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  1. Membrane Transporter/Ion Channel Neuronal Signaling Metabolic Enzyme/Protease Protein Tyrosine Kinase/RTK
  2. iGluR Tyrosinase c-Met/HGFR Glutaminase
  3. Decanoic acid

Decanoic acid 是椰子油中發(fā)現(xiàn)的中鏈甘油三酯 (MCT) 的關(guān)鍵成分。Decanoic acid 是一種具有腦滲透和非競(jìng)爭(zhēng)性的 AMPA 受體抑制劑,在大鼠中具有抗癲癇活性。Decanoic acid 降低 tyrosinase 活性,抑制 melanosome 成熟。Decanoic acid 通過(guò)抑制多種致癌蛋白的表達(dá),抑制肝癌細(xì)胞 c-Met 的磷酸化,誘導(dǎo)細(xì)胞凋亡,有望用于在 mTORC1 信號(hào)通路、肝癌和癲癇等領(lǐng)域的研究。

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Decanoic acid Chemical Structure

Decanoic acid Chemical Structure

CAS No. : 334-48-5

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10 mM * 1 mL in DMSO ¥500
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Other Forms of Decanoic acid:

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

查看 iGluR 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

Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy[1][2][3].

IC50 & Target

Human Endogenous Metabolite

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO EC50
30 μM
Compound: 1
Agonist activity at recombinant human N-terminally HA-tagged GPR84 expressed in CHO cells co-expressing Gqi5 assessed as inhibition of forskolin-induced cAMP accumulation by fluo-4AM dye based FLIPR assay
Agonist activity at recombinant human N-terminally HA-tagged GPR84 expressed in CHO cells co-expressing Gqi5 assessed as inhibition of forskolin-induced cAMP accumulation by fluo-4AM dye based FLIPR assay
[PMID: 31721581]
CHO EC50
4.6 μM
Compound: 1
Agonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
Agonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method
[PMID: 31721581]
CHO EC50
4.6 μM
Compound: 1
Agonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin addition and measured after 20 mins
Agonist activity at human N-terminal FLAG-tagged GPR84 receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin addition and measured after 20 mins
[PMID: 31721581]
CHO EC50
48 μM
Compound: 1
Agonist activity at recombinant human GPR84 expressed in CHO cells co-expressing Galpha16/Gqs5/Gqo5/Gqi9 assessed as increase in calcium mobilization measured for 20 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
Agonist activity at recombinant human GPR84 expressed in CHO cells co-expressing Galpha16/Gqs5/Gqo5/Gqi9 assessed as increase in calcium mobilization measured for 20 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
[PMID: 31721581]
HEK293 EC50
10 μM
Compound: 1
Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assay
Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assay
[PMID: 31721581]
MONO-MAC-6 IC50
> 200 μM
Compound: Decanoic acid
Cytostatic activity against human MONO-MAC-6 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Cytostatic activity against human MONO-MAC-6 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
[PMID: 28384546]
Sf9 EC50
48 μM
Compound: 1
Agonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by liquid scintillation counting method
Agonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 30 mins by liquid scintillation counting method
[PMID: 31721581]
體外研究
(In Vitro)

Decanoic acid (60 μM, 1 h 或 24 h) 在 Dictyostelium 中靶向 mTORC1 獨(dú)立于 PI3K/AKT,AMPK 信號(hào)傳導(dǎo),并且在不改變 mTORC2 激活的情況下抑制 mTORC1,還降低 Ddp97 的活性[1]
Decanoic acid (300 μM, 24 h) 降低 p-4E-BP1/total-4E-BP1 和 p-S6K/total-S6K 的比值,以降低結(jié)節(jié)性硬化癥患者源性星形膠質(zhì)細(xì)胞的 mTORC1 活性[1]
Decanoic acid (80 μM, 2 h 30 min) 降低細(xì)胞活力,抑制 HCCLM3 和 HepG2 細(xì)胞里肝細(xì)胞生長(zhǎng)因子 (HGF) 誘導(dǎo)的 c-Met 磷酸化[2]。
Decanoic acid (80 μM, 24 h) 在 HCCLM3、HepG2 和 HGF 誘導(dǎo)的細(xì)胞中觸發(fā)凋亡[2]。
Decanoic acid (0.3 mM or 1 mM, 灌注, 40 min) 在表達(dá)同源 (GluA1 亞基) 和異源 (GluA1/2 和 GluA2/3) AMPA 受體的卵母細(xì)胞中以亞基依賴(lài)性、非競(jìng)爭(zhēng)性和電壓依賴(lài)性的方式成為一種廣譜 AMPA 受體抑制劑[3]

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

Cell Viability Assay[1]

Cell Line: Dictyostelium cells
Concentration: 0 - 80 μM
Incubation Time: 50 h
Result: Decreased p-4E-BP1 levels, but had no significant difference in p-AKT-S and p-AMPK levels at 1 h and 24 h in dictyostelium cells.

