CXCR7 modulator 2 (C09-1120-791)

CXCR7 modulator 2 is a modulator of C-X-C Chemokine Receptor Type 7 ( CXCR7 ), with a K i of 13 nM.In VitroCXCR7 modulator 2 (compound 18) demonstrates potent CXCR7-binding affinity (K i =13 nM) and β-arrestin activity (EC 50 =11 nM). CXCR7 modulator 2 also exhibits improved selectivity in the GPCR panel and an improved therapeutic index in the hERG patch-clamp assay in comparison with 11c. CXCR7 modulator 2 exhibits moderate to high in vitro turn over in both NADPH-supplemented mouse-liver microsomes (MLM, 93 μL/min/mg) and hepatocytes (28 μL/min per million cells), shows poor passive absorptive permeability in the MDCK II-permeability assay, and has good aqueous solubility. CXCR7 modulator 2 is rapidly absorbed with a mean maximal plasma concentration (C max ) of 682 ng/mL, which occurrs at 0.25 h (T max ). The corresponding mean area under the plasma-concentration-versus-time profile (AUC) is 740 ng/mL/h. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoThe administration of isoproterenol for 9 days leads to the development of cardiac fibrosis, as attested by the approximately 4-fold increase in collagen deposition relative to that in the control, which is detected by picrosirius-red staining. Treatment with CXCR7 modulator 2 results in a statistically significant reduction in cardiac fibrosis, thereby demonstrating the protective role of CXCR7 modulation with CXCR7 modulator 2 in an isoproterenol-induced cardiac injury . MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:CXCR7 13 nM (Ki). Specifications and Purity: 98%. Molecular Formula: C29H42N6O3. Molecular Weight: 522.68. PubChem CID: 134694953. Isomeric SMILES: CCC1=C(C2=NC=CN2C=C1)N3CCCN(CC3)[C@@H](CC(=O)N)C4CCN(CC4)C(=O)[C@H]5C[C@@H]6CC[C@H]5O6.