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  2. GPCR/G Protein
  3. Leukotriene Receptor LPL Receptor
  4. MK-571

MK-571 (L-660711) 是一種口服有效、選擇性的和競爭性的白三烯 D4 (LTD4) 受體拮抗劑，在豚鼠和人肺膜中的 Ki 值分別為 0.22 和 2.1 nM。MK-571 也是一種 MRP4 和 ABCC1 (MRP1) 抑制劑。MK-571 可抑制構(gòu)成性和抗原刺激的 S1P 釋放。

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MK-571 Chemical Structure

MK-571 Chemical Structure

CAS No. : 115104-28-4

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1 mg ￥344
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5 mg ￥780
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10 mg ￥1244
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25 mg ￥2400
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50 mg ￥4200
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100 mg ￥5880
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Other Forms of MK-571:

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  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

MK-571 (L-660711) is an orally active, potent and selective competitive leukotriene D4 (LTD4) receptor antagonist, with Ki values of 0.22 and 2.1 nM in guinea pig and human lung membranes, respectively. MK-571 is also a MRP4 and ABCC1 (MRP1) inhibitor. MK-571 inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release[1][2][3].

IC50 & Target[1]

LTD4

0.22 nM (Ki, In guinea pig lung)

LTD4

2.1 nM (Ki, In human lung)

LTD4

10.5 (pA2, on guinea pig ileum)

LTE4

10.4 (pA2, on guinea pig ileum)

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
0.06 μM
Compound: MK571
Potentiation of etoposide-induced cytotoxicity against HEK293 cells assessed as etoposide IC50 at 25000 nM after 72 hrs by CCK8 assay (Rvb = 0.11 +/- 0.03 nM)
Potentiation of etoposide-induced cytotoxicity against HEK293 cells assessed as etoposide IC50 at 25000 nM after 72 hrs by CCK8 assay (Rvb = 0.11 +/- 0.03 nM)
[PMID: 27504669]
HEK293 IC50
0.16 nM
Compound: MK-571
Effect on etoposide-induced cytotoxicity against HEK293 cells by measuring etoposide IC50 at 25 uM after 72 hrs by CCK8 assay (Rvb =0.21 +/- 0.04 uM)
Effect on etoposide-induced cytotoxicity against HEK293 cells by measuring etoposide IC50 at 25 uM after 72 hrs by CCK8 assay (Rvb =0.21 +/- 0.04 uM)
[PMID: 32347726]
HEK293 IC50
2.9 μM
Compound: MK-571
Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting
Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting
[PMID: 22541068]
HEK293 IC50
4.4 μM
Compound: MK-571
Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting
Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting
[PMID: 22541068]
HEK293 IC50
5.22 μM
Compound: MK571
Inhibition of human ABCC1 transfected in HEK293 cells assessed as potentiation of etoposide-induced cytotoxicity by measuring etoposide IC50 at 25000 nM after 72 hrs by CCK8 assay (Rvb = 38.54 +/- 5.62 nM)
Inhibition of human ABCC1 transfected in HEK293 cells assessed as potentiation of etoposide-induced cytotoxicity by measuring etoposide IC50 at 25000 nM after 72 hrs by CCK8 assay (Rvb = 38.54 +/- 5.62 nM)
[PMID: 27504669]
HEK293 IC50
6.4 μM
Compound: MK-571
Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting
Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting
[PMID: 22541068]
L929 IC50
> 100 μM
Compound: MK571
Cytotoxicity against mouse L929 cells assessed as reduction in cell survival after 5 days by MTS assay
Cytotoxicity against mouse L929 cells assessed as reduction in cell survival after 5 days by MTS assay
[PMID: 30351934]
MDCK IC50
> 1000 nM
Compound: MK-571
Inhibition of ABCC2 overexpressed in MDCK cells at 100 uM by flow cytometric-based chloromethylfluorescein-diacetate accumulation assay
Inhibition of ABCC2 overexpressed in MDCK cells at 100 uM by flow cytometric-based chloromethylfluorescein-diacetate accumulation assay
[PMID: 19170519]
MDCK EC50
2.85 μM
Compound: MK-571
Inhibition of MRP1 expressed in MDCK cells assessed as calcein AM accumulation by fluorescence assay
Inhibition of MRP1 expressed in MDCK cells assessed as calcein AM accumulation by fluorescence assay
[PMID: 20684594]
NCI-H69 EC50
12.4 μM
Compound: MK-571
Modulation of MRP1 mediated drug efflux in doxorubicin-resistant human H69 cells assessed as accumulation of calcein AM incubated for 15 mins prior to calcein AM addition measured after 30 mins by fluorescence analysis
Modulation of MRP1 mediated drug efflux in doxorubicin-resistant human H69 cells assessed as accumulation of calcein AM incubated for 15 mins prior to calcein AM addition measured after 30 mins by fluorescence analysis
[PMID: 25311564]
體外研究
(In Vitro)

