Maraviroc free base · Synonyms: UK-427857

Maraviroc is a selective CCR5 antagonist.

For research use only. Not for human or veterinary use.

Target CCR HIV

Research area Inflammation/Immunology Endocrinology Cancer

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Data Sheet SDS COA

Maraviroc structure

CAS No.: 376348-65-1

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 585.00	BP-02217-250mg	In stock	Get quote
500 mg	USD 700.00	BP-02217-500mg	In stock	Get quote
1 g	USD 985.00	BP-02217-1g	In stock	Get quote
5 g	USD 2,850.00	BP-02217-5g	In stock	Get quote
10 g	Inquire	BP-02217-10g	In stock	Inquire

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Description

Maraviroc (UK-427857) is a selective CCR5 antagonist with activity against human HIV.

Biological activity

In Vitro Maraviroc (UK-427857) is a selective CCR5 antagonist with potent anti-human immunodeficiency virus type 1 (HIV-1) activity. Maraviroc inhibits the downstream event of chemokine-induced intracellular calcium redistribution, with IC50s ranging from 7 to 30 nM obtained against MIP-1β, MIP-1α and RANTES. Maraviroc (UK-427857) is active (IC90) at low nanomolar concentrations against HIV-1 Ba-L (a lab-adapted R5 strain) when measured in a 5-day antiviral assay using either isolated multiple (pooled) donor PBMC (IC90, 3.1 nM), single-donor PBMC (IC90, 1.8 nM) or PM-1 cells (IC90, 1.1 nM) In Vivo Clearance values are moderate to high in both rat and dog species following i.v. administration (74 and 21 mL/min/kg, respectively). Maraviroc also has a moderate volume of distribution in both species (4.3 to 6.5 liters/kg). The half-life values of maraviroc are 0.9 h in the rat and 2.3 h in the dog. Following oral administration (2 mg/kg) to the dog, the Cmax(256 ng/mL) occurs 1.5 h. post-dose, and the bioavailability is 40%. For the rat, investigation of the concentrations obtain in the portal vein following oral administration indicated that approximately 30% of the administered dose is absorbed from the intestinal tract[1]. In the DSS/TNBS colitis and in the transfer model, Maraviroc attenuates development of intestinal inflammation by selectively reducing the recruitment of CCR5 bearing leukocytes

Identifiers

SMILES: [H][C@]12CC[C@]([H])(CC(C1)N1C(C)=NN=C1C(C)C)N2CC[C@H](NC(=O)C1CCC(F)(F)CC1)C1=CC=CC=C1
InChIKey: GSNHKUDZZFZSJB-HLMSNRGBSA-N

Specifications

MW (average): 513.6655
Formula: C₂₉H₄₁F₂N₅O
CAS No.: 376348-65-1
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO : 50 mg/mL (97.34 mM; Need ultrasonic) Ethanol : 6.5 mg/mL (12.65 mM; Need ultrasonic)

Documents

References

[1]. Dorr P, et al. 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. Antimicrob Agents Chemother. 2005 Nov;49(11):472

[2]. Mencarelli A, et al. Highly specific blockade of CCR5 inhibits leukocyte trafficking and reduces mucosal inflammation in murine colitis. Sci Rep. 2016 Aug 5;6:30802.

Same target

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Same research area

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