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Maraviroc

Cat. No. M1971
Maraviroc Structure
Synonym:

Selzentry, Celsentri, UK-427857

Size Price Availability Quantity
2mg USD 30  USD30 In stock
5mg USD 50  USD50 In stock
10mg USD 87  USD87 In stock
25mg USD 175  USD175 In stock
100mg USD 465  USD465 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
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
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] Wilfredo Alejandro González-Arriagada, et al. J Cancer Res Clin Oncol. CR5/CCL5 axis is linked to a poor outcome, and inhibition reduces metastasis in oral squamous cell carcinoma

[2] Garcia-Perez J, et al. J Biol Chem. New insights into the mechanisms whereby low molecular weight CCR5 ligands inhibit HIV-1 infection.

[3] Dorr P, et al. Antimicrob Agents Chemother. Maraviroc (UK-427,857), a potent, orally bioavailable, and selective small-molecule inhibitor of chemokine receptor CCR5 with broad-spectrum anti-human immunodeficiency virus type 1 activity.

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Keywords: Maraviroc, Selzentry, Celsentri, UK-427857 supplier, CCR, inhibitors, activators


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