2. Immunology/Inflammation
  3. Complement System
  4. 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.

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C5aR1 antagonist 2 Chemical Structure

C5aR1 antagonist 2 Chemical Structure

CAS No. : 2365161-92-6

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C5aR1 antagonist 2 Related Antibodies

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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]

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

509.56

Formula

C29H30F3N3O2
CAS No.
Unlabeled CAS

SMILES

O=C1N(CC2=C(C(F)(F)F)C=CC=C2)C3=C(N1C4CCN(CC4)C5=C(C)C=CC=C5C)C=CC=C3OC
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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C5aR1 antagonist 2 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

C5aR1 antagonist 22365161-92-6Complement SystemDISCOmigrationneutrophilinflammatoryInhibitorinhibitorinhibit

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