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Maraviroc

別名: UK-427857 中文名稱：馬拉維若

Maraviroc是一種CCR5拮抗劑，作用于MIP-1α，MIP-1β和RANTES，無細(xì)胞試驗(yàn)中IC50分別為3.3 nM，7.2 nM和5.2 nM。Maraviroc可應(yīng)用于治療HIV感染。

Maraviroc Chemical Structure

Maraviroc Chemical Structure

CAS: 376348-65-1

規(guī)格 價(jià)格 庫存 購買數(shù)量
10mM (1mL in DMSO) 808.23 現(xiàn)貨
5mg 567.05 現(xiàn)貨
25mg 2204.08 現(xiàn)貨
100mg 6314.62 現(xiàn)貨
1g 10401.3 現(xiàn)貨
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常與Maraviroc一起在實(shí)驗(yàn)中被使用的化合物

Pembrolizumab (anti-PD-1)

Maraviroc和Pembrolizumab在轉(zhuǎn)移性結(jié)直腸癌的1期試驗(yàn)中顯示出陽性毒性模式。

Haag GM, et al. Eur J Cancer. 2022 May;167:112-122.

Leronlimab (anti-CCR5)

在RET細(xì)胞-細(xì)胞融合測定中，Maraviroc和Leronlimab(PRO-140)共同抑制HIV-1JR-FL包膜介導(dǎo)的膜融合。

Murga JD, et al. Antimicrob Agents Chemother. 2006 Oct;50(10):3289-96.

Etravirine

Maraviroc和Etravirine可用于挽救核苷逆轉(zhuǎn)錄酶抑制劑(NRTI)完全耐藥的患者。

Vallabhaneni S, et al. J Int AIDS Soc. 2013 Jun 3;16(1):18449.

Vicriviroc Malate

Maraviroc和Vicriviroc可減少免疫功能正常小鼠的前列腺癌細(xì)胞向骨骼、大腦和內(nèi)臟的轉(zhuǎn)移。

Jiao X, et al. Cancer Res. 2019 Oct 1;79(19):4801-4807.

Tenofovir Disoproxil Fumarate

Maraviroc和Tenofovir對孕激素受體B(PR-B)的激活具有背景特異性影響。

Enfield K, et al. Biochem Biophys Res Commun. 2020 Dec 17;533(4):1027-1033.

