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  2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Autophagy Neuronal Signaling Membrane Transporter/Ion Channel
  3. Mineralocorticoid Receptor Androgen Receptor Autophagy Calcium Channel
  4. Spironolactone

Spironolactone  (Synonyms: 螺內(nèi)酯; SC9420)

目錄號(hào): HY-B0561 純度: 99.66%
COA 產(chǎn)品使用指南 技術(shù)支持

Spironolactone 是一種醛固酮拮抗劑，作用于醛固酮礦物質(zhì)皮質(zhì)激素受體 (IC50=24 nM) 和雄性激素受體 (IC50=77 nM)，促進(jìn)足細(xì)胞自噬 (autophagy) 并調(diào)節(jié)疼痛。Spironolactone 通過(guò)減少血管緊張素 II 誘導(dǎo)的炎癥改善高血壓相關(guān)的血管肥大和重構(gòu)，并通過(guò) PIT1 依賴(lài)性信號(hào)減少醛固酮引起的血管及軟組織鈣化，還能通過(guò)降低氧化應(yīng)激和恢復(fù) NO/GC 信號(hào)傳導(dǎo)減輕 Ⅱ 型糖尿病小鼠的血管功能障礙；低濃度時(shí)，它及其代謝物可干擾腎上腺皮質(zhì)中醛固酮的生物合成，并抑制電壓依賴(lài)性 Ca2+ 通道以發(fā)揮抗高血壓作用。

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Spironolactone Chemical Structure

Spironolactone Chemical Structure

CAS No. : 52-01-7

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥550
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100 mg ￥500
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1 g ￥650
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5 g ￥1200
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10 g   詢(xún)價(jià)  
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Customer Review

Other Forms of Spironolactone:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Spironolactone is an aldosterone antagonist that acts on the aldosterone mineralocorticoid receptor (IC50=24 nM) and androgen receptor (IC50=77 nM), promotes podocyte autophagy and regulates pain. Spironolactone improves hypertension-related vascular hypertrophy and remodeling by reducing angiotensin II (AngⅡ)-induced inflammation, reduces aldosterone-induced vascular and soft tissue calcification through PIT1-dependent signaling, and alleviates vascular dysfunction in type Ⅱ diabetic mice by reducing oxidative stress and restoring NO/GC signaling; at low concentrations, it and its metabolites can interfere with aldosterone biosynthesis in the adrenal cortex and inhibit voltage-dependent Ca2+ channels to exert antihypertensive effects[1][2][3][4][5][6][7][8][9][10].

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO-K1 IC50
0.67 μM
Compound: B, SPL
Antagonist activity at human androgen receptor expressed in CHOK1 cells assessed as inhibition of D(-)-norgestrel-induced protein interaction with steroid receptor co-activator peptide after 24 hrs by beta-galactosidase reporter gene assay
Antagonist activity at human androgen receptor expressed in CHOK1 cells assessed as inhibition of D(-)-norgestrel-induced protein interaction with steroid receptor co-activator peptide after 24 hrs by beta-galactosidase reporter gene assay
[PMID: 25941555]
COS-1 IC50
60 nM
Compound: Spironolactone
Antagonist activity at human mineralocorticoid receptor expressed in COS1 cells after 1 day by luciferase reporter gene assay
Antagonist activity at human mineralocorticoid receptor expressed in COS1 cells after 1 day by luciferase reporter gene assay
[PMID: 25187277]
COS-1 IC50
60 nM
Compound: Spironolactone
Antagonist activity at human MR transfected in human COS1 cells after 1 day by luciferase reporter gene assay
Antagonist activity at human MR transfected in human COS1 cells after 1 day by luciferase reporter gene assay
[PMID: 22074142]
COS-7 IC50
1.6 nM
Compound: Spironolactone
Antagonist activity at mineralocorticoid receptor ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay
Antagonist activity at mineralocorticoid receptor ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay
[PMID: 19863083]
HEK293 IC50
18.6 μM
Compound: spironolactone
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
[PMID: 23241029]
HEK293 IC50
49 nM
Compound: Spironolactone
Displacement of [3H]aldosterone from cytosolic human MR expressed in HEK293 cells after 16 hrs by scintillation counting
Displacement of [3H]aldosterone from cytosolic human MR expressed in HEK293 cells after 16 hrs by scintillation counting
[PMID: 22074142]
Huh-7 IC50
13 nM
Compound: spironolactone
Antagonist activity at Gal4-tagged mineralocorticoid receptor expressed in human Huh7 cells by luciferase reporter gene assay
Antagonist activity at Gal4-tagged mineralocorticoid receptor expressed in human Huh7 cells by luciferase reporter gene assay
[PMID: 20672822]
體外研究
(In Vitro)