Western Blot Analysis[1]

Cell Line: Astrocytes derived from patients with tuberous sclerosis complex
Concentration: 300 μM
Incubation Time: 24 h
Result: Reduced the ratio of p-4E-BP1/total-4E-BP1 and p-S6K/total-S6K in astrocytes derived from control patients and patients with mutations in TSC1.

Cell Viability Assay[2]

Cell Line: HCCLM3 and HepG2 cells
Concentration: 0 - 80 μM
Incubation Time: 50 h
Result: Reduced the cell viability in HGF-induced/uninduced HCC cells.

Western Blot Analysis[2]

Cell Line: HCCLM3 and HepG2 cells
Concentration: 80 μM
Incubation Time: 2 h 30 min
Result: Suppressed constitutive as well as HGF-induced c-Met phosphorylation in both HCCLM3 and HepG2 cells.

Apoptosis Analysis[2]

Cell Line: HCCLM3, HepG2 and HGF-induced cells
Concentration: 80 μM
Incubation Time: 24 h
Result: Downregulated the levels of antiapoptotic proteins such as Bcl-2, Survivin, IAP-1, Cyclin D1, and COX-2 in HCCLM3, HepG2 and HGF-induced cells.
體內(nèi)研究
(In Vivo)

Decanoic acid (100 μM 和 300 μM, 1 小時(shí)) 顯著降低血漿 PTH 濃度,并且在較高的流速下降低 Cyp24a1 在腎臟的表達(dá)。此外,在 Dictyostelium 和大鼠海馬切片中,Decanoic acid 對(duì) p-AKT(Thr308)/total-AKT 或 p-AKT(Ser473)/total-AKT 均無(wú)影響[1]。
Decanoic acid (50 mg/kg, i.p., 一周三次,連續(xù)四周) 在肝細(xì)胞癌小鼠模型中有效減輕腫瘤發(fā)生而不顯示毒性[2]。

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

Animal Model: Rat Hippocampal Slices[1]
Dosage: 100 μM and 300 μM
Administration: 1 h
Result: Decreased p-4E-BP1/total-4E-BP1 levels at 300 μM in rat hippocampal slices
Animal Model: NCr-nude female mice[2]
Dosage: 5, 50, 100 mg/kg (0.1% DMSO)
Administration: i.p., measured body weight daily for 8 days
Result: Caused no substantial effects on body weight and on the levels of various enzymes in the liver and kidney of mice
Animal Model: HCC mouse model[2]
Dosage: 50 mg/kg (0.1% DMSO)
Administration: i.p., thrice a week for four weeks
Result: Significantly regressed the growth of tumors in the HCC mouse model
分子量

172.27

Formula

C10H20O2

CAS 號(hào)
性狀

<27°C 固體,>32°C 液體

顏色

Colorless to off-white

中文名稱(chēng)

癸酸;正癸酸;羊蠟酸;十烷酸

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

Store at room temperature 3 years

In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : ≥ 130 mg/mL (754.63 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)

* "≥" 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 5.8048 mL 29.0242 mL 58.0484 mL
5 mM 1.1610 mL 5.8048 mL 11.6097 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, 2 years; -20°C, 1 year。-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)?年內(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: ≥ 2.17 mg/mL (12.60 mM); 澄清溶液

    此方案可獲得 ≥ 2.17 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 21.7 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: ≥ 2.17 mg/mL (12.60 mM); 澄清溶液

    此方案可獲得 ≥ 2.17 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 21.7 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: ≥98.0%

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, 2 years; -20°C, 1 year。-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)?年內(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 5.8048 mL 29.0242 mL 58.0484 mL 145.1210 mL
5 mM 1.1610 mL 5.8048 mL 11.6097 mL 29.0242 mL
10 mM 0.5805 mL 2.9024 mL 5.8048 mL 14.5121 mL
15 mM 0.3870 mL 1.9349 mL 3.8699 mL 9.6747 mL
20 mM 0.2902 mL 1.4512 mL 2.9024 mL 7.2561 mL
25 mM 0.2322 mL 1.1610 mL 2.3219 mL 5.8048 mL
30 mM 0.1935 mL 0.9675 mL 1.9349 mL 4.8374 mL
40 mM 0.1451 mL 0.7256 mL 1.4512 mL 3.6280 mL
50 mM 0.1161 mL 0.5805 mL 1.1610 mL 2.9024 mL
60 mM 0.0967 mL 0.4837 mL 0.9675 mL 2.4187 mL
80 mM 0.0726 mL 0.3628 mL 0.7256 mL 1.8140 mL
100 mM 0.0580 mL 0.2902 mL 0.5805 mL 1.4512 mL
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產(chǎn)品名稱(chēng):
Decanoic acid
目錄號(hào):
HY-W015309
需求量: