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Palmatine chloride

Cat No.:V27077 Purity: ≥98%
Palmatine chloride is an orally bioactive, irreversible IDO-1 inhibitor (antagonist) with IC50s of 3 μM and 157 μM for HEK 293-hIDO-1 and rhIDO-1, respectively.
Palmatine chloride
Palmatine chloride Chemical Structure CAS No.: 10605-02-4
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
250mg
1g
Other Sizes

Other Forms of Palmatine chloride:

  • Palmatine hydroxide
  • Palmatine
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
Palmatine chloride is an orally bioactive, irreversible IDO-1 inhibitor (antagonist) with IC50s of 3 μM and 157 μM for HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine chloride also noncompetitively inhibits West Nile virus (WNV) NS2B-NS3 protease with IC50 of 96 μM. Palmatine chloride has anticancer, anti~inflammatory, neuro-protective (neuro-protection), antibacterial, and anti-viral effects.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
Palmatin (0-100 μM; 42 h) diminishes the viral titers of DENV-2 and YFV with EC50 values of 26.4 μM and 7.3 μM, respectively, and suppresses WNV with an EC50 value of 3.6 μM [3]. The growth of colon cancer cells is inhibited by palmatin (0-1128 μM; 24-72 hours) [5]. By means of mitochondria-related pathways, palmatin (0-704 μM; 24 hours) can cause AURKA protein levels to drop, G2/M phase arrest, and death in colon cancer cells [5].
ln Vivo
Oral palmatine (50 or 100 mg/kg; given once daily for 7 days) reduces the infiltration of inflammatory cells and ameliorates colitis caused by dextran sulfate sodium (DSS) [1]. ?In mice, fulminant liver failure produced by lipopolysaccharide and D-galactosamine can be lessened by intraperitoneal injection of palmatin (0-200 mg/kg) once [2]. ?In mice, palmatine (0–1 mg/kg; i.p.; 10 days) has memory-improving effects [4]. ?The growth of HCT-116 xenografts in mice is successfully inhibited by palmatine (33.75–135 mg/kg; oral; once daily for 26 days) [5].
Cell Assay
Cell proliferation assay[5]
Cell Types: HCT-116, SW480, HT-29
Tested Concentrations: 0, 88, 176, 352 and 704 μM (HCT-116, SW480); 0, 141, 282, 564 and 1128 μM (HT -29)
Incubation Duration: 24, 48 and 72 hrs (hours)
Experimental Results: Cell viability diminished in a dose-dependent manner.

Western Blot Analysis [5]
Cell Types: HCT-116, SW480, HT-29
Tested Concentrations: 100 nM for HCT-116, 500 nM for SW480 and HT-29
Incubation Duration: 24 hrs (hours)
Experimental Results: Promote the expression of apoptosis markers, For example, P53/P73, Caspase3 and Caspase9. AURKA protein levels are diminished. Cytochrome increases. c In the cytoplasm, both Bcl2 and Bcl-xl were diminished in a dose-dependent manner.

Cell cycle analysis[5]
Cell Types: HCT-116, SW480
Tested Concentrations: 88, 176, 352 and 704 μM
Incubation Duration: 24 hrs (hours)
Experimental Results: Induced G2/M phase arrest in a dose-dependent manner.

Apoptosis analysis [5]
Cell Types: HCT-116, SW480
Tested Concentrations: 88, 176, 352 and 704 μM
Incubation Duration: 24 h
Experimental Results: Apoptosis was induced in a dose-dependent manner.
Animal Protocol
Animal/Disease Models: DSS-induced colitis BALB/c mouse model (8 weeks old) [1]
Doses: 50 or 100 mg/kg
Route of Administration: Orally, daily, for 7 days
Experimental Results: Improved DSS-induced colitis It also prevents the infiltration of inflammatory cells in colitis; Dramatically extends the length of the colon; and Dramatically inhibits colonic MPO activity. Reduce the levels of colon inflammatory cytokines (TNF-α, IFN-γ, IL-1β, IL-6, IL-4 and IL-10); protect mucosal integrity by regulating TJs proteins and apoptotic proteins; restore DSS-induced Reduction of TJ proteins ZO-1, ZO-2 and Claudin-1; 100 mg/kg dose diminished Bax expression and enhanced Bcl-2 expression, preventing epithelial cell apoptosis and improving intestinal integrity. Preventing changes in intestinal microbiota in mice with DSS-induced colitis.

Animal/Disease Models: Male ICR mouse (20-22 g), D-galactosamine/lipopolysaccharide (GalN/LPS)-induced fulminant liver failure model [2]
Doses: 25, 50, 100 or 200 mg/kg given Medication: intraperitonealinj
References
[1]. Zhang XJ, et al. Palmatine ameliorated murine colitis by suppressing tryptophan metabolism and regulating gut microbiota.Pharmacol Res. 2018 Nov;137:34-46.
[2]. Lee WC, et al. Palmatine attenuates D-galactosamine/lipopolysaccharide-induced fulminant hepatic failure in mice. Food Chem Toxicol. 2010 Jan;48(1):222-8.
[3]. Jia F, et al. Identification of palmatine as an inhibitor of West Nile virus. Arch Virol. 2010 Aug;155(8):1325-9.
[4]. Dhingra D, et al. Memory-enhancing activity of palmatine in mice using elevated plus maze and morris water maze. Adv Pharmacol Sci. 2012;2012:357368