Spironolactone 顯著抑制 A7r5 細(xì)胞中血管緊張素 Ⅱ (AngⅡ) 介導(dǎo)的 ERK 和 AKT 磷酸化，而不影響 EGFR 磷酸化[1]。
Spironolactone 在人主動(dòng)脈平滑肌細(xì)胞中，以劑量依賴(lài)方式增加 PIT1 表達(dá)，逆轉(zhuǎn)醛固酮的作用[2]。
Spironolactone (0, 100 nM, 1 μM, 10 μM，30 min) 抑制 AngⅡ 誘導(dǎo)的炎癥[5]。
Spironolactone 提高了足細(xì)胞特異性標(biāo)志物 WT1 和 NPHS2 以及自噬標(biāo)志物 Beclin1 和 LC3B 的表達(dá)，促進(jìn)細(xì)胞自噬[10]。

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

Real Time qPCR[2]

Cell Line: HAoSMCs (induced by 100 nM aldosterone)
Concentration: 10 μM
Incubation Time: 24 h
Result: Inhibited the mRNA expression of PITI, TNFA, MSX2, CBFA1 and ALPL.

Western Blot Analysis[5]

Cell Line: Angiotensin II-induced hu-PBMC
Concentration: 0, 100 nM, 1 μM, 10 μM
Incubation Time: 30 min
Result: Inhibited the expression of monocyte chemoattractant protein-1 (MCP-1) and tumor necrosis factor-α (TNF-α).
體內(nèi)研究
(In Vivo)

Spironolactone 阻斷醛固酮 (ALDO)，可恢復(fù)長(zhǎng)期腎素-血管緊張素系統(tǒng) (RAS) 增強(qiáng)引起的血管重構(gòu)[1]。
Spironolactone (80 mg/L，口服) 延長(zhǎng)了 mesothelin 基因突變小鼠的壽命，減少醛固酮引起的血管和軟組織鈣化[2]。
Spironolactone (10-80 mg/mL，皮下注射) 在雄性瑞士白化小鼠熱痛和電痛模型中以劑量依賴(lài)方式增加疼痛行為，但減少了由腹腔醋酸引起的炎癥性?xún)?nèi)臟疼痛及足底辣椒素引起的化學(xué)性疼痛[3]。
Spironolactone (50 mg/kg，每日一次，持續(xù) 6 周，口服) 能降低糖尿病相關(guān)的血管氧化應(yīng)激，并通過(guò)增加抗氧化酶和可溶性胍基環(huán)化酶 (sGC) 的表達(dá)預(yù)防血管功能障礙[4]。
Spironolactone (40mg/kg，每天一次，8 周，灌胃) 降低尿白蛋白排泄、血脂和空腹血糖水平，減輕腎損害，促進(jìn)自噬減輕足細(xì)胞損失[10]。

