Autophagy Apoptosis PI3K/Akt/mTOR Epigenetics Stem Cell/Wnt JAK/STAT Signaling Immunology/Inflammation TGF-beta/Smad MAPK/ERK Pathway NF-κB Metabolic Enzyme/Protease
Autophagy Apoptosis AMPK mTOR STAT Interleukin Related PKC p38 MAPK NF-κB COX Reactive Oxygen Species (ROS) PI3K Akt MMP
Phellodendrine chloride

Cat. No.: HY-N0735

Phellodendrine chloride

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

Phellodendrine chloride is an orally active plant alkaloid. Phellodendrine chloride inhibits the proliferation of KRAS-mutated pancreatic cancer cells by suppressing macropinocytosis and glutamine metabolism, inducing ROS accumulation and mitochondrial apoptosis. Phellodendrine chloride promotes autophagy by activating the AMPK/mTOR pathway, alleviating intestinal damage in ulcerative colitis. Phellodendrine chloride can alleviate gouty arthritis by inhibiting the IL-6/STAT3 signaling pathway. Phellodendrine chloride suppresses allergic reactions by altering the conformation of MRGPRB3/MRGPRX2 protein, thereby inhibiting the activation of PKC and subsequent downstream MAPK and NF-κB signaling. Phellodendrine chloride inhibits the AKT/NF-κB pathway and down-regulates the expression of COX-2, thereby protecting zebrafish embryos from oxidative stress. Phellodendrine chloride has an anti-major depressive disorder (MDD) effect by down-regulating CHRM1, HTR1A, and the PI3K/Akt signaling pathway.

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Pureté: 99.68%
CAS No.: 104112-82-5
Formule: C₂₀H₂₄ClNO₄
Masse moléculaire:377.86

Stockage:

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

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

Phellodendrine chloride Chemical Structure

CAS No.: 104112-82-5

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[3]^[4]^[7]

IL-6

STAT3

MMP-3

IL-1β

IL-4

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In Vitro

Phellodendrine chloride (0.6-80 μM, 24 h-14 d) significantly inhibits the proliferation and colony formation ability of KRAS-mutated PANC-1 and MiaPaCa-2 cells and its driven macropinocytosis, while showing no obvious toxicity to KRAS wild-type BxPC-3 cells and normal pancreatic cells HPDE6-c7^[1].
Phellodendrine (10-40 μM, 12-24 h) diminishes the albumin (Alb) driven intracellular glutamine level, induces reactive oxygen species generation and causes mitochondrial membrane potential (MMP) depolarization in PANC-1 cells^[1].
Phellodendrine chloride (5-40 μM, 0-48 h) induces apoptosis cell death in PANC-1 cells through caspase-dependent mitochondrial intrinsic pathway^[1].
Phellodendrine (5-20 μM) chloride activates the p-AMPK/mTOR signalling pathway, as well as autophagy in Caco-2 cells stimulated by H₂O₂^[2].
Phellodendrine chloride (5 μM) attenuates Monosodium urate (MSU) (HY-B2130A)-induced MMP3 production and proteoglycan degradation by inhibiting IL-6/STAT3 pathway in rabbit primary chondrocytes and C28/I2 cells (human normal chondrocytes)^[3].
Phellodendrine (0-50 μM) chloride reduces the mRNA expression of MRGPRB3 and responsiveness of MRGPRX2 by altering its structure, is able to decrease Ca²⁺ levels, phosphorylation levels of CaMK, PLCβ1, PKC, ERK, JNK, p38, and p65, and inhibits the degradation of IκB-α in RBL-2H3 cells^[4].
Phellodendrine (25-200 μg/mL, 37 h) chloride increases the survival rate of zebrafish embryos and restores the abnormal heart rate levels^[5].
Phellodendrine (50-200 μg/mL, 13 h) chloride reduces the ROS level in zebrafish embryos and inhibits lipid peroxidation^[5].
Phellodendrine (100 μg/mL) chloride reverses the expression of AKT and NF-κB3, IKK, COX-2 which were abnormally changed by AAPH (HY-Y0525)-induced oxidative stress in zebrafish embryos^[5].
Phellodendrine (2.5-160 μg/mL, 24-48 h) chloride has an anti-MDD effect by regulating the mRNA levels of CHRM1, HTR1A and key targets of the PI3K/Akt signalling pathway (PI3K, Akt, mTOR) in PC12 cells^[6].

