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ACT-1004-1239

Cat. No. M21310
ACT-1004-1239 Structure
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Biological Activity

ACT-1004-1239 is a potent, selective, orally administered CXCR7 antagonist with an IC50 value of 3.2 nM.

Chemical Information
Molecular Weight 522.55
Formula C27H28F2N6O3
CAS Number 2178049-58-4
Solubility (25°C) N/A
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] Christine Huynh, et al. Front Pharmacol. Absorption, Metabolism, and Excretion of ACT-1004-1239, a First-In-Class CXCR7 Antagonist: In Vitro, Preclinical, and Clinical Data

[2] Christine Huynh, et al. Biomed Pharmacother. Target engagement of the first-in-class CXCR7 antagonist ACT-1004-1239 following multiple-dose administration in mice and humans

[3] Laetitia Pouzol, et al. FASEB J. ACT-1004-1239, a first-in-class CXCR7 antagonist with both immunomodulatory and promyelinating effects for the treatment of inflammatory demyelinating diseases

[4] Christine Huynh, et al. Clin Pharmacol Ther. A Multipurpose First-in-Human Study With the Novel CXCR7 Antagonist ACT-1004-1239 Using CXCL12 Plasma Concentrations as Target Engagement Biomarker

[5] Sylvia Richard-Bildstein, et al. J Med Chem. Discovery of the Potent, Selective, Orally Available CXCR7 Antagonist ACT-1004-1239

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Keywords: ACT-1004-1239 supplier, CXCR, inhibitors, activators
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