DPM-1003
DPM-1003 is a modulator of protein tyrosine phosphatase 1B (PTP1B) and C-X-C chemokine receptor 4 (CXCR4). DPM-1003 binds to the non-catalytic disordered C-terminal fragment of PTP1B. DPM-1003 inhibits the PI3Kγ-mediated AKT/mTOR signaling pathway downstream of CXCR4. DPM-1003 improves the survival rate of mice in a transfusion-related acute lung injury model, and exerts a lung injury protective effect in preclinical mouse models of acute lung injury and sepsis. DPM-1003 can be used in research related to acute lung injury, acute respiratory distress syndrome, transfusion-related acute lung injury and sepsis.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 3018836-86-4
- 分子式: C35H57N3O3
- 分子量:567.85
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
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PTP1B |
体外実験
DPM-1003 (4 μM) inhibits PMA-induced AKT phosphorylation in mouse bone marrow-derived neutrophils in vitro[1].
DPM-1003 (2-4 μM) selectively inhibits the PI3Kγ-mediated AKT signaling pathway downstream of CXCR4 in ex vivo models of mouse bone marrow-derived neutrophils and HL-60 promyelocytes, while exerting no significant effect on HeLa cells[1].
DPM-1003 (4 μM) inhibits the migration of mouse primary neutrophils toward the CXCR4 ligand CXCL12 in vitro[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
体内実験
DPM-1003 (single dose) induces an aged-neutrophil phenotype in healthy mice, characterized by neutrophilia, reduced granule content, and downregulation of fresh neutrophil surface markers[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice (TRALI model induced by LPS priming followed by anti-MHC-I antibody injection)[1]
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Dosage:5.0 mg/kg; 20 mg/kg
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Administration:i.p.; single dose
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Result:Achieved 80% mouse survival at 120 minutes post TRALI induction.
Achieved 100% mouse survival at 120 minutes post TRALI induction.
化学情報
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CAS 番号 3018836-86-4
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分子量 567.85
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分子式 C35H57N3O3
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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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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LPS-Induced Endotoxemia/Systemic Inflammation
Lipopolysaccharide (LPS)-induced endotoxemia is a widely used in vivo model of acute systemic inflammation in which LPS, a Gram-negative bacterial endotoxin, activates innate immune signaling primarily through TLR4, leading to rapid and transient induction of pro-inflammatory cytokines such as TNF-α, IL-6, and IL-1β in circulation and tissues. This cytokine surge is commonly used as a measurable readout of systemic inflammatory activation and immune dysregulation, and is typically assessed within hours after intraperitoneal LPS administration in mouse models of endotoxemia. The model captures key features of systemic inflammatory response syndrome, including cytokine release, immune cell activation, and downstream tissue responses, and has been used to evaluate anti-inflammatory interventions such as cytokine modulation, lipid mediators, and immune cell-targeting therapies.
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Inhalation Toxicity Study
Inhalation toxicity studies expose rodents to a controlled aerosol, vapor, gas, or smoke atmosphere and assess respiratory and systemic toxicity using exposure-atmosphere characterization, clinical observations, body and organ weights, bronchoalveolar lavage fluid, histopathology, blood chemistry, hematology, and, when included, molecular endpoints such as transcriptomics, proteomics, lipidomics, or tissue burden analysis. The primary biological readouts are airway irritation, pulmonary inflammation, cytotoxicity, altered surfactant or lipid homeostasis, impaired particle clearance, and tissue remodeling, reflected by BALF cell differentials, BALF protein, LDH, phosphatase activities, cytokines, lung weight, microscopic respiratory-tract lesions, and retained lung burden.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)