Maraviroc相關(guān)產(chǎn)品

相關(guān)信號通路圖

CCR Signaling Pathways

CCR信號通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)信息
TZM-bl Function assay 48 hrs Antagonist activity against CCR5 receptor in human TZM-bl cells assessed as inhibition of HIV-1 YU2-induced cell-cell fusion between viral envelope protein expressing human HEK293 cells to TZM-bl cells after 48 hrs by luciferase reporter gene assay, IC50 = 0.00043 μM. 24563723
TZM-bl Function assay 48 hrs Antagonist activity against CCR5 receptor in human TZM-bl cells assessed as inhibition of HIV-1 MGC26-induced cell-cell fusion between viral envelope protein expressing human HEK293 cells to TZM-bl cells after 48 hrs by luciferase reporter gene assay, IC50 = 0.00037 μM. 24563723
TZM-bl Function assay 3 days Inhibition of CCR5 in human TZM-bl cells infected with HIV1 Bal R5 assessed as antiviral activity by measuring reduction in viral infection pre-incubated with cells followed by viral infection measured after 3 days by luciferase reporter gene assay, IC50 = 0.0002 μM. 28082070
HeLa-P4 Function assay 20 hrs Antagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assay, IC50 = 0.0002 μM. 21128663
PM1 Antiviral assay 5 days Antiviral activity against CCR5-dependent HIV1 Ba-L infected in human PM1 cells assessed as reduction in virus infection measured after 5 days by luciferase reporter gene assay, IC50 = 0.001 μM. 30234300
SupT1 Antiviral assay 48 hrs Antiviral activity against HIV-1 infected in human SupT1 cells assessed as inhibition of viral infectivity after 48 hrs by luciferase reporter gene assay, IC50 = 0.0011 μM. 24316669
TZM-bl Function assay 48 hrs Antagonist activity against CCR5 receptor in human TZM-bl cells assessed as inhibition of HIV-1 92RW-induced cell-cell fusion between viral envelope protein expressing human HEK293 cells to TZM-bl cells after 48 hrs by luciferase reporter gene assay, IC50 = 0.0013 μM. 24563723
CHO Function assay 2 hrs Displacement of [128I]RANTES from human CCR5 receptor coexpressed with Galphai6 in CHO cells after 2 hrs by scintillation counting, IC50 = 0.0014 μM. 20137937
TZM-bl Function assay 48 hrs Antagonist activity against CCR5 receptor in human TZM-bl cells assessed as inhibition of HIV-1 JR-FL-induced cell-cell fusion between viral envelope protein expressing human HEK293 cells to TZM-bl cells after 48 hrs by luciferase reporter gene assay, IC50 = 0.0016 μM. 24563723
HOS Antiviral assay 5 days Antiviral activity against CCR5-dependent HIV1 Ba-L infected in human HOS cells assessed as reduction in virus infection measured after 5 days by luciferase reporter gene assay, IC50 = 0.0019 μM. 30234300
MOLT4 Function assay 15 mins Antagonist activity at CCR5 in Gqi5 transfected human MOLT4 cells assessed as inhibition of RANTES-stimulated Ca2+ influx preincubated for 15 mins followed by DAMGO challenge, IC50 = 0.0022 μM. 23682308
JC53-BL Antiviral assay 3 days Antiviral activity against CCR5-tropic recombinant HIV1 NLBal virus infected in JC53-BL cells assessed as inhibition of viral replication after 3 days by luciferase reporter gene assay, IC50 = 0.0028 μM. 20137937
JC53-BL Antiviral assay 3 days Antiviral activity against HIV1 NL4-3 infected in human JC53-BL cells assessed as luciferase activity after 3 days post infection, IC50 = 0.003 μM. 20417098
HOS Antiviral assay 5 days Antiviral activity against CCR5-dependent HIV1 SF162 infected in human HOS cells assessed as reduction in virus infection measured after 5 days by luciferase reporter gene assay, IC50 = 0.0047 μM. 30234300
NIH/3T3 Function assay 1 hr Displacement of [125I]-RANTES from CCR5 in mouse NIH/3T3 cells after 1 hr, IC50 = 0.0052 μM. 29425816
SupT1 Antiviral assay 48 hrs Antiviral activity against HIV1 infected in human SupT1 cells exposed to supernatant from HIV1 infected human 293T cells incubated for 48 hrs by firefly luciferase assay based single-cycle HIV1 replication assay, IC50 = 0.0055 μM. 25638498
TZM-bl Antiviral assay 48 hrs Antiviral activity against CCR5-dependent HIV1 SF162 infected in human TZM-bl cells assessed as reduction in virus infection measured after 48 hrs post infection by luciferase reporter gene assay, IC50 = 0.0067 μM. 30234300
HEK293 Function assay 10 mins Antagonist activity at CCR5 (unknown origin) expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of RANTES-induced calcium flux preincubated for 10 mins followed by RANTES addition by fluo-4AM-based fluorescence assay, IC50 = 0.008 μM. 30234300
CHO Function assay 10 mins Antagonist activity against CCR5 (unknown origin) expressed in CHO cells co-expressing Galpha16 incubated for 10 mins assessed as inhibition of RANTES-induced calcium mobilization, IC50 = 0.0131 μM. 25638498
CHO Function assay 10 mins Inhibition of CCR5 (unknown origin) expressed in CHO cells assessed as inhibition of RANTES-induced intracellular Ca2+ mobilization after 10 mins by Fluo-4 AM staining-based fluorescence assay, IC50 = 0.02543 μM. 24316669
HEK293 Function assay 1.5 mins Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay, IC50 = 17.3 μM. 23241029
HeLa-P4 Function assay Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay, IC50 = 0.0002 μM. 19171484
PM1 Antiviral assay Antiviral activity against HIV1 Bal infected in human PM1 cells assessed as inhibition of viral replication, IC90 = 0.0007 μM. 19171484
HOS Antiviral assay Antiviral activity against HIV1 Ba-L infected in HOS cells assessed as inhibition of viral infection, IC50 = 0.002 μM. 19664920
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells 29435139
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生物活性

