C5aR1 antagonist 2
C5aR1 antagonist 2 (Compound 6a) is an orally active C5a receptor 1 (C5aR1) antagonist that shows efficacy in inhibiting the C5a-induced neutrophil count increase. C5aR1 antagonist 2 is potent in the DISCO and migration assays, with IC50 values of 21 and 3 nM, respectively. C5aR1 antagonist 2 can be used for the research of acute and chronic inflammatory diseases.
For research use only. We do not sell to patients.
- CAS No.: 2365161-92-6
- Formula: C29H30F3N3O2
- Molecular Weight:509.56
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
Description
C5aR1 antagonist 2 (Compound 6a) is an orally active C5a receptor 1 (C5aR1) antagonist that shows efficacy in inhibiting the C5a-induced neutrophil count increase. C5aR1 antagonist 2 is potent in the DISCO and migration assays, with IC50 values of 21 and 3 nM, respectively. C5aR1 antagonist 2 can be used for the research of acute and chronic inflammatory diseases[1].
In Vivo
C5aR1 antagonist 2 (1-10 mg/kg, p.o., once time) fully inhibits CD11b upregulation in a rat model of C5a-induced neutrophilia in a dose-dependent manner[1].
C5aR1 antagonist 2 (1-10 mg/kg, p.o., once time) inhibits C5a-induced neutrophilia in Sprague−Dawley female hC5aR1 knock rats[1].
Pharmacokinetic Analysis in Wistar Rat Model[1]
C5aR1 antagonist 2 (1-10 mg/kg, p.o., once time) inhibits C5a-induced neutrophilia in Sprague−Dawley female hC5aR1 knock rats[1].
Pharmacokinetic Analysis in Wistar Rat Model[1]
| Route | Dose (mg/kg) | AUC0-last (ng·h/mL) | Cmax (ng/mL) | Tmax (h) | CL(mL/(min*kg)) | Vss_obs (L/kg) | t1/2 (h) |
| p.o. | 10 | 35700 | 3610 | 2.5 | 39 | 7.1 | 3.7 |