

维生素

显色及标记试剂

植物生长激素

其他生化试剂

其他生化试剂表面活性剂无机盐

还原剂

蛋白修饰

交联剂

表面活性剂/去垢剂

非离子表活剂/去垢剂阴离子表活剂/去垢剂阳离子表活剂/去垢剂

生物耗材

吸头类

常规吸头滤芯吸头（PCR用）

PCR类

离心管类

常规离心管

细胞培养类

细胞培养板细胞培养皿细胞冻存培养瓶

液体处理类

移液管

体外诊断

核心原料

亲和素

植物研究相关

植物激素

赤霉素类(GA) 细胞分裂素(CTK) 油菜素甾醇(BR) 其他植物激素脱落酸（ABA）乙烯(ETH)

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Pamapimod (R-1503, Ro4402257)

总货号: MB2608

货号	规格	发货时间
MB2608-1	1MG [￥900.00] :￥900.00	现货，一周内发货
MB2608-2	5MG [￥3000.00] :￥3000.00	现货，一周内发货

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相关论文

Pamapimod (R-1503, Ro4402257)
分子式：C19H20F2N4O4分子量：406.38

简介： Pamapimod (R-1503, Ro4402257)是新型的、选择性的p38 MAPK抑制剂。它能抑制p38α和p38β， IC50分别为0.014±0.002和0.48± 0.04 μM。对p38delta和p38gamma没有活性。
物理性状及指标：
外观：……………………粉末
溶解性：…………………H2O : Insoluble；DMSO: 81 mg/mL (199.32 mM)；Ethanol：28 mg/mL (68.90 mM)
含量：……………………>98%
储存温度：-20℃，避光防潮密闭干燥

生物活性

描述

Pamapimod (R-1503, Ro4402257)是新型的、选择性的p38 MAPK抑制剂。它能抑制p38α和p38β， IC50分别为0.014±0.002和0.48± 0.04 μM。对p38delta和p38gamma没有活性。

IC50 & Target

p38α (Cell-free assay)	p38β (Cell-free assay)
0.014 μM	0.48 μM

体外

Pamapimod抑制p38，但没有观测到JNK被抑制。Pamapimod也能抑制LPS刺激下单核细胞TNFα的产生、人全血细胞中IL-1β的生成以及RA患者滑膜外植体的自发性TNFα的产生。

体内

在小鼠胶原诱导性关节炎中，50 mg/kg pamapimod能减少炎症临床症状以及减少骨质流失。在痛觉过敏的大鼠模型中，pamapimod能增强其耐压力，说明p38在炎症相关的疼痛中的重要作用。Pamapimod能抑制RA患者滑膜外植体的自发性TNFα的产生。在啮齿类动物中，pamapimod抑制LPS-和TNFα-刺激下TNFα和IL-6的生成。

细胞实验

Cell lines: 人单核细胞株, THP-1
Concentrations: 15 μM
Incubation Time: 150 min
Method:

将生长至对数期的THP-1细胞用离心法收集好后，重悬于含5.5×10-5 M 巯基乙醇及10%胎牛血清的RPMI培养基中，最终细胞密度为2.5×106 cells/ml。预先配好25 μL稀释好的pamapimod溶液，在加入到细胞前，先加至圆底96孔板中。最开始的浓度为100 μM（5% DMSO）,然后配置6个半对数稀释浓度进行处理。每孔加入200 μL细胞悬浮液和25 μL 5μg/ml的LPS到培养基中，DMSO的终浓度为0.5%，化合物再稀释10倍，LPS终浓度为500 ng/ml。将细胞悬浮液和化合物稀释液混合在一起，在37℃、5% CO2的细胞培养箱中共同孵育30分钟。然后加入LPS，孵育2小时，离心，将细胞上清液储存于4度，用于分析TNF-alpha含量。
(Only for Reference)

动物实验

Animal Models: BALB/c小鼠
Formulation: 0.9% NaCl, 0.5% 羧甲基纤维素钠, 0.4% 聚山梨醇酯80, 0.9%苯甲醇, 97.3% 蒸馏水
Dosages: 25, 50, 100, 150 mg/kg
Administration: 口服
(Only for Reference)

美仑相关产品推荐 (更多相关靶点抑制剂请详询官网或客服)

MB1084	达马莫德;BIRB796
MB1650	PH-797804
MB2609	Losmapimod (GW856553X)

储液配置及储存：按表中溶解性配置；如溶解困难，可以通过快速搅拌，超声或温和加热（在45-60°C下水浴）。液体稳定性报道的很少，建议现配现用，如需储存，建议：-20℃1-3月；-80℃ 3-6月。

	1 mg	5 mg	10 mg
1 mM	2.4608 mL	12.3038 mL	24.6075 mL
5 mM	0.4922 mL	2.4608 mL	4.9215 mL
10 mM	0.2461 mL	1.2304 mL	2.4608 mL
50 mM	0.0492 mL	0.2461 mL	0.4922 mL

●我司产品为非无菌包装，若用于细胞培养，请提前做预处理，除去热原细菌，否则会导致染菌。

●部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，以上数据仅供参考交流研究之用。

我司所售出产品仅供于科研研究用途（非临床科研研究），每次销售产品行为都适用于我司网上所列明的通用销售条款。

CAS 号：449811-01-2

英文名字：Pamapimod (R-1503, Ro4402257)

质量标准：>98%,BR

分子式：C19H20F2N4O4

摩尔浓度计算器（本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系）

摩尔浓度计算公式：质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

质量（g）

浓度 (mol/L)

体积 (L)

分子量 (g/mol)