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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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。
- 純度: 99.96%
- CAS 番号: 1254036-23-1
- 分子式: C49H63FN10O9
- 分子量:955.08
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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
化学情報
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CAS 番号 1254036-23-1
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性状 Solid
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分子量 955.08
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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 -
J Transl Med
Targeting C5AR1 disrupts complement-driven G0-phase maintenance and overcomes metabolic drug resistance in glioma. [Abstract]2026 May 22. PMID: 42174621 -
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 -
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (282 KB)
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取扱説明書 (2659 KB)
参考文献
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 関連分類
HY-148141 関連分類
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