Free shipping on all orders over $ 500

Cenicriviroc Mesylate

Cat. No. M9444
Cenicriviroc Mesylate Structure
Synonym:

TBR-652 Mesylate; TAK-652 Mesylate

Size Price Availability
10mg USD 260  USD260 1-2 Weeks
50mg USD 830  USD830 1-2 Weeks
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

Cenicriviroc Mesylate is a dual CCR2/CCR5 antagonist, and it also inhibits both HIV-1 and HIV-2. Cenicriviroc Mesylate shows a median EC50 of 0.39 nM for the four R5-tropic HIV-2 isolates. 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).

Chemical Information
Molecular Weight 793.05
Formula C42H56N4O7S2
CAS Number 497223-28-6
Solubility (25°C) DMSO ≥ 80 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] Lefebvre E, et al. PLoS One. Antifibrotic Effects of the Dual CCR2/CCR5 Antagonist Cenicriviroc in Animal Models of Liver and Kidney Fibrosis.

[2] Visseaux B, et al. PLoS One. Cenicriviroc, a Novel CCR5 (R5) and CCR2 Antagonist, Shows In Vitro Activity against R5 Tropic HIV-2 Clinical Isolates.

[3] Lalezari J, et al. J Acquir Immune Defic Syndr. Safety, efficacy, and pharmacokinetics of TBR-652, a CCR5/CCR2 antagonist, in HIV-1-infected, treatment-experienced, CCR5 antagonist-naive subjects.

[4] Baba M, et al. Antimicrob Agents Chemother. TAK-652 inhibits CCR5-mediated human immunodeficiency virus type 1 infection in vitro and has favorable pharmacokinetics in humans.

Related CCR Products
IPG7236

IPG7236 is a selective CCR8 antagonist that also exhibits significant tumor suppression in a mouse xenograft model of human breast cancer.IPG7236 can be used in cancer-related studies.

CKLF1-C19

CKLF1-C19 is the C-terminal peptide of human chemokine-like factor 1 (CKLF1).

Met-RANTES (human)

Met-RANTES (human) is a partial antagonist of CCR5.

IPG0521

IPG0521 is a bifunctional antibody targeting CCR8, which can block CCR8 signaling with high intensity and weak ADCC function, and can effectively inhibit the growth of multiple tumor types in homologous and immunohumanized mouse models.

IPGA05

IPGA05 is a monoclonal antibody targeting CCR8 for tumor-related studies.

  Catalog
Abmole Inhibitor Catalog




Keywords: Cenicriviroc Mesylate, TBR-652 Mesylate; TAK-652 Mesylate supplier, CCR, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.