Maraviroc is an antiretroviral compound in the CCR5 receptor antagonist class used in the treatment of HIV infection. It is also classed as an entry inhibitor. Maraviroc is extensively metabolized by CYP3A4, with renal clearance accounting for approximately 23% of total clearance. Maraviroc is an entry inhibitor. Specifically, maraviroc is a negative allosteric modulator of the CCR5 receptor, which is found on the surface of certain human cells. Maraviroc (UK-427857) inhibits CCL3 (MIP-1α) binding to CCR5, thereby blocking the HIV protein gp120 from associating with the receptor. Maraviroc (brand-named Selzentry, or Celsentri) displays potent anti-HIV-1 activity. UK-427857 prevents the interaction of HIV-1 gp120 and CCR5 (IC50 = 6.4 nM), inhibiting HIV-1 entry. Maraviroc has no detectable in vitro cytotoxicity and is highly selective for CCR5, as confirmed against a wide range of receptors and enzymes, including the hERG ion channel (50% inhibitory concentration, >10 μM), indicating potential for an excellent clinical safety profile. Maraviroc also appeared to reduce graft-versus-host disease in patients treated with allogeneic bone marrow transplantation for leukemia, in a phase 1/2 study. In addition, those who received the entry inhibitor had a mean increase in CD4 cells of 110 cells/µL in the once-daily group, 106 cells/µL in the twice-daily group, and 56 cells/µL in the placebo group.
Molecular Weight | 513.67 |
Formula | C29H41F2N5O |
CAS Number | 376348-65-1 |
Solubility (25°C) | DMSO 50 mg/mL Ethanol 10 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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.
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. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.