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  1. Neuronal Signaling Apoptosis
  2. Monoamine Oxidase Apoptosis
  3. Isatin

Isatin  (Synonyms: 吲哚-2,3-二酮; Indoline-2,3-dione)

目錄號(hào): HY-Y0265 純度: 99.89%
COA 產(chǎn)品使用指南 技術(shù)支持

Isatin (Indoline-2,3-dione) 是單胺氧化酶 (MAO)的有效抑制劑,IC50 為3 μM。 也與中樞苯二氮卓受體結(jié)合 (對(duì)抗氯硝西泮IC50=123 μM)。 還充當(dāng)心房鈉尿肽刺激和一氧化氮刺激的鳥(niǎo)苷酸環(huán)化酶拮抗劑。 對(duì)5-羥色胺系統(tǒng)有影響。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào),我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Isatin Chemical Structure

Isatin Chemical Structure

CAS No. : 91-56-5

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10 mM * 1 mL in DMSO ¥110
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500 mg ¥100
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Customer Review

Other Forms of Isatin:

查看 Monoamine Oxidase 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Isatin (Indoline-2,3-dione) is a potent inhibitor of monoamine oxidase (MAO) with an IC50 of 3 μM. Also binds to central benzodiazepine receptors (IC50 against clonazepam, 123 μM)[1]. Also acts as an antagonist of both atrial natriuretic peptide stimulated and nitric oxide-stimulated guanylate cyclase activity[2]. Shows effect on the serotonergic system[3].

IC50 & Target

IC50: 3 μM (MAO B)[1]

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
13.5 μM
Compound: 1
Cytotoxicity against human A549 cells after 48 hrs by MTT assay
Cytotoxicity against human A549 cells after 48 hrs by MTT assay
[PMID: 22386528]
BTI-TN-5B1-4 IC50
18.75 μM
Compound: Is
Inhibition of human MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate incubated for 15 mins prior to substrate addition measured for 15 mins by Amplex red assay
Inhibition of human MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate incubated for 15 mins prior to substrate addition measured for 15 mins by Amplex red assay
[PMID: 23153812]
BTI-TN-5B1-4 IC50
18.75 μM
Compound: Isatin
Inhibition of human recombinant MAOB expressed in baculovirus infected insect BTI-TN-5B1-4 cells assessed as production of hydrogen peroxide from p-tyramine by amplex red assay
Inhibition of human recombinant MAOB expressed in baculovirus infected insect BTI-TN-5B1-4 cells assessed as production of hydrogen peroxide from p-tyramine by amplex red assay
[PMID: 20715818]
BTI-TN-5B1-4 IC50
18.75 μM
Compound: Isatin
Inhibition of human recombinant MAO-B expressed in baculovirus-infected BTI-TN-5B1-4 cell microsomes assessed as decrease in H2O2 production using p-tyramine as substrate preincubated for 15 mins by Amplex Red reagent based fluorimetric method
Inhibition of human recombinant MAO-B expressed in baculovirus-infected BTI-TN-5B1-4 cell microsomes assessed as decrease in H2O2 production using p-tyramine as substrate preincubated for 15 mins by Amplex Red reagent based fluorimetric method
[PMID: 24746464]
BTI-TN-5B1-4 IC50
18.75 μM
Compound: Isatin
Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as production of hydrogen peroxide from p-tyramine after 15 mins by microplate fluorescence assay
Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as production of hydrogen peroxide from p-tyramine after 15 mins by microplate fluorescence assay
[PMID: 21872365]
BTI-TN-5B1-4 IC50
18.75 μM
Compound: Is
Inhibition of human MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate assessed as hydrogen peroxide production by fluorimetric method
Inhibition of human MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate assessed as hydrogen peroxide production by fluorimetric method
10.1039/C0MD00014K
BTI-TN-5B1-4 IC50
18754 nM
Compound: isatin
Inhibition of human recombinant MAOB expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine by amplex red assay
Inhibition of human recombinant MAOB expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine by amplex red assay
[PMID: 20579890]
BTI-TN-5B1-4 IC50
34.39 μM
Compound: Isatin
Inhibition of human recombinant microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate assessed as reduction in H2O2 production preincubated for 15 mins followed by substrate addition measured for 15 mins Ample
Inhibition of human recombinant microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate assessed as reduction in H2O2 production preincubated for 15 mins followed by substrate addition measured for 15 mins Ample
[PMID: 27135371]
BTI-TN-5B1-4 IC50
40 μM
Compound: Isatin
Inhibition of human recombinant MAOA expressed in baculovirus infected insect BTI-TN-5B1-4 cells assessed as production of hydrogen peroxide from p-tyramine by amplex red assay
Inhibition of human recombinant MAOA expressed in baculovirus infected insect BTI-TN-5B1-4 cells assessed as production of hydrogen peroxide from p-tyramine by amplex red assay
[PMID: 20715818]
HepG2 IC50
> 10 μM
Compound: 1a
Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
[PMID: 30055465]
HepG2 IC50
> 10 μM
Compound: 1a
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
[PMID: 24360564]
HT-29 IC50
> 10 μM
Compound: 1a
Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay
Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay
[PMID: 24360564]
Jurkat IC50
> 10 μM
Compound: 1a
Anticancer activity against human Jurkat cells after 48 hrs by MTT assay
Anticancer activity against human Jurkat cells after 48 hrs by MTT assay
[PMID: 26890120]
K562 IC50
> 10 μM
Compound: 1a
Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
Antiproliferative activity against human K562 cells after 48 hrs by MTT assay
[PMID: 30055465]
K562 IC50
> 10 μM
Compound: 1a
Cytotoxicity against human K562 cells after 48 hrs by MTT assay
Cytotoxicity against human K562 cells after 48 hrs by MTT assay
[PMID: 24360564]
KB 3-1 IC50
> 50 μM
Compound: 8
Cytotoxicity against human P-gp-negative KB-3-1 cells after 72 hrs by MTT assay
Cytotoxicity against human P-gp-negative KB-3-1 cells after 72 hrs by MTT assay
[PMID: 19397322]
KB-V1 IC50
> 50 μM
Compound: 8
Cytotoxicity against human P-glycoprotein-expressing KBV1 cells after 72 hrs by MTT assay
Cytotoxicity against human P-glycoprotein-expressing KBV1 cells after 72 hrs by MTT assay
[PMID: 19397322]
MDA-MB-231 IC50
> 100 μM
Compound: 1
Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay
[PMID: 22386528]
MRC5 IC50
> 100 μM
Compound: 1
Cytotoxicity against human MRC5 cells after 48 hrs by MTT assay
Cytotoxicity against human MRC5 cells after 48 hrs by MTT assay
[PMID: 22386528]
SK-N-SH IC50
9.84 μM
Compound: 1
Cytotoxicity against human SK-N-SH cells after 48 hrs by MTT assay
Cytotoxicity against human SK-N-SH cells after 48 hrs by MTT assay
[PMID: 22386528]
體外研究
(In Vitro)

