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  2. mAChR Indoleamine 2,3-Dioxygenase (IDO) Virus Protease Aurora Kinase Apoptosis Bacterial Parasite
  3. Palmatine chloride

Palmatine chloride  (Synonyms: 鹽酸巴馬汀)

目錄號: HY-N0110 純度: 99.81%
COA 產(chǎn)品使用指南 技術(shù)支持

Palmatine chloride 是一種具有口服活性的、不可逆的 IDO-1 抑制劑,對 HEK 293-hIDO-1 和 rhIDO-1 的 IC50 分別為 3 μM 和 157 μM。Palmatine chloride 也能非競爭性抑制西尼羅病毒 (WNV) NS2B-NS3 蛋白酶,IC50 為 96 μM。Palmatine chloride 具有抗癌、抗炎、神經(jīng)保護、抗細菌、抗病毒活性。

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Palmatine chloride Chemical Structure

Palmatine chloride Chemical Structure

CAS No. : 10605-02-4

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10 mM * 1 mL in DMSO ¥220
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250 mg ¥200
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1 g ¥500
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Customer Review

Other Forms of Palmatine chloride:

查看 mAChR 亞型特異性產(chǎn)品:

查看 Indoleamine 2,3-Dioxygenase (IDO) 亞型特異性產(chǎn)品:

查看 Aurora Kinase 亞型特異性產(chǎn)品:

查看 Parasite 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

Palmatine chloride is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC50s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine chloride can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC50 of 96 μM. Palmatine chloride shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities[1][2][3][4][5].

IC50 & Target[1]

IDO-1

3 μM (IC50, HEK 293-hIDO-1)

IDO-1

157 μM (IC50, rhIDO-1)

WNV NS2B-NS3

96 μM (IC50)

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
G-402 GI50
83.14 μM
Compound: 3
Growth inhibition against human G402 cells after 48 hrs by MTT assay
Growth inhibition against human G402 cells after 48 hrs by MTT assay
[PMID: 21401114]
HCT-116 IC50
> 100 μM
Compound: Palmatine Chloride
Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
[PMID: 28359045]
HepG2 IC50
> 100 μM
Compound: Palmatine Chloride
Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay
[PMID: 28359045]
HL-60 IC50
> 100 μM
Compound: Palmatine Chloride
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
[PMID: 28359045]
KM12C IC50
393 μM
Compound: B-11
Inhibition of cell proliferation of human KM12C cells incubated for 15 hrs by MTT assay
Inhibition of cell proliferation of human KM12C cells incubated for 15 hrs by MTT assay
[PMID: 32391701]
L02 IC50
> 100 μM
Compound: Palmatine Chloride
Cytotoxicity against human LO2 cells after 72 hrs by MTT assay
Cytotoxicity against human LO2 cells after 72 hrs by MTT assay
[PMID: 28359045]
SMMC-7721 IC50
> 100 μM
Compound: Palmatine Chloride
Cytotoxicity against human SMMC7721 cells after 72 hrs by MTT assay
Cytotoxicity against human SMMC7721 cells after 72 hrs by MTT assay
[PMID: 28359045]
體外研究
(In Vitro)

Palmatine (0-100 μM; 42 h) suppresses WNV with an EC50 value of 3.6 μM, and reduce the viral titers of DENV-2 and YFV with EC50 values of 26.4 μM and 7.3 μM, respectively[3].
? Palmatine (0-1128 μM; 24-72 h) inhibits colon cancer cell proliferation[5].
? Palmatine (0-704 μM; 24 h) reduces AURKA protein levels, induces G2/M phase arrest, and induces apoptosis in colon cancer cells via the mitochondrial associated pathway[5].

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

Cell Proliferation Assay[5]

Cell Line: HCT-116, SW480, HT-29
Concentration: 0, 88, 176, 352, and 704 μM (HCT-116, SW480); 0, 141, 282, 564, and 1128 μM (HT-29)
Incubation Time: 24, 48 and 72 h
Result: Decreased cell viability in a dose-dependent manner.

Western Blot Analysis[5]

Cell Line: HCT-116, SW480, HT-29
Concentration: 100 nM for HCT-116, 500 nM for SW480 and HT-29
Incubation Time: 24 h
Result: Promoted the expression of apoptosis markers such as P53 / P73, Caspase3, and Caspase9. Reduced AURKA protein levels. Increased cyt. c in the cytoplasm while reduced Bcl2 and Bcl-xl in a dose-dependent manner.

Cell Cycle Analysis[5]

Cell Line: HCT-116, SW480
Concentration: 88, 176, 352 and 704 μM
Incubation Time: 24 h
Result: Induced G2/M phase arrest in a dose-dependent manner.

Apoptosis Analysis[5]

Cell Line: HCT-116, SW480
Concentration: 88, 176, 352 and 704 μM
Incubation Time: 24 h
Result: Induced apoptosis in a dose-dependent manner.
體內(nèi)研究
(In Vivo)

Palmatine (50 or 100 mg/kg; p.o.; daily for 7 days) ameliorates DSS (dextran sulfate sodium)-induced colitis and prevents infiltration of inflammatory cells[1].
? Palmatine (0-200 mg/kg; i.p.; once) attenuates D-galactosamine/Lipopolysaccharides (HY-D1056)-induced fulminant hepatic failure in mice[2].
? Palmatine (0-1 mg/kg; i.p.; 10 days) shows memory-enhancing activity in mice[4].
? Palmatine (33.75-135 mg/kg; p.o.; daily for 26 days) can effectively inhibit the growth of HCT-116 xenografts in mice[5].

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

Animal Model: DSS- induced Colitis BALB/c mice model (8-week-old)[1]
Dosage: 50 or 100 mg/kg
Administration: Orally, daily, for 7 days
Result: Ameliorated DSS-induced colitis and prevented infiltration of inflammatory cells; remarkably extended the colon length; significantly suppressed the colonic MPO activity. Decreased the levels of colonic inflammatory cytokines (TNF-α, IFN-γ, IL-1β, IL-6, IL-4 and IL-10); Protected mucosal integrity by modulating TJs protein and apoptosis proteins; Restored DSS-induced decreases of TJ protein ZO-1, ZO-2 and claudin-1; Reduced Bax expression and enhanced Bcl-2 expression at the dose of 100?mg/kg, prevented epithelial apoptosis and improved intestinal integrity. Prevented DSS-induced changes of gut microbiota in colitis mice.
Animal Model: Male ICR mice (20–22 g), D-galactosamine/lipopolysaccharide (GalN/LPS)-induced fulminant hepatic failure model[2]
Dosage: 25, 50, 100, or 200 mg/kg
Administration: Intraperitoneal injection, 1 h before the GalN/LPS treatment
Result: Attenuated the mortality and serum aminotransferase activities increased by GalN/LPS. Prevented the increase of serum TNF-α and augmented that of serum IL-10. Decreased the TNF-a mRNA expression and increased the IL-10 mRNA expression. Attenuated the apoptosis of hepatocytes.
Animal Model: Swiss young male albino mice, with Scopolamine (HY-N0296)- and diazepam-induced amnesia model[4]
Dosage: 0.1, 0.5, 1 mg/kg
Administration: Intraperitoneal injection, 10 days
Result: Significantly improved learning and memory of mice at 0.5 and 1 mg/kg and did not show any significant effect on locomotor activity of the mice. Significantly reversed scopolamine- and diazepam-induced amnesia in mice. Significantly reduced brain acetylcholinesterase activity of mice.
Animal Model: BALB/c-nude mice, HCT-116 xenograft model[5]
Dosage: 33.75, 67.5 and 135 mg/kg
Administration: Oral administration, once a day for 26 days
Result: The tumor volume and weight of the treatment group were significantly reduced.
分子量

387.86

Formula

C21H22ClNO4

CAS 號
性狀

固體

顏色

Light yellow to yellow

中文名稱

鹽酸巴馬汀;鹽酸巴馬亭;鹽酸掌葉防己堿;氯化巴馬亭;棕櫚堿

結(jié)構(gòu)分類
初始來源
運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light)

溶解性數(shù)據(jù)
細胞實驗: 

DMSO 中的溶解度 : ≥ 32 mg/mL (82.50 mM; 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)

H2O 中的溶解度 : 5 mg/mL (12.89 mM; 超聲助溶)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.5782 mL 12.8912 mL 25.7825 mL
5 mM 0.5156 mL 2.5782 mL 5.1565 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(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light)。-80°C儲存時,請在1年內(nèi)使用, -20°C儲存時,請在6個月內(nèi)使用。

* 備注:如您選擇水作為儲備液,請稀釋至工作液后,再用 0.22 μm 的濾膜過濾除菌后使用。

  • 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

動物實驗:

請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實驗結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當(dāng)保存;體內(nèi)實驗的工作液,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;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.45 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。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 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

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

    Solubility: ≥ 2.5 mg/mL (6.45 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。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 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。

以下溶解方案,請直接配制工作液。建議現(xiàn)用現(xiàn)配,在短期內(nèi)盡快用完。 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; 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶。

  • 方案 一

    請依序添加每種溶劑: PBS

    Solubility: 2.5 mg/mL (6.45 mM); 澄清溶液; 超聲助溶 (<60°C)

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

由于實驗過程有損耗,建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動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 2%。
方案所需 助溶劑 包括:DMSO ,均可在 MCE 網(wǎng)站選購。 ,Tween 80,均可在 MCE 網(wǎng)站選購。
計算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。

*In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light)

您所需的儲備液濃度超過該產(chǎn)品的實測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術(shù)支持聯(lián)系。
動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液,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)給藥周期超過半月以上,請謹慎選擇該方案。
請確保第一步儲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: 99.81%

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(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture and light)。-80°C儲存時,請在1年內(nèi)使用, -20°C儲存時,請在6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
H2O / DMSO 1 mM 2.5782 mL 12.8912 mL 25.7825 mL 64.4562 mL
5 mM 0.5156 mL 2.5782 mL 5.1565 mL 12.8912 mL
10 mM 0.2578 mL 1.2891 mL 2.5782 mL 6.4456 mL
DMSO 15 mM 0.1719 mL 0.8594 mL 1.7188 mL 4.2971 mL
20 mM 0.1289 mL 0.6446 mL 1.2891 mL 3.2228 mL
25 mM 0.1031 mL 0.5156 mL 1.0313 mL 2.5782 mL
30 mM 0.0859 mL 0.4297 mL 0.8594 mL 2.1485 mL
40 mM 0.0645 mL 0.3223 mL 0.6446 mL 1.6114 mL
50 mM 0.0516 mL 0.2578 mL 0.5156 mL 1.2891 mL
60 mM 0.0430 mL 0.2149 mL 0.4297 mL 1.0743 mL
80 mM 0.0322 mL 0.1611 mL 0.3223 mL 0.8057 mL

* 備注:如您選擇水作為儲備液,請稀釋至工作液后,再用 0.22 μm 的濾膜過濾除菌后使用。

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產(chǎn)品名稱:
Palmatine chloride
目錄號:
HY-N0110
需求量: