2. GPCR/G Protein Immunology/Inflammation Anti-infection
  3. CCR HIV
  4. Maraviroc

マラビロク  (Synonyms: Maraviroc; UK-427857)

製品番号: HY-13004 純度: 99.98%
COA 取扱説明書 Technical Support

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

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CAS 番号 : 376348-65-1

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 68 在庫あり
Solution
10 mM * 1 mL in DMSO USD 68 在庫あり
Solid
5 mg $60 在庫あり
10 mg $108 在庫あり
25 mg $195 在庫あり
50 mg $348 在庫あり
100 mg $624 在庫あり
500 mg $1260 在庫あり
1 g $1890 在庫あり
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カスタマーレビュー

Based on 51 publication(s) in Google Scholar

Other Forms of Maraviroc:

マラビロク 関連抗体

Top Publications Citing Use of Products

顧客検証

In Vivo Efficacy Study
Cell Migration/Invasion Assay
IHC
WB

    Maraviroc purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jul 21:e00950.  [Abstract]

    Freshly isolated neutrophils were pre-treated overnight with culture supernatant from AGS or AGS-EBV cells (H), supplemented with Maraviroc (1 µM).

    Maraviroc purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jun 19:e16476.  [Abstract]

    LLC‐Vector and LLC‐ENH‐OV tumor growth in mice treated with or without maraviroc (i.p., 10 mg/kg, every other day).

    Maraviroc purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Jun 19:e16476.  [Abstract]

    Representative images of IF staining for CD31 and IHC staining for F4/80 in LLC‐Vector and LLC‐ENH‐OV tumors sections treated with or without maraviroc (i.p., 10 mg kg−1, every other day i.p., 10 mg/kg, every other day ).

    Maraviroc purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Nov 25;11(1):5994.  [Abstract]

    Aortic diameters in CaCl2-treated mice after maraviroc (intraperitoneally injected with 10 mg/kg , daily for 3 weeks) application (n = 4 each).

    Maraviroc purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2017 May 3:8:230.  [Abstract]

    Inhibition of total and phosphorylation levels of CCR5, PKC δ, and p38 in MIP-1β-induced U937 cells by WTD. Cells are pretreated with PMA for 48 h and then incubated with or without WTD or MVC for 2 h. Subsequently, cells are stimulated with MIP-1β (25 nM). After 10 min of stimulation, cells are collected to detect total and phosphorylated (p) CCR5 (A), PKC δ (B), and p38 (C) by western blotting.

    CCR アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

    HIV アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    HIV HIV-1 HIV-2

    • 生物活性

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

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

    IC50 & Target[1]

    MIP-1α-CCR5

    3.3 nM (IC50, in HEK-293 cell membrane)

    RANTES-CCR5

    5.2 nM (IC50, in HEK-293 cell membrane)

    MIP-1β-CCR5

    7.2 nM (IC50, in HEK-293 cell membrane)

    HIV-1 (Ba-L)

    1.1 nM (IC50, in PM-1 cells)

    Cellular Effect
    Cell Line Type Value Description References
    HOS CC50
    > 200 1
    Compound: MVC
    Cytotoxicity against human HOS cells after 48 hrs by MTT assay
    Cytotoxicity against human HOS cells after 48 hrs by MTT assay
    		[PMID: 30234300]
    PBMC CC50
    > 200 1
    Compound: MVC
    Cytotoxicity against human PBMC after 48 hrs by MTT assay
    Cytotoxicity against human PBMC after 48 hrs by MTT assay
    		[PMID: 30234300]
    TZM CC50
    > 200 3
    Compound: MVC
    Cytotoxicity against human TZM-bl cells after 48 hrs by MTT assay
    Cytotoxicity against human TZM-bl cells after 48 hrs by MTT assay
    		[PMID: 30234300]
    体外実験

    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)[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    マラビロク 関連抗体
    体内実験

    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[2]

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    臨床実験
    分子量

    513.67

    分子式

    C29H41F2N5O
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1CCC(F)(F)CC1)N[C@H](C2=CC=CC=C2)CCN3[C@H]4C[C@@H](N5C(C)=NN=C5C(C)C)C[C@@H]3CC4
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 50 mg/mL (97.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : 6.5 mg/mL (12.65 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9468 mL 9.7339 mL 19.4678 mL
    5 mM 0.3894 mL 1.9468 mL 3.8936 mL
    10 mM 0.1947 mL 0.9734 mL 1.9468 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

    C2

    ×
    体積 （終了）

    V2

    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

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    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    % 
    +
    %
    Tween-80 +
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    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.98%

    COA (250 KB) RP-HPLC (245 KB) MS (72 KB)

    取扱説明書 (2659 KB)
    参考文献
    キナーゼ実験
    [1]