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

Apoptosis Analysis^[1]

Cell Line:

PANC-1 cells
Concentration:

10, 20 and 40 μM
Incubation Time:

48 h
Result:

Showed a higher apoptosis cells ratio both in early and late apoptosis.
Revealed a marked increase in the number of cells showing nuclear condensation and fragmentation.

Western Blot Analysis^[1]

Cell Line:

PANC-1 cells
Concentration:

5, 10 and 20 μM
Incubation Time:

0, 6, 12, 24 h
Result:

Induced the expressions of apoptotic proteins (cleaved caspase-3, 7, 9, PARP and Bax) and reduced the levels of Bcl-2 in time and dose dependent manner.

Cell Viability Assay^[7]

Cell Line:

PC12 cells
Concentration:

2.5, 5, 10, 20, 40, 80, 160 μg/mL
Incubation Time:

24 and 48 h
Result:

Reduced cells’ viability at all concentrations for 48 h.

Western Blot Analysis^[7]

Cell Line:

PC12 cells
Concentration:

5, 10, 20, 40, 80, 160 μg/mL
Incubation Time:

24 h
Result:

Decreased the IL-6 and IL-1β production.

RT-PCR^[7]

Cell Line:

PC12 cells
Concentration:

5, 10, 20 μg/mL
Incubation Time:

24 and 48 h
Result:

Inhibited mRNA levels of CHRM1, HTR1A, PI3K and AKT.
Had no significant effect on the expression of mTOR.

In Vivo

Phellodendrine chloride (30-60 mg/kg, i.p., once daily for 2 weeks) inhibits macropinocytosis in mice and effectively reduces the growth of PANC-1 xenograft tumors^[1].
Phellodendrine (30 mg/kg, p.o., once daily for 7 days) chloride reduces the intestinal damage of ulcerative colitis (UC) in mice^[2].
Phellodendrine chloride(40 mg/kg, i.p., mice single dose or rats once daily for 5 days) alleviated Uric acid sodium (MSU) (HY-B2130A)-induced acute peritonitis in mice and arthritis in rats^[3].
Phellodendrine (0.3-3 mg/kg, i.v.) chloride protects against C48/80 (HY-130592)-induced foot swelling and Evans blue exudation in mice, and suppresses C48/80-induced RBL-2H3 rat basophilic leukemia cells degranulation, and β-HEX, HIS, IL-4, and TNF-α release^[4].

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

Animal Model:

PANC-1 xenograft model established in Balb/c nude mice (male, 7 weeks old)^[1]
Dosage:

30 and 60 mg/kg
Administration:

Intraperitoneal injection (i.p.), once daily for 2 weeks
Result:

Resulted in lower tumor weights and volumes.
Inhibited macropinocytosis in tumor tissues.
Reduced the proliferation activity of tumor cells.

Animal Model:

DSS (HY-116282C) induced UC model established in female C57BL/6 mice (18-22 g)^[2]
Dosage:

30 mg/kg
Administration:

Oral administration (p.o.), once daily for 7 days
Result:

Significantly restored the length of the colon.
Significantly reduced the disease activity index (DAI) score and the pathological damage score.

Animal Model:

MSU crystal-induced arthritis model established in male Sprague-Dawley (SD) rats with a mass of 240-270 g^[3]
Dosage:

40 mg/kg
Administration:

Intraperitoneal injection (i.p.), once daily for 5 days
Result:

Significantly reduced the degree of joint swelling in rats.
Reduced the inflammatory score and restored the loss of proteoglycans.
Significantly inhibited the expression of MMP-3.

Animal Model:

MSU induced peritonitis model established in male C57BL/6 mice (18-20 g)^[3]
Dosage:

40 mg/kg
Administration:

Intraperitoneal injection (i.p.), single dose
Result:

Reduced proportion of neutrophils in the peritoneal lavage fluid.

