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  2. GPCR/G Protein Neuronal Signaling Metabolic Enzyme/Protease Anti-infection Epigenetics Cell Cycle/DNA Damage Apoptosis
  3. mAChR Indoleamine 2,3-Dioxygenase (IDO) Virus Protease Aurora Kinase Apoptosis Bacterial Parasite
  4. Palmatine

Palmatine  (Synonyms: 巴馬??；黃藤素)

目錄號: HY-N0110A
產(chǎn)品使用指南 技術支持

Palmatine 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 也能非競爭性抑制西尼羅病毒 (WNV) NS2B-NS3 蛋白酶，IC50 為 96 μM。Palmatine 具有抗癌、抗炎、神經(jīng)保護、抗細菌、抗病毒活性。

在相同的摩爾濃度下，化合物鹽形式與游離形式有相同的生物活性，但鹽形式 Palmatine hydroxide 通常具有更好的水溶性和穩(wěn)定性。

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Palmatine Chemical Structure

Palmatine Chemical Structure

CAS No. : 3486-67-7

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Palmatine 的其他形式現(xiàn)貨產(chǎn)品:

Customer Review

Other Forms of Palmatine:

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 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 can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC50 of 96 μM. Palmatine 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)

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

352.40

Formula

C21H22NO4+
CAS 號
性狀

固體

顏色

Light yellow to yellow

中文名稱

巴馬汀；黃藤素
結構分類
初始來源
運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

純度 & 產(chǎn)品資料
參考文獻

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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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Palmatine
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HY-N0110A
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