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

For research use only. We do not sell to patients.

C5aR1 antagonist 1 Chemical Structure

C5aR1 antagonist 1 Chemical Structure

CAS No. : 2365325-67-1

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

C5aR1 antagonist 1 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target

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.

C5aR1 antagonist 1 Related Antibodies
In Vivo

The pharmacokinetic profile of C5aR1 antagonist 1 (compound 7e) (10/30/50 mg/kg, single administration) in vivo in rat, dog, and cynomolgus monkey indicates that the low solubility of the compound waslimiting the exposure[1].
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

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

Animal Model: Neutrophilia Rat Model[1]
Dosage: 1/3/10 mg/kg
Administration: Oral gavage (p.o.), Rats were administered po with compound or vehicle at 23.5/15.5/7.5/1.5 h before hC5a iv injection.
Result: Inhibited reactive neutrophilia induced by hC5a administration in vivo.
Molecular Weight

497.53

Formula

C28H27F4N3O
CAS No.
SMILES

O=C1N(CC2=C(C(F)(F)F)C=CC=C2)C3=C(CN1C4CCN(CC4)C5=C(C)C=CC=C5F)C=CC=C3
Shipping

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

C5aR1 antagonist 1 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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 12365325-67-1Complement SystemHumanized C5aR1 RatsC5aR1 Knockout RatsInflammationNeutrophilia Rat ModelInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
C5aR1 antagonist 1
Cat. No.:
HY-163378
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.