Cenicriviroc Mesylate - 10mM in DMSO , CAS No.497223-28-6

CAS: 497223-28-6 Cat. No.: C654622 Summenformel: C₄₂H₅₆N₄O₇S₂ Molekulargewicht: 793.05 EG-Nummer: 824-584-9 PubChem CID: 11285791

QUALITÄT & REINHEIT 10mM in DMSO

Storage

Desiccated,Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

Cenicriviroc Mesylate (TAK-652 Mesylate) is a dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2 , and displays potent anti-inflammatory and antiinfective activity.

In Vitro

Migration of mouse monocytes in response to carbon tetrachloride (CCL2) is reduced following pre-treatment with Cenicriviroc Mesylate (CVC) at a concentration of 1 μM. Compare to untreated and unstimulated cells, the average fold change in migrating cells (±SD) is 0.8±0.2 (p>0.05) and 0.7±0.4 (p>0.05) for CCL2-stimulated cells treated with Cenicriviroc Mesylate and unstimulated cells treated with Cenicriviroc Mesylate, respectively. Phenotypic susceptibility testing shows, for the four R5-tropic HIV-2 isolates, a median EC 50 for Cenicriviroc Mesylate of 0.39 nM (0.03, 0.33, 0.45 and 0.98 nM). The dual-tropic and the X4-tropic HIV-2 strains are resistant to Cenicriviroc Mesylate with EC 50 at >1000 nM, and Maximum percentages of inhibition (MPI) at 33% and 4%, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Cenicriviroc Mesylate (CVC) treatment leads to dose-related decrease in monocyte/macrophage recruitment, and achieving statistical significance at doses ≥20 mg/kg/day (p<0.05). Compare to the vehicle-control group, peritoneal lavage monocyte/macrophage counts are decreased by: 5.7%, 45.2%, 76.5% and 26.0% for Cenicriviroc Mesylate 5 twice daily (BID), Cenicriviroc Mesylate20 twice daily (BID), Cenicriviroc Mesylate100 BID, Cenicriviroc Mesylate 20 once-daily (QD), respectively. Exposure to Cenicriviroc Mesylate is dose-related and correlated with the decrease in monocyte/macrophage recruitment, with Cenicriviroc Mesylate appearing to be more effective when given BID versus QD, in line with the higher plasma concentrations achieved with BID dosing and the known short half-life in mice (~2 hours) . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Spezifikationen

Spezifikationen & Reinheit

10mM in DMSO

Biochemische und physiologische Mechanismen

Cenicriviroc Mesylate (TAK-652 Mesylate) is a dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2 , and displays potent anti-inflammatory and antiinfective activity.

Storage

Desiccated,Store at -80°C

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Aktionsart

INHIBITOR

Namen und Kennungen

Isomere SMILES

CCCCOCCOC1=CC=C(C=C1)C2=CC/3=C(C=C2)N(CCC/C(=C3)/C(=O)NC4=CC=C(C=C4)[S@@](=O)CC5=CN=CN5CCC)CC(C)C.CS(=O)(=O)O

PubChem CID

11285791

Molekulargewicht

793.05