C5aR1 antagonist 1
C5aR1 antagonist 1 (Compound 7e) is an orally active C5a receptor 1 (C5aR1) antagonist. C5aR1 antagonist 1 is active in DISCO and migration assays, with IC50 values of 38 nM and 17 nM, respectively. C5aR1 antagonist 1 can be used for the research of acute and chronic inflammatory diseases.
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- CAS No.: 2365325-67-1
- Formule: C28H27F4N3O
- Masse moléculaire:497.53
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Description
IC50 & Target
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C5aR1 |
In Vitro
C5aR1 antagonist 1 (compound 7e) is a surmountable and competitive antagonist of C5aR, with the KD value of 15 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
C5aR1 antagonist 1 (1/3/10 mg/kg, administered orally 2/8/16h before blood sampling for neutrophil quantification) dose-dependent inhibits the increase of neutrophils in the blood of the neutrophilic rat model[1].
C5aR1 antagonist 1 (0/1/3/10/30 mg/kg, administered orally 2 h before blood sampling) inhibites the upregulation of CD11b of the female hC5aR1 knock-in rats by around 90%[1].
Pharmacokinetic Properties of Compound 7e[1]
| Animals | Route | Dose (mg/kg) | CL mL/(min×kg) | Vss_obs (L/kg) | T1/2 (h) | AUC0‑last (ng×h)/mL | Cmax (ng×h)/mL | Tmax (h) |
| rat | p.o. | 10 | 39 | 7.1 | 4.1 | 32200 | 3890 | 2 |
| dog | p.o. | 30 | 2.3 | 7.6 | 1.1 | 14900 | 2530 | 1 |
| monkey | p.o. | 50 | 3500 | 635 | 2 | 41900 | 3940 | 4 |