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.
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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