Maraviroc

製品コードS2003 別名:UK-427857

Maraviroc化学構造

分子量(MW):513.67

Maraviroc is a CCR5 antagonist for MIP-1α, MIP-1β and RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2 nM in cell-free assays, respectively.

サイズ 価格(税別)  
JPY 16268.00
JPY 11620.00
JPY 44820.00
JPY 127820.00

カスタマーフィードバック(5)

  • The functional significance of the PI3K/Akt pathway in CCR5-mediated DNA damage signaling was assessed using the ATP-competitive, small-molecule pan-Akt inhibitor (ipatasertib) and or the CCR5 inhibitor Maraviroc in doxorubicin-treated cells. Western blot analysis was conducted as shown for SUM-159 cells (B).

    Clin Cancer Res, 2018, 78(7):1657-1671. Maraviroc purchased from Selleck.

    (F) Representative timed photon emission of mice injected with SUM-159 cells treated with either vehicle control or CCR5 antagonist Maraviroc (8 mg/kg) for six weeks. Colorimetric scale of photon flux (x107 p/sec/cm2/sr) reflects tumor volume.

    Cancer Res, 2018, 78(7):1657-1671. Maraviroc purchased from Selleck.

  • CCR5 antagonists block FBS-induced breast cancer cell invasion. 3D reconstruction of FBS-induced invasion into collagen gels by Hs578T (A) or SUM-159 (C) breast cancer cells in presence of CCR5 antagonists (100 nmol/L). The corresponding quantifications (mean ±SEM, n = 3) and analysis (Bonferronit test) are displayed in B and D.

    Cancer Res 2012 72(15), 3839-50. Maraviroc purchased from Selleck.

    (E)CAF-induced migration of Huh7 cells was blocked by antagonists of chemokine receptors. CCR2 antagonist (INCB3284, 100 nM), CCR5 antagonist (Maraviroc, 100 nM) and selective CCR1 and CCR3 antagonists (UCB35625, 100 nM) were added to CAF-CM in the transwell assay.

    Cancer Lett, 2016, 379(1):49-59.. Maraviroc purchased from Selleck.

  • Analysis of receptor mechanisms mediating the induction of MMP-9 expression in THP-1 cells by AFP. Maraviroc, an inhibitor of chemokine receptor CCR5, was added to the cells in the indicated concentrations 1 hour before addition of 50 μg/ml AFP or 150 ng/ml RANTES. After 24 hours of cell stimulation, conditioned media were collected and analyzed for MMP-9 activity by the method of zymography

    2010 Dr. Johanna Weiss of University Hospital Heidelberg. Maraviroc purchased from Selleck.

製品安全説明書

CCR阻害剤の選択性比較

生物活性

製品説明 Maraviroc is a CCR5 antagonist for MIP-1α, MIP-1β and RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2 nM in cell-free assays, respectively.
ターゲット
CCR5 [3]
(Cell-free assay)
MIP-1α [1]
(Cell-free assay)
RANTES [1]
(Cell-free assay)
MIP-1β [1]
(Cell-free assay)
3.3 nM 5.2 nM 7.2 nM
体外試験

Maraviroc inhibits MIP-1β-stimulated γ-S-GTP binding to HEK-293 cell membranes, indicating its ability to inhibit chemokine-dependent stimulation of GDP-GTP exchange at the CCR5/G protein complex. Maraviroc also 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. In the same experiments, Maraviroc does not trigger release of intracellular calcium at concentrations up to 10 μM, indicating that it is devoid of CCR5 agonist activity. Consistent with this, Maraviroc fails to induce CCR5 internalization. Maraviroc is active at low nanomolar concentrations against HIV-1 Ba-L. Maraviroc inhibits all 200 pseudotyped viruses with a geometric mean IC90 of 13.7 nM. [1] At concentrations >1000 times the 50% inhibitory concentration, maraviroc did not inhibit other chemokine receptors (CCR1, 2, 3, 4, 7, and 8; CXCR1 and 2) to a clinically relevant degree[3].

