DPM-1003
Based on 1 Customer Validation
DPM-1003 is an allosteric PTP1B inhibitor that acts through the non-catalytic C-terminal disordered segment. DPM-1003 inhibits CXCL12-directed migration, CXCR4-dependent PI3Kγ/AKT/mTOR, CXCR4-mediated AKT, CXCL2-stimulated AKT/ERK, and PMA-induced Akt phosphorylation. In APP/PS1 mice, DPM-1003 improves recognition/spatial memory and reduces fibrillar/non-fibrillar plaques and soluble/insoluble Aβ42. DPM-1003 can be used in research on transfusion-related acute lung injury (TRALI), Rett syndrome, and Alzheimer's disease.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.89%
- No. CAS: 3018836-86-4
- Fòrmula: C35H57N3O3
- Peso molecular:567.85
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Almacenamiento:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
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PTP1B |
CXCR4 |
In Vitro
DPM-1003 (4 μM; 30 min-2 h) reduces CXCL12-directed neutrophil migration and enhances fMLP-directed migration[1].
DPM-1003 suppresses CXCR4/CXCL12-mediated AKT signaling in neutrophils, HeLa, and HL-60 cells and differentially modulates CXCL2- and fMLP-stimulated AKT/ERK1/2 phosphorylation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c bearing transfusion-related acute lung injury (TRALI)[1]
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Dosage:5.0 mg/kg; 20 mg/kg
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Administration:i.p.; single dose; 2 hours before anti-MHC-I antibody injection
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Result:In the survival analysis, 120-minute survival was 100% at 20 mg/kg and 80% at 5.0 mg/kg.
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Animal Model:B6.129P2(C)-Mecp2tm1.1Bird/J (Mecp2-/+; C57BL/6J background; female; 12-14 weeks at initiation)[2]
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Dosage:5 mg/kg
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Administration:i.p.; twice weekly; 12 weeks
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Result:Attenuated pathological body-weight gain in Mecp2-/+ mice over 12 weeks.
Improved rotarod motor performance over 12 weeks.
After withdrawal, rotarod performance declined gradually but remained improved relative to vehicle-treated Mecp2-/+ controls.
Normalized QTc intervals in affected Mecp2-/+ mice and reduced QTc across the cohort without evidence of cardiotoxicity.
Prevented worsening of apnea frequency and reduced apnea duration, restoring respiratory parameters to levels comparable with wild-type animals.
- Kinase activity and phosphorylation assays
- Western Blot
- Zigmond Chamber Chemotaxis Assay
- Cell migration
- Under-Agarose Cell Migration Assay
- Protocol for Water Maze
- Protocol for Kinase activity and phosphorylation assays
- Inhalation Toxicity Study
- Dunn/Insall Chamber Chemotaxis Assay
- Alzheimer’s Disease Modeling
Chemical Information
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No. CAS 3018836-86-4
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Appearance Oil
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Peso molecular 567.85
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Fòrmula C35H57N3O3
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Color White to off-white
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SMILES
O[C@H]1[C@]2([H])[C@@](CC[C@]3([C@@]2([H])CC[C@]3([H])[C@H](C)CCC(OC)=O)C)([H])[C@@]4([C@@](CC(CC4)NCCCCNCC5=CN=CC=C5)([H])C1)C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 41.67 mg/mL (73.38 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.7610 mL | 8.8051 mL | 17.6103 mL | 44.0257 mL |
| 5 mM | 0.3522 mL | 1.7610 mL | 3.5221 mL | 8.8051 mL | |
| 10 mM | 0.1761 mL | 0.8805 mL | 1.7610 mL | 4.4026 mL | |
| 15 mM | 0.1174 mL | 0.5870 mL | 1.1740 mL | 2.9350 mL | |
| 20 mM | 0.0881 mL | 0.4403 mL | 0.8805 mL | 2.2013 mL | |
| 25 mM | 0.0704 mL | 0.3522 mL | 0.7044 mL | 1.7610 mL | |
| 30 mM | 0.0587 mL | 0.2935 mL | 0.5870 mL | 1.4675 mL | |
| 40 mM | 0.0440 mL | 0.2201 mL | 0.4403 mL | 1.1006 mL | |
| 50 mM | 0.0352 mL | 0.1761 mL | 0.3522 mL | 0.8805 mL | |
| 60 mM | 0.0294 mL | 0.1468 mL | 0.2935 mL | 0.7338 mL |
DPM-1003 Related Classifications
HY-160550 Related Classifications
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