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

MK-571  (Synonyms: L-660711)

目錄號(hào): HY-19989 純度: 98.56%
COA 產(chǎn)品使用指南

MK-571 (L-660711) 是一種口服有效、選擇性的和競(jìng)爭(zhēng)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 MRP4ABCC1 (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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Customer Review

Other Forms of MK-571:

查看 Leukotriene Receptor 亞型特異性產(chǎn)品:

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  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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)

體外研究
(In Vitro)

MK571(15 μM,1 小時(shí))顯著抑制 RBL-2H3 細(xì)胞和肥大細(xì)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(duì)接受美西麥角 (3 μg/kg) 治療的清醒致敏大鼠中抗原誘導(dǎo)的呼吸困難持續(xù)時(shí)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(shí)的松鼠猴中 LTD4- 和蛔蟲誘導(dǎo)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(dòng)脈高壓 (PH),并保護(hù)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(hào)
性狀

固體

顏色

Off-white to light yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)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(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 175 mg/mL (339.75 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)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(chǔ)備液配制表

* 請(qǐng)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(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)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(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過(guò)程有損耗,建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)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(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)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
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.

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產(chǎn)品名稱:
MK-571
目錄號(hào):
HY-19989
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