Animal Model:

C48/80-induced Hind paw swelling model established in adult male mice^[4]
Dosage:

0.3 and 3 mg/kg
Administration:

Intravenously injection (i.v.)
Result:

Was associated with reductions in both foot swelling and the degree of Evans blue exudation in mice.
suppressed C48/80-induced RBL-2H3 rat basophilic leukemia cells degranulation, and β-HEX, HIS, IL-4, and TNF-α release.

Chemical Information

CAS No. 104112-82-5
Appearance Solid
Masse moléculaire 377.86
Formule C₂₀H₂₄ClNO₄
Color White to off-white
SMILES

C[N@@+]12CCC3=CC(OC)=C(O)C=C3[C@]1([H])CC4=CC(O)=C(OC)C=C4C2.[Cl-]
Structure Classification
- Alkaloids
- Isoquinoline Alkaloids
- Phenols
- Polyphenols
Initial Source
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

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

Publications (2)

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Int Immunopharmacol

Phellodendrine alleviates acute pancreatitis by inhibiting p38 MAPK-p47phox pathway-mediated neutrophil extracellular traps formation and ROS production. [Abstract]

2025 Oct 9:167:115658. PMID: 41072078
Int Immunopharmacol

Phellodendrine ameliorates intestinal inflammation and protects mucosal barrier via modulating COL1A1, VCAM1 and IL-17 a. [Abstract]

2025 Apr 16:152:114403. PMID: 40101527

Solvant et solubilité

In Vitro:

DMSO : 50 mg/mL (132.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6465 mL

13.2324 mL

26.4648 mL

5 mM

0.5293 mL

2.6465 mL

5.2930 mL

10 mM

0.2646 mL

1.3232 mL

2.6465 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 5 mg/mL (13.23 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (13.23 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (13.23 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (292 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
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MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Thu PM, et al. Phellodendrine chloride suppresses proliferation of KRAS mutated pancreatic cancer cells through inhibition of nutrients uptake via macropinocytosis. Eur J Pharmacol. 2019 May 5;850:23-34. [Content Brief]

[2]. Su S, Wang X, Xi X, et al. Phellodendrine promotes autophagy by regulating the AMPK/mTOR pathway and treats ulcerative colitis. J Cell Mol Med. 2021;25(12):5707-5720. [Content Brief]

[3]. Qin YY, et al. Phellodendrine chloride alleviates gouty arthritis through IL-6/STAT3 signaling pathway. Immunobiology. 2025 Jul;230(4):152918. [Content Brief]

[4]. Wang J, et al. Inhibitory effect of phellodendrine on C48/80-induced allergic reaction in vitro and in vivo. Int Immunopharmacol. 2024 Jun 15;134:112256. [Content Brief]

[5]. Li L, et al. The defensive effect of phellodendrine against AAPH-induced oxidative stress through regulating the AKT/NF-κB pathway in zebrafish embryos. Life Sci. 2016 Jul 15;157:97-106. [Content Brief]

[6]. Hu L, et al. Network pharmacology combined with experimental verification for exploring the potential mechanism of phellodendrine against depression. Sci Rep. 2025 Jan 14;15(1):1958. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6465 mL	13.2324 mL	26.4648 mL	66.1621 mL
	5 mM	0.5293 mL	2.6465 mL	5.2930 mL	13.2324 mL
	10 mM	0.2646 mL	1.3232 mL	2.6465 mL	6.6162 mL
	15 mM	0.1764 mL	0.8822 mL	1.7643 mL	4.4108 mL
	20 mM	0.1323 mL	0.6616 mL	1.3232 mL	3.3081 mL
	25 mM	0.1059 mL	0.5293 mL	1.0586 mL	2.6465 mL
	30 mM	0.0882 mL	0.4411 mL	0.8822 mL	2.2054 mL
	40 mM	0.0662 mL	0.3308 mL	0.6616 mL	1.6541 mL
	50 mM	0.0529 mL	0.2646 mL	0.5293 mL	1.3232 mL
	60 mM	0.0441 mL	0.2205 mL	0.4411 mL	1.1027 mL
	80 mM	0.0331 mL	0.1654 mL	0.3308 mL	0.8270 mL
	100 mM	0.0265 mL	0.1323 mL	0.2646 mL	0.6616 mL

Phellodendrine chloride

2 Cited Publications

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Phellodendrine chloride

Apoptosis Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

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