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

Animal Model: Hypertensive transgenic mice that overproduce angiotensin II (AngII)[1]
Dosage: 20 mg/kg; Once day; 4 weeks
Administration: i.h.
Result: Eliminated intimal hyperplasia and medial hypertrophy, inhibited the expression of osteopontin (OPN), and had an inhibitory effect on AngII.
Animal Model: Klotho-hypomorphic mice (kl/kl mice)[2]
Dosage: 80 mg/L
Administration: Oral gavage (p.o.)
Result: Increased mouse lifespan, did not significantly improve hypercalcemia, hyperphosphatemia or excess 1,25(OH)2D3 and FGF23 plasma concentrations, reduced tissue calcification in kl/kl mice, reduced PIT1, osteoblast differentiation Promoter for expression of Tnfa, Alpl, Msx2, Cbfa1, Osx.
Animal Model: Male Swiss albino mice[3]
Dosage: 10, 20, 40 or 80 mg/kg
Administration: Subcutaneous injection (s.c.) for Hot-plate assay, Tail electric stimulation test, Capsaicin-induced hind paw licking; Oral gavage (p.o.) for Acetic acid-induced writhing; i.p. for Rotarod testing
Result: Reduced response latency in the hot plate test. Lowering the nociceptive threshold of electrically induced pain in mice. Caused significant anti-pain effects in acetic acid-induced writhing experiments in mice and reduced capsaicin-induced chemical pain at doses of 20-160 mg/kg. Reduced locomotor activity in mice and produced significant impairment in the rotation test at doses of 40 or 80 mg/kg.
Animal Model: Leptin receptor knockout (db/db) mice, a model of DM2[4]
Dosage: 50 mg/kg , daily, 6 weeks
Administration: Oral gavage (p.o.)
Result: Eliminated endothelial dysfunction in the arteries of db/db mice, increased endothelial nitric oxide synthase (eNOS) phosphorylation (Ser1177), increased the expression of superoxide dismutase-1 and catalase in the arteries of db/db mice, improved relaxation induced by sodium nitroprusside and BAY 41-2277, and increased the expression of soluble corona yl cyclase (sGC) β subunit.
Animal Model: SD rat diabetic nephropathy (DN) model[10]
Dosage: 40mg/kg, daily, 8weeks
Administration: i.g.
Result: Decreased blood lipid and blood glucose levels, improved liver and kidney function, reduced urinary albumin excretion, restored podocyte morphology to relative normality, and autophagic vacuoles could be seen in podocytes.
Clinical Trial
分子量

416.57

Formula

C24H32O4S
CAS 號(hào)
性狀

固體

顏色

White to off-white

中文名稱(chēng)

螺內(nèi)酯；螺內(nèi)脂；螺甾內(nèi)酯
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : ≥ 50 mg/mL (120.03 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.4006 mL 12.0028 mL 24.0056 mL
5 mM 0.4801 mL 2.4006 mL 4.8011 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, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(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)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.00 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.00 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
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

只
由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.66%

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, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(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 2.4006 mL 12.0028 mL 24.0056 mL 60.0139 mL
5 mM 0.4801 mL 2.4006 mL 4.8011 mL 12.0028 mL
10 mM 0.2401 mL 1.2003 mL 2.4006 mL 6.0014 mL
15 mM 0.1600 mL 0.8002 mL 1.6004 mL 4.0009 mL
20 mM 0.1200 mL 0.6001 mL 1.2003 mL 3.0007 mL
25 mM 0.0960 mL 0.4801 mL 0.9602 mL 2.4006 mL
30 mM 0.0800 mL 0.4001 mL 0.8002 mL 2.0005 mL
40 mM 0.0600 mL 0.3001 mL 0.6001 mL 1.5003 mL
50 mM 0.0480 mL 0.2401 mL 0.4801 mL 1.2003 mL
60 mM 0.0400 mL 0.2000 mL 0.4001 mL 1.0002 mL
80 mM 0.0300 mL 0.1500 mL 0.3001 mL 0.7502 mL
100 mM 0.0240 mL 0.1200 mL 0.2401 mL 0.6001 mL
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產(chǎn)品名稱(chēng)：
Spironolactone
目錄號(hào)：
HY-B0561
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