Free shipping on all orders over $ 500

CCR2 antagonist 5 

Cat. No. M27990
CCR2 antagonist 5  Structure
Size Price Availability Quantity
Free Delivery on orders over USD 500 Bulk Inquiry?
Quality Control & Documentation
Biological Activity

CCR2 antagonist 5 is a selective, orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM). CCR2 antagonist 5 displays a Ki of 9.6 µM for mCCR2 binding. CCR2 antagonist 5 can be used in the research of inflammatory disease.

Chemical Information
Molecular Weight 482.52
Formula C22H25F3N4O3S
CAS Number 1228650-83-6
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Tobias Puengel, et al. Int J Mol Sci. Combined Therapy with a CCR2/CCR5 Antagonist and FGF21 Analogue Synergizes in Ameliorating Steatohepatitis and Fibrosis

[2] Ruaa Al-Qazazi, et al. Am J Respir Crit Care Med. Macrophage-NLRP3 Activation Promotes Right Ventricle Failure in Pulmonary Arterial Hypertension

[3] Ronghui Lin, et al. J Labelled Comp Radiopharm. Synthesis of deuterium-labeled CCR2 antagonist JNJ-26131300, [4-(1H-indol- 3-yl)-piperidin-1-yl]-{1-[3-(3,4,5-trifluoro-phenyl)-acryloyl]-piperidin-4-yl}-acetic acid

[4] Ayse Bassez, et al. Nat Med. A single-cell map of intratumoral changes during anti-PD1 treatment of patients with breast cancer

[5] Aditya Ambade, et al. Hepatology. Pharmacological Inhibition of CCR2/5 Signaling Prevents and Reverses Alcohol-Induced Liver Damage, Steatosis, and Inflammation in Mice

Related CCR Products
CCR6 antagonist 1

CCR6 antagonist 1 is a CCR6 antagonist that inhibits the CCL20/CCR6 axis. CCR6 antagonist 1 can be used in the research of autoimmune-mediated inflammatory diseases, such as inflammatory bowel diseases (IBDs).
IPG7236

IPG7236 is a selective CCR8 antagonist that also exhibits significant tumor suppression in a mouse xenograft model of human breast cancer.IPG7236 can be used in cancer-related studies.
CKLF1-C19

CKLF1-C19 is the C-terminal peptide of human chemokine-like factor 1 (CKLF1).
Met-RANTES (human)

Met-RANTES (human) is a partial antagonist of CCR5.
IPG0521

IPG0521 is a bifunctional antibody targeting CCR8, which can block CCR8 signaling with high intensity and weak ADCC function, and can effectively inhibit the growth of multiple tumor types in homologous and immunohumanized mouse models.
  Catalog
Abmole Inhibitor Catalog




Keywords: CCR2 antagonist 5  supplier, CCR, inhibitors, activators

 
Get to Know Us
Customer Support
Resources
Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.