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CCR8 Antagonist 1

Cat. No. M40749
CCR8 Antagonist 1 Structure
Size Price Availability Quantity
10mg USD 365  USD365 In stock
25mg USD 780  USD780 In stock
50mg USD 1200  USD1200 In stock
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Quality Control & Documentation
Biological Activity

CCR8 Antagonist 1 is a potent human CCR8 antagonist with a Ki value of 1.6 nM.

Chemical Information
Molecular Weight 495.59
Formula C26H29N3O5S
CAS Number 723304-76-5
Form Solid
Solubility (25°C) DMSO 25 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Yong Wu et al. J Med Chem. Discovery of a Potent and Selective CCR8 Small Molecular Antagonist IPG7236 for the Treatment of Cancer

[2] Joseph R Campbell et al. Cancer Res. Fc-Optimized Anti-CCR8 Antibody Depletes Regulatory T Cells in Human Tumor Models

[3] Helena Van Damme et al. J Immunother Cancer. Therapeutic depletion of CCR8+ tumor-infiltrating regulatory T cells elicits antitumor immunity and synergizes with anti-PD-1 therapy

[4] Tomoyuki Oshio et al. PLoS One. Chemokine receptor CCR8 is required for lipopolysaccharide-triggered cytokine production in mouse peritoneal macrophages

[5] David Chantry et al. Curr Drug Targets Inflamm Allergy. Chemokines in allergy

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