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HeLa-P4 cells MmnMSpVv[3Srb36gZZN{[Xl? Mmf3NlAh\GG7cx?= MkSyRY51[WexbnnzeEBi[3Srdnn0fUBifCCFQ2K1JJJm[2WydH;yJIV5eHKnc4Pl[EBqdiCKZVzhMXA1KGOnbHzzJINwNWW6cILld5NqdmdiQ1S0JIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gbY5nfXOrb36geI8hUEmYIHfwNVIxKGW6cILld5Nm\CCrbjDDTG8ufGG2MUCgZ4VtdHNiYX\0[ZIhOjBiaILzJIJ6KGOnbHytZ4VtdCCodYPpc44h[XO|YYmsJGlEPTB;MD6yJI5O MoD4NlEyOjh4NkO=
rhesus monkey Chem-1 cell MniySpVv[3Srb36gZZN{[Xl? M3P3fFEzOCCvaX7z NVjiOnN6TGm|cHzhZ4Vu\W62IH;mJHsyOjWLXT3NTXAuOWGucHjhJIZzd21iQ1PSOUBqdiC{aHXzeZMhdW:wa3X5JGNp\W1vMTDj[YxtKG2nbXLyZY5meyCjZoTldkAyOjBibXnud{BjgSCuaYH1bYQhe2OrboTpcIxifGmxbjDjc5VvfGmwZzDhcoFtgXOrczygT4k:OC5{NDDuUS=> MonWNlM3QDJ|MEi=
human TZM-bl cells M33wXGZ2dmO2aX;uJIF{e2G7 MWG0PEBp M{jVfmFvfGGpb37pd5Qh[WO2aY\peJkh[WejaX7zeEBES1J3IILlZ4VxfG:{IHnuJIh2dWGwIGTaUU1jdCClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGhKXi1zIF3HR|I3NWmwZIXj[YQh[2WubD3j[YxtKG[3c3nvckBj\XS5ZXXuJJZqemGuIHXueoVtd3CnIIDyc5RmcW5iZYjwdoV{e2mwZzDoeY1idiCKRVuyPVMh[2WubIOgeI8hXFqPLXLsJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGlEPTB;MD6zO{BvVQ>? M3G4dVI1PTZ|N{Kz
CHO cells NHT4UIdHfW6ldHnvckBie3OjeR?= NXXxSIhHOiCq M1XkfGRqe3CuYXPlcYVvfCCxZjDbNVI5UV2UQV7USXMh\nKxbTDoeY1idiCFQ2K1JJJm[2WydH;yJINw\XiycnXzd4VlKHerdHigS4FteGijaU[gbY4hS0iRIHPlcIx{KGGodHXyJFIhcHK|IHL5JJNkcW62aXzsZZRqd25iY3;1cpRqdmduIFnDOVA:OS52IH7N M2rsfVIxOTN5OUO3
HOS cells M1nEeWZ2dmO2aX;uJIF{e2G7 MojCRY51cX[rcnHsJIFkfGm4aYT5JIFo[Wmwc4SgTGlXOSCEYT3MJIlv\mWldHXkJIlvKEiRUzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKH[rcnHsJIlv\mWldHnvckwhUUN3ME2yJI5O NG\SOWYyQTZ4NEmyNC=>
HEK293 cells MlPOSpVv[3Srb36gZZN{[Xl? MkXCTY5pcWKrdHnvckBw\iCqdX3hckBOSVSHMT3t[YRq[XSnZDDBV3AsKHWydHHr[UBmgHC{ZYPz[YQhcW5iSFXLNlk{KGOnbHzzJIFnfGW{IEGuOUBucW6|IHL5JIZtfW:{ZYPj[Y5k\SCjc4PhfUwhUUN3ME2xO{4{KM7ebR?= Ml63NlMzPDFyMkm=
human astrocytes NFu3eVZHfW6ldHnvckBie3OjeR?= MkjrNVAxKG6P M3\xPVMxKHSxIE[wJI1qdnN? NUnmeoY1SmmwZHnu[{Bi\m[rbnn0fUB1dyCFQ2K1M21QWiCrbjDoeY1idiCjc4Tyc4N6fGW|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiUkWgTGlXNTFiU1[xOlIhcW6oZXP0bY9vKGK7IH3lZZN2emmwZzDUZZQheHKxdHXpckBmgHC{ZYPzbY9vKGG2IEGwNEBvVSCycnXpcoN2[mG2ZXSg[o9zKDNyIITvJFYxKG2rboOg[o9tdG:5ZXSgZpkhfmm{YXygbY5n\WO2aX;uJI1m[XO3cnXkJIFnfGW{IEG4JIhzeyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZk> NYHFSVltOjN4OEKzNFg>

