For research use only. Not for therapeutic Use.
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].
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].
| Catalog Number | I042877 |
| CAS Number | 1254036-23-1 |
| Synonyms | (4S)-N-[(2S)-1-[[(2S)-5-amino-1-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-(4-fluorophenyl)-1-oxopropan-2-yl]amino]-5-methyl-1-oxohexan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-2,6-dioxo-1,3-diazinane-4-carboxamide |
| Molecular Formula | C49H63FN10O9 |
| Purity | ≥95% |
| InChI | InChI=1S/C49H63FN10O9/c1-29(2)17-22-34(43(63)56-38(27-32-18-20-33(50)21-19-32)45(65)55-36(42(52)62)25-30-11-5-3-6-12-30)53-47(67)40-16-10-24-60(40)48(68)35(15-9-23-51)54-44(64)37(26-31-13-7-4-8-14-31)57-46(66)39-28-41(61)59-49(69)58-39/h3-8,11-14,18-21,29,34-40H,9-10,15-17,22-28,51H2,1-2H3,(H2,52,62)(H,53,67)(H,54,64)(H,55,65)(H,56,63)(H,57,66)(H2,58,59,61,69)/t34-,35-,36-,37-,38-,39-,40-/m0/s1 |
| InChIKey | HXKFHHNEFCZKPG-OAKHNGAUSA-N |
| SMILES | CC(C)CCC(C(=O)NC(CC1=CC=C(C=C1)F)C(=O)NC(CC2=CC=CC=C2)C(=O)N)NC(=O)C3CCCN3C(=O)C(CCCN)NC(=O)C(CC4=CC=CC=C4)NC(=O)C5CC(=O)NC(=O)N5 |
| Reference | [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. |
