JPE-1375
Based on 5 publication(s) in Google Scholar
JPE-1375 is a complement C5a receptor 1 (C5aR1) antagonist. JPE-1375 effectively inhibits polymorphonuclear leukocyte mobilization (EC50=6.9 μM) and reduces TNF levels (EC50=4.5 μM) in mice. JPE-1375 can be used in studies of autoimmune and inflammatory diseases.
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- Pureté: 99.96%
- CAS No.: 1254036-23-1
- Formule: C49H63FN10O9
- Masse moléculaire:955.08
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) JPE-1375
More
Activité biologique
C5aR1[1].
JPE-1375 (1 mg/kg; i.v.; single) demonstrates a rapid distribution in the plasma, followed by elimination in mice[1].
JPE-1375 (1 mg/kg; i.v.; single) shows a strong negative correlation between PMN mobilization and TNF production with plasma concentrations[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J wild-type (10 to 12-week-old; C5a pharmacodynamic model)[1].
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Dosage:0.3, 1.0, 3.0 mg/kg
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Administration:Intravenous injection; single.
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Result:Significantly decreased C5a-mediated PMN mobilization at 1 and 3 mg/kg doses, while no effect was observed at a 0.3 mg/kg dose.
Showed a significant reduction in TNF plasma levels at 1 and 3 mg/kg dose with both compounds reducing C5a-mediated TNF by about 90%.
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Animal Model:C57BL/6J wild-type mice(10 to 12-week-old)[1].
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Dosage:1 mg/kg
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Administration:Intravenous injection; single.
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Result:
1.19 Pharmacokinetic Parameters of JPE-1375 in C57BL/6J wild-type mice[1].
IV (1 mg/kg) T1/2 (h) 0.13 Cmax (µg/mL) 7.18 AUC0-t (μg/mL•h) 2.40 AUC0-inf, obs (μg/mL•h) 2.41 AUC0-t/0-inf, obs (μg/mL•h) 1.00 AUMC0-inf, obs (μg/mL•h2) 0.13 MRT0-inf, obs (h) 0.05 Vz, obs ((μg)/(μg/mL)) 2.38 CL, obs ((μg)/(μg/mL)/h) 12.47 Vss, obs ((μg)/(μg/mL)) 0.66
Chemical Information
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CAS No. 1254036-23-1
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Appearance Solid
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Masse moléculaire 955.08
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Formule C49H63FN10O9
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Color White to off-white
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SMILES
O=C([C@@H]1CC(NC(N1)=O)=O)N[C@@H](CC2=CC=CC=C2)C(N[C@@H](CCCN)C(N3[C@@H](CCC3)C(N[C@@H](CCC(C)C)C(N[C@H](C(N[C@H](C(N)=O)CC4=CC=CC=C4)=O)CC5=CC=C(C=C5)F)=O)=O)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (5)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
UPR-induced intracellular C5aR1 promotes adaptation to the hypoxic tumour microenvironment. [Abstract]2025 Jul 22;16(1):547. PMID: 40695778 -
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Invest Ophthalmol Vis Sci
The Intracellular C5a-mtC5aR1 Axis Promotes Necroptosis in Dry Eye Through DRP1-Mediated Mitochondrial Dysfunction. [Abstract]2026 Feb 2;67(2):35. PMID: 41705776 -
Med Microbiol Immunol
Exploration of compounds to inhibit the Panton-Valentine leukocidin of Staphylococcus aureus. [Abstract]2024 Sep 19;213(1):19. PMID: 39297970 -
Solvant et solubilité
DMSO : 100 mg/mL (104.70 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 (protect from light). 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 (protect from light). 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)
Pureté et documentation
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Fiche technique (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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Instruction de manipulation (2659 KB)
Références
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 (protect from light). 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.0470 mL | 5.2352 mL | 10.4703 mL | 26.1758 mL |
| 5 mM | 0.2094 mL | 1.0470 mL | 2.0941 mL | 5.2352 mL | |
| 10 mM | 0.1047 mL | 0.5235 mL | 1.0470 mL | 2.6176 mL | |
| 15 mM | 0.0698 mL | 0.3490 mL | 0.6980 mL | 1.7451 mL | |
| 20 mM | 0.0524 mL | 0.2618 mL | 0.5235 mL | 1.3088 mL | |
| 25 mM | 0.0419 mL | 0.2094 mL | 0.4188 mL | 1.0470 mL | |
| 30 mM | 0.0349 mL | 0.1745 mL | 0.3490 mL | 0.8725 mL | |
| 40 mM | 0.0262 mL | 0.1309 mL | 0.2618 mL | 0.6544 mL | |
| 50 mM | 0.0209 mL | 0.1047 mL | 0.2094 mL | 0.5235 mL | |
| 60 mM | 0.0175 mL | 0.0873 mL | 0.1745 mL | 0.4363 mL | |
| 80 mM | 0.0131 mL | 0.0654 mL | 0.1309 mL | 0.3272 mL | |
| 100 mM | 0.0105 mL | 0.0524 mL | 0.1047 mL | 0.2618 mL |
JPE-1375 Related Classifications
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