    Binding of 125I-labeled MIP-1α, MIP-1β, and RANTES to CCR5 is measured essentially using intact HEK-293 cells stably expressing the receptor or membrane preparations thereof. Briefly, cells are resuspended in binding buffer (50 mM HEPES containing 1 mM CaCl2, 5 mM MgCl2, and 0.5% bovine serum albumin [BSA] and adjusted to pH 7.4) to a density of 2×106 cells/mL. For membrane preparations, phosphate-buffered saline (PBS)-washed cells are resuspended in lysis buffer (20 mM HEPES, 1 mM CaCl2, 1 tablet COMPLETE per 50 mL, pH 7.4; Boehringer) prior to homogenization in a Polytron hand-held homogenizer, ultracentrifugation (40,000× g for 30 min), and resuspension in binding buffer to a protein concentration of 0.25 mg/mL (12.5 μg of membrane protein is used in each well of a 96-well plate). 125I-radiolabeled MIP-1α, MIP-1β, and RANTES are prepared and diluted in binding buffer to a final concentration of 400 pM in the assay. Appropriate maraviroc dilutions are added to each well to a final volume of 100 μL, the assay plates incubated for 1 h, and the contents filtered through preblocked and washed Unifilter plates which are counted following overnight drying[1].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    細胞実験
    [1]

    HEK-293 cell aliquots (100 μL at 1×106 cells/mL) are plated into poly-D-lysine-coated plates and incubated at 37°C overnight. A 1:1 mix of soluble recombinant human CD4 (sCD4) (diluted to 4.5 nM in culture medium) and HIV-1 gp120 is incubated at room temperature for 15 min prior to its addition to PBS-washed cells in the presence of dilutions of maraviroc to enable IC50 determination. The assay plates are incubated at 37°C for 1 h and washed. Eu3+-labeled anti-gp120 antibody (1/500 dilution in assay buffer) is added to each well (50 μL) and incubated for 1 h. The plate is washed three times with wash buffer prior to the addition of enhancement solution (200 μL/well) and measurement of Eu3+ fluorescence (Victor2multilabel counter; “Europium” protocol). Nonspecific binding is taken as the fluorescence measured for gp120 incubated with cells in the absence of preincubation with sCD4[1].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [1][2]

    Rats and Dogs[1]
    Preclinical pharmacokinetic studies are carried out with maraviroc following a single intravenous and oral administration to both male Sprague-Dawley rats (1 mg/kg of body weight given intravenously [i.v.] and 10 mg/kg given orally [p.o.]; n=2) and male beagle dogs (0.5 mg/kg i.v. and 2 mg/kg p.o; n=4). Plasma samples are taken for up to 24 h postdose, and the concentrations of unchanged maraviroc are determined using a specific high-performance liquid chromatography-tandem mass spectrum assay.
    Mice[2]
    Splenocytes are collected from 6-10 week old CCR5-/- mice or wild-type controlmice (n=8 per group) and naive CD4+ CD45RBhigh T-cells are isolated by cell sorting. A total of 3×105 CD45RBhigh cells are then injected intravenously into Rag1-/- mice that are subsequently weighed and assessed for fecal score every 20 days to evaluate IBD development. To investigate whether Maraviroc rescues from intestinal inflammation induced by transfer colitis, Rag1-/- mice are injected with CD4+ CD45RB-/- T-cells and 34 days later randomized into either a control group (no further treatment, n=6) or treatment with Maraviroc, 50 mg/kg/d Maraviroc per os (n=4) for 3 weeks, 5 d/week.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    Ethanol / DMSO 1 mM 1.9468 mL 9.7339 mL 19.4678 mL 48.6694 mL
    5 mM 0.3894 mL 1.9468 mL 3.8936 mL 9.7339 mL
    10 mM 0.1947 mL 0.9734 mL 1.9468 mL 4.8669 mL
    DMSO 15 mM 0.1298 mL 0.6489 mL 1.2979 mL 3.2446 mL
    20 mM 0.0973 mL 0.4867 mL 0.9734 mL 2.4335 mL
    25 mM 0.0779 mL 0.3894 mL 0.7787 mL 1.9468 mL
    30 mM 0.0649 mL 0.3245 mL 0.6489 mL 1.6223 mL
    40 mM 0.0487 mL 0.2433 mL 0.4867 mL 1.2167 mL
    50 mM 0.0389 mL 0.1947 mL 0.3894 mL 0.9734 mL
    60 mM 0.0324 mL 0.1622 mL 0.3245 mL 0.8112 mL
    80 mM 0.0243 mL 0.1217 mL 0.2433 mL 0.6084 mL
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    Maraviroc Related Classifications

    • Molarity Calculator

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    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Maraviroc376348-65-1UK-427857UK427857UK 427857CCRHIVCC chemokine receptorHuman immunodeficiency virusInhibitorinhibitorinhibit

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    製品名:
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    製品番号:
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