L-Phenylalaninamide, (4S)-hexahydro-2,6-dioxo-4-pyrimidinecarbonyl-L-phenylalanyl-L-ornithyl-L-prolyl-5-methyl-L-norleucyl-4-fluoro-L-phenylalanyl-
- CAS No.
- 1254036-23-1
- Chemical Name:
- L-Phenylalaninamide, (4S)-hexahydro-2,6-dioxo-4-pyrimidinecarbonyl-L-phenylalanyl-L-ornithyl-L-prolyl-5-methyl-L-norleucyl-4-fluoro-L-phenylalanyl-
- Synonyms
- JPE-1375;Hoo-Phe-Orn-Pro-HomoLeu-Phe(4-F)-Phe-NH2;L-Phenylalaninamide, (4S)-hexahydro-2,6-dioxo-4-pyrimidinecarbonyl-L-phenylalanyl-L-ornithyl-L-prolyl-5-methyl-L-norleucyl-4-fluoro-L-phenylalanyl-
- CBNumber:
- CB912151797
- Molecular Formula:
- C49H63FN10O9
- Molecular Weight:
- 955.1
- MDL Number:
- MOL File:
- 1254036-23-1.mol
L-Phenylalaninamide, (4S)-hexahydro-2,6-dioxo-4-pyrimidinecarbonyl-L-phenylalanyl-L-ornithyl-L-prolyl-5-methyl-L-norleucyl-4-fluoro-L-phenylalanyl- Properties
| Density | 1.280±0.06 g/cm3(Predicted) |
|---|---|
| storage temp. | 4°C, protect from light |
| solubility | DMSO : 100 mg/mL (104.70 mM; Need ultrasonic) |
| form | Solid |
| pka | 10.38±0.40(Predicted) |
| color | White to off-white |
L-Phenylalaninamide, (4S)-hexahydro-2,6-dioxo-4-pyrimidinecarbonyl-L-phenylalanyl-L-ornithyl-L-prolyl-5-methyl-L-norleucyl-4-fluoro-L-phenylalanyl- Chemical Properties,Uses,Production
Uses
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[1].
in vivo
JPE-1375 (0.3, 1.0, 3.0 mg/kg; i.v.; single) inhibits PMN (polymorphonuclear leukocytes) mobilization and TNF with EC50 values of 6.9 and 4.5 μM, respectively[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].
| Animal Model: | C57BL/6J wild-type (10 to 12-week-old; C5a pharmacodynamic model)[1]. |
| Dosage: | 0.3, 1.0, 3.0 mg/kg |
| Administration: | Intravenous injection; single. |
| 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%. |
| Animal Model: | C57BL/6J wild-type mice(10 to 12-week-old)[1]. | ||||||||||||||||||||||
| Dosage: | 1 mg/kg | ||||||||||||||||||||||
| Administration: | Intravenous injection; single. | ||||||||||||||||||||||
| Result: | 1.19Pharmacokinetic Parameters of JPE-1375 in C57BL/6J wild-type mice[1].
|
References
[1] Cui CS, et al. In Vivo Pharmacodynamic Method to Assess Complement C5a Receptor Antagonist Efficacy. ACS Pharmacol Transl Sci. 2021 Dec 21;5(1):41-51. DOI:10.1021/acsptsci.1c00227
L-Phenylalaninamide, (4S)-hexahydro-2,6-dioxo-4-pyrimidinecarbonyl-L-phenylalanyl-L-ornithyl-L-prolyl-5-methyl-L-norleucyl-4-fluoro-L-phenylalanyl- Preparation Products And Raw materials
Raw materials
Preparation Products
L-Phenylalaninamide, (4S)-hexahydro-2,6-dioxo-4-pyrimidinecarbonyl-L-phenylalanyl-L-ornithyl-L-prolyl-5-methyl-L-norleucyl-4-fluoro-L-phenylalanyl- Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354; | support@targetmol.com | United States | 39035 | 58 |
| Beijing Solarbio Science & Tecnology Co., Ltd. | 010-50973130 18101056239 | 3193328036@qq.com | China | 29759 | 68 |
| Hangzhou Peptidego Biotech Co.,Ltd. | 0571-87213919 | Eric@peptidego.com | China | 7408 | 58 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24961 | 58 |
| Hangzhou Sinoda Pharmaceutical Technology Co. LTD | 0571-87213919 17306812703 | 3007955328@qq.com | China | 6979 | 58 |
| Shanghai Yifei Biotechnology Co. , Ltd. | 021-65675885 18964387627 | customer_service@efebio.com | China | 11973 | 58 |
| Shanghai?Medlife?Pharm-Tech?Co.,?Ltd | 021-59167510 18117107507 | vip@med-life.cn | China | 5002 | 58 |
| RD International Technology Co., Limited | 18024082417 | market@ubiochem.com | China | 9835 | 58 |
| Guangzhou Lucheng Biotechnology Co., Ltd. | 16620452357 | CHINA | 0 | 58 |