產(chǎn)品描述 Maraviroc是一種CCR5拮抗劑，作用于MIP-1α，MIP-1β和RANTES，無細(xì)胞試驗(yàn)中IC50分別為3.3 nM，7.2 nM和5.2 nM。Maraviroc可應(yīng)用于治療HIV感染。
靶點(diǎn)
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
體外研究(In Vitro)
體外研究活性

Maraviroc 抑制MIP-1β刺激的γ-S-GTP 結(jié)合到HEK-293細(xì)胞膜上, 說明 Maraviroc 可抑制GDP-GTP 在CCR5/G 蛋白復(fù)合體上交換的趨化因子依賴性刺激。Maraviroc 也抑制趨化因子誘導(dǎo)的細(xì)胞內(nèi)鈣重新分配的下游事件，作用于 MIP-1β, MIP-1α 和RANTES時(shí)，IC50s 為 7 到 30 nM。在相同實(shí)驗(yàn)中, Maraviroc 即使?jié)舛雀哌_(dá)10 μM，也不會觸發(fā)細(xì)胞內(nèi)鈣釋放，說明Maraviroc 缺乏 CCR5興奮劑活性。與此相應(yīng)地, Maraviroc也不能誘導(dǎo)CCR5內(nèi)化。Maraviroc 低納摩爾濃度時(shí)，也有效作用于 HIV-1 Ba-L。 Maraviroc 抑制所有 200種假型病毒，平均IC90為13.7 nM。[1] 在濃度高達(dá)其IC50的1000倍時(shí)，Maraviroc對其他chemokine receptors (CCR1, 2, 3, 4, 7, 8; CXCR1, 2) 沒有相關(guān)臨床程度的抑制作用[3].
激酶實(shí)驗(yàn) 趨化因子與 CCR5結(jié)合的抑制作用
使用穩(wěn)定表達(dá)受體或膜及其制品的昆蟲HEK-293細(xì)胞測量125I-標(biāo)記的 MIP-1α, MIP-1β,和 RANTES 與CCR5結(jié)合情況。細(xì)胞按2 × 106 個(gè)細(xì)胞/ml的密度再懸浮在結(jié)合buffer (50 mM HEPES 含1 mM CaCl2, 5 mM MgCl2, 和 0.5%牛血清蛋白[BSA]，調(diào)節(jié)pH為 7.4) 中。為了制備膜，PBS沖洗的細(xì)胞再懸浮在 裂解 buffer (20 mM HEPES, 1 mM CaCl2, 1 片 COMPLETE /50 mL, pH 7.4)中，然后在Polytron 手持勻漿器中攪勻, 在40,000× g下超速離心30分鐘，再懸浮在 結(jié)合 buffer中，蛋白濃度為0.25 mg/mL (96-孔板的每孔中含 12.5 μg 膜蛋白)。制備125I-放射性標(biāo)記的 MIP-1α, MIP-1β, 和 RANTES ，在 結(jié)合 buffer中稀釋，終濃度為400 pM。每孔加入Maraviroc 稀釋液，終體積為100 μL, 實(shí)驗(yàn)板溫育1小時(shí), 通過預(yù)阻斷和沖洗的 Unifilter 板過濾，計(jì)數(shù)，烘干過夜。
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 PHA刺激的PBMC或PM-1細(xì)胞
濃度 0-1 μM
孵育時(shí)間 5天或7天
方法

