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Cenicriviroc Mesylate - 10mM in DMSO, high purity , CAS No.497223-28-6(DMSO)

  • 10mM in DMSO
Item Number
C654622
Grouped product items
SKUSizeAvailabilityPrice Qty
C654622-1ml
1ml
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$227.90

Basic Description

Specifications & Purity10mM in DMSO
Storage TempDesiccated,Store at -80°C
Shipped InIce chest + Ice pads
Product Description

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.

Names and Identifiers

Canonical SMILES O=C(/C1=C/C2=CC(C3=CC=C(OCCOCCCC)C=C3)=CC=C2N(CC(C)C)CCC1)NC4=CC=C([S@](CC5=CN=CN5CCC)=O)C=C4.OS(=O)(C)=O
Molecular Weight 793.05

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