MK571（15 μM，1 小時）顯著抑制 RBL-2H3 細胞和肥大細胞的組成型和 Ag 刺激的 S1P 分泌，并抑制 Fluo-3 外排[3]。

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

Cell Viability Assay[3]

Cell Line: RBL-2H3 cells, human LAD2 mast cells
Concentration: 15 μM
Incubation Time: 1 h
Result: Inhibited S1P secretion by vector and SphK1 transfected RBL-2H3 cells, whereas it did not affect uptake and intracellular conversion of [3H]Sph to S1P. Inhibited Fluo-3 efflux, inhibited S1P export by LAD2 cells, and blocked Ag-stimulated release of S1P.
體內(nèi)研究
(In Vivo)

MK-571（0-0.5 mg/kg，口服，一次）對接受美西麥角 (3 μg/kg) 治療的清醒致敏大鼠中抗原誘導的呼吸困難持續(xù)時間產(chǎn)生劑量依賴性抑制[1]。
MK-571（0-1 mg/kg，口服，一次）可阻斷有意識的松鼠猴中 LTD4- 和蛔蟲誘導的支氣管收縮[1]。
MK-571（0-25 mg/kg，口服，每天，持續(xù) 2 周以上）可逆轉(zhuǎn)缺氧性肺動脈高壓 (PH)，并保護小鼠免受缺氧性 PH 的影響[2]。

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

Animal Model: Hyperreactive rats (male and female, 200-400 g, pretreated intravenously with 3 μg/kg methysergide, 5 min before antigen chdlenge)[1]
Dosage: 0.5, 0.15, and 0.05 mg/kg
Administration: Orally, once, 1 or 4 h before challenge
Result: Produced dose-dependent inhibition of the duration of antigen-induced dyspnea, with ED50 values of 0.13 (95% confidence interval (CI), 0.03-0.62) and 0.11 (95% CI, 0.009-1.47) mg/kg, respectively. MK-571 was even more active when administered orally as a suspension in 1% Methocel (4 h pretreatment), with an ED50 of 0.068 (95% CI, 0.83-0.14) mg/kg.
Animal Model: Csnscisus squirrel msnkeys[1]
Dosage: 0.1, 0.5, and 1 mg/kg
Administration: Orally, once, 2 h prior to challenge with Ascaris antigen
Result: Produced significant inhibition of the bronchoconstriction at 0.5 mg/kg, produced significant inhibition of the increases in RL and decreases in Cdyn at 1 mg/kg.
Animal Model: FVB (Friend virus B-type) mice (Mrp4–/– and WT, 6 weeks old, exposed to chronic hypoxia (10% O2) in a ventilated chamber for 28 days)[2]
Dosage: 0, 5, and 25 mg/kg
Administration: Orally, daily, for 2 more weeks, maintain in hypoxic conditions
Result: Showed reversal of hypoxic pulmonary hypertension (PH), and mice were protected from hypoxic PH. MK-571-treated mice displayed lower RVSP and Fulton index and a decrease in the medial thickening of small pulmonary arteries and arterioles.
分子量

515.09

Formula

C26H27ClN2O3S2
CAS 號
性狀

固體

顏色

Off-white to light yellow

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : 125 mg/mL (242.68 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 1.9414 mL 9.7070 mL 19.4141 mL
5 mM 0.3883 mL 1.9414 mL 3.8828 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 98.66%

參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9414 mL 9.7070 mL 19.4141 mL 48.5352 mL
5 mM 0.3883 mL 1.9414 mL 3.8828 mL 9.7070 mL
10 mM 0.1941 mL 0.9707 mL 1.9414 mL 4.8535 mL
15 mM 0.1294 mL 0.6471 mL 1.2943 mL 3.2357 mL
20 mM 0.0971 mL 0.4854 mL 0.9707 mL 2.4268 mL
25 mM 0.0777 mL 0.3883 mL 0.7766 mL 1.9414 mL
30 mM 0.0647 mL 0.3236 mL 0.6471 mL 1.6178 mL
40 mM 0.0485 mL 0.2427 mL 0.4854 mL 1.2134 mL
50 mM 0.0388 mL 0.1941 mL 0.3883 mL 0.9707 mL
60 mM 0.0324 mL 0.1618 mL 0.3236 mL 0.8089 mL
80 mM 0.0243 mL 0.1213 mL 0.2427 mL 0.6067 mL
100 mM 0.0194 mL 0.0971 mL 0.1941 mL 0.4854 mL
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產(chǎn)品名稱：
MK-571
目錄號：
HY-19989
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