在24孔組織培養(yǎng)板上進(jìn)行藥物敏感性試驗(yàn)。在DMSO中制備重復(fù)的8點(diǎn)連續(xù)稀釋Maraviroc，實(shí)驗(yàn)中DMSO終濃度為 0.1% (vol/vol)。PHA刺激的PBMC或PM-1細(xì)胞感染細(xì)胞，在37oC下進(jìn)行1小時(shí)。細(xì)胞隨后稀釋一次，3.6 × 105 PBMC 或2.0 × 105 PM-1細(xì)胞加到含稀釋 Maraviroc的每孔中。實(shí)驗(yàn)板在37oC下在含5% CO2 (vol/vol) 環(huán)境下溫育5天（實(shí)驗(yàn)室適應(yīng)株）或7天（原始分離株）。所有實(shí)驗(yàn)中含Saquinavir (一種 HIV-1 蛋白酶抑制劑) 和RANTES。
實(shí)驗(yàn)圖片 檢測方法 檢測指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western blot cleaved caspase-3 / cleaved caspase-9 / cleaved PARP / XIAP / Survivin / c-IAP1 / c-IAP2 / Bax / Bad / Bcl2 / Bcl-xl 28469959
體內(nèi)研究(In Vivo)
體內(nèi)研究活性

Maraviroc 作用于大鼠的半衰期為 0.9小時(shí)，作用于犬類的半衰期為2.3小時(shí)。 隨后Maraviroc按2 mg/kg劑量口服給藥犬類，1.5小時(shí)后達(dá)到 Cmax(256 ng/ml)，生物有效性為40%。Maraviroc作用于大鼠，大約 30% 給藥劑量從腸道吸收。[1]雌性RAG-hu小鼠陰道內(nèi)部加入 Maraviroc凝膠后，再陰道注入HIV-1 1小時(shí)。Maraviroc 凝膠處理的小鼠完全免受HIV-1 感染，而安慰劑處理的小鼠則全部感染。說明Maraviroc 完全保護(hù)小鼠免受 HIV-1 感染。在安慰劑處理的病毒感染小鼠內(nèi)，CD4 T細(xì)胞明顯下降，而Maraviroc 凝膠處理小鼠中水平穩(wěn)定。[2]
動物實(shí)驗(yàn) Animal Models 人性化的 BALB/c-Rag2?/?γc?/?和BALB/c-Rag1?/?γc?/? (RAG-hu)小鼠
Dosages ~64 μg
Administration 25μL凝膠配方小心地加到小鼠的陰道穹窿中。
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04966429 Recruiting
Post Stroke Cognitive Impairment
Tel-Aviv Sourasky Medical Center|Hadassah Medical Organization|Soroka University Medical Center
 May 1 2021 Phase 2
NCT04710199 Completed
Virus Diseases
Fundación Pública Andaluza para la gestión de la Investigación en Sevilla
 February 23 2021 Phase 2
NCT02881762 Completed
Hepatitis C|Human Immunodeficiency Virus
University of Maryland Baltimore|ViiV Healthcare
 June 1 2017 Phase 4
NCT02778204 Completed
HIV Infections
National Institute of Allergy and Infectious Diseases (NIAID)|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)|ViiV Healthcare|GlaxoSmithKline
 June 5 2017 Phase 1
NCT02741323 Completed
HIV Infections|Kidney Diseases
National Institute of Allergy and Infectious Diseases (NIAID)
 January 1 2017 Phase 2

化學(xué)信息&溶解度

分子量 513.67 分子式

C29H41F2N5O
CAS號 376348-65-1 SDF Download Maraviroc SDF
Smiles CC1=NN=C(N1C2CC3CCC(C2)N3CCC(C4=CC=CC=C4)NC(=O)C5CCC(CC5)(F)F)C(C)C
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 100 mg/mL ( (194.67 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 100 mg/mL (194.67 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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常見問題及建議解決方法

問題 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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