In dopaminergic SH-SY5Y cells isatin (1-400 μM) induces cell death in dose- and time dependent manner. This death occurred as a continuum of survival, apoptosis and necrosis[2].

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

體內(nèi)研究
(In Vivo)

A single dose of isatin (80 mg/kg) has a rapid effect on the serotonergic system in the hypothalamus. Isatin significantly increases 5-HT concentrations in the hypothalamus and cortex but did not significantly alter 5-HIAA concentrations[3].

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

分子量

147.13

Formula

C8H5NO2

CAS 號(hào)
性狀

固體

顏色

Yellow to orange

中文名稱(chēng)

靛紅;吲哚-2,3-二酮

結(jié)構(gòu)分類(lèi)
初始來(lái)源
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 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 100 mg/mL (679.66 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(kāi)封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 6.7966 mL 33.9829 mL 67.9657 mL
5 mM 1.3593 mL 6.7966 mL 13.5931 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。-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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.75 mg/mL (18.69 mM); 澄清溶液

    此方案可獲得 ≥ 2.75 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 27.5 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

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: 99.89%

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。-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 6.7966 mL 33.9829 mL 67.9657 mL 169.9143 mL
5 mM 1.3593 mL 6.7966 mL 13.5931 mL 33.9829 mL
10 mM 0.6797 mL 3.3983 mL 6.7966 mL 16.9914 mL
15 mM 0.4531 mL 2.2655 mL 4.5310 mL 11.3276 mL
20 mM 0.3398 mL 1.6991 mL 3.3983 mL 8.4957 mL
25 mM 0.2719 mL 1.3593 mL 2.7186 mL 6.7966 mL
30 mM 0.2266 mL 1.1328 mL 2.2655 mL 5.6638 mL
40 mM 0.1699 mL 0.8496 mL 1.6991 mL 4.2479 mL
50 mM 0.1359 mL 0.6797 mL 1.3593 mL 3.3983 mL
60 mM 0.1133 mL 0.5664 mL 1.1328 mL 2.8319 mL
80 mM 0.0850 mL 0.4248 mL 0.8496 mL 2.1239 mL
100 mM 0.0680 mL 0.3398 mL 0.6797 mL 1.6991 mL
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產(chǎn)品名稱(chēng):
Isatin
目錄號(hào):
HY-Y0265
需求量: