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CCR2-RA-[R]

Cat. No. M13923
CCR2-RA-[R] Structure
Size Price Availability
5mg USD 78  USD78 4-7 Days
10mg USD 120  USD120 4-7 Days
25mg USD 240  USD240 4-7 Days
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Biological Activity

CCR2-RA-[R] is an allosteric antagonist of the C-C chemokine receptor type 2 (CCR2) with an IC50 of 103 nM.

Chemical Information
Molecular Weight 351.8
CAS Number 512177-83-2
Solubility (25°C) DMSO ≥ 90 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] Xiaoli An, et al. Revealing the Positive Binding Cooperativity Mechanism between the Orthosteric and the Allosteric Antagonists of CCR2 by Metadynamics and Gaussian Accelerated Molecular Dynamics Simulations

[2] Natalia V Ortiz Zacaras, et al. Pyrrolone Derivatives as Intracellular Allosteric Modulators for Chemokine Receptors: Selective and Dual-Targeting Inhibitors of CC Chemokine Receptors 1 and 2

[3] Yi Zheng, et al. Structure of CC chemokine receptor 2 with orthosteric and allosteric antagonists

[4] Annelien J M Zweemer, et al. Discovery and mapping of an intracellular antagonist binding site at the chemokine receptor CCR2

[5] Annelien J M Zweemer, et al. Multiple binding sites for small-molecule antagonists at the CC chemokine receptor 2

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Keywords: CCR2-RA-[R] supplier, CCR, inhibitors, activators

 
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