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

体内試験 The half-life values of Maraviroc are 0.9 hour in the rat and 2.3 hours in the dog. Following oral administration (2 mg/kg) to the dog, the Cmax (256 ng/ml) occurred 1.5 hours post-dose, and the bioavailability is 40%. For the rat, approximately 30% of the administered dose is absorbed from the intestinal tract. [1] Female RAG-hu mice are challenged vaginally with HIV-1 an hour after intravaginal application of the Maraviroc gel. Maraviroc gel treated mice are fully protected against vaginal HIV-1 challenge in contrast to placebo gel treated mice which all became infected. Vaginal administration of Maraviroc fully protects mice against HIV-1 vaginal challenge. While there is a clear pattern of CD4 T cell decline in placebo-gel treated and viral challenged mice, their levels are stable in mice receiving Maraviroc gel. [2]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

+ 展開

Inhibition of chemokine binding to CCR5:

Binding of 125I-labeled MIP-1α, MIP-1β, and RANTES to CCR5 is measured 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) 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. Maraviroc dilutions are added to each well to a final volume of 100 μL, the assay plates incubate for 1 hour, and the contents filter through preblocked and washed Unifilter plates which are counted following overnight drying.
細胞試験:

[1]

+ 展開
  • 細胞株: PHA-stimulated PBMC or PM-1 cells
  • 濃度: 0-1 μM
  • 反応時間: 5 days or 7 days
  • 実験の流れ:

    Drug susceptibility assays are performed in 24-well tissue culture plates. Duplicate eight-point dilution series of Maraviroc are prepared in DMSO and medium to yield a final DMSO concentration of 0.1% (vol/vol) in the assay. PHA-stimulated PBMC or PM-1 cells are infected with virus for 1 hour at 37 °C. Cells are subsequently washed once, and 3.6 × 105 PBMC or 2.0 × 105 PM-1 cells are added to each well of assay plates containing diluted Maraviroc. Plates are incubated for 5 days (lab-adapted strains) or 7 days (primary isolates) at 37 °C in a humidified 5% CO2 (vol/vol) atmosphere.


    (参考用のみ)
動物試験:

[2]

+ 展開
  • 動物モデル: Humanized BALB/c-Rag2−/−γc−/− and BALB/c-Rag1−/−γc−/− (RAG-hu) mice
  • 製剤: Dissolved in phosphate-buffered saline, sterile-filtered and adjusted to a final concentration of 4 mg/mL (7.8 mM). A 3.4% gel preparation of hydroxyl-ethyl cellulose (HEC) is added to achieve a final concentration of 5 mM Maraviroc in 2.2% HEC gel.
  • 投薬量: ~64 μg
  • 投与方法: A 25 μL volume of the gel formulation is carefully applied in to the vaginal vault of mice.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 100 mg/mL (194.67 mM)
Ethanol 100 mg/mL (194.67 mM)
Water Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
2% DMSO+corn oil
混合させたのち直ちに使用することを推奨します。
10mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 513.67
化学式

C29H41F2N5O

CAS No. 376348-65-1
保管
in solvent
別名 UK-427857

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03172026 Recruiting Stroke University of California Los Angeles|Burke Rehabilitation Hospital May 1 2018 Phase 2|Phase 3
NCT03274804 Recruiting Metastatic Colorectal Cancer|MSS University Hospital Heidelberg|Institut für Klinisch-Onkologische Forschung Krankenhaus Nordwest GmbH April 1 2018 Phase 1
NCT02881762 Recruiting Hepatitis C|Human Immunodeficiency Virus University of Maryland|ViiV Healthcare June 1 2017 Phase 4
NCT03218592 Active not recruiting HIV/AIDS University of North Carolina Chapel Hill|National Institute of Allergy and Infectious Diseases (NIAID) June 28 2017 Phase 4
NCT02990312 Recruiting Hiv|Kidney Transplant|HIV Reservoir|CCR5 University of Maryland May 1 2017 Phase 4
NCT02778204 Recruiting HIV Infections National Institute of Allergy and Infectious Diseases (NIAID) May 1 2017 Phase 1

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問1:

    What’s the vehicle do you recommend to dissolve the compound for in vivo experiments?

  • 回答:

    S2003 Maraviroc can be dissolved in 5% DMSO/castor oil at 62 mg/ml as suspension for oral administration. As to a clear solution for injection, following three vehicles at 10mg/ml will help: 1. 2% DMSO/castor oil; 2. 2%DMSO/sunflower oil; 3. 2%DMSO/30%PEG 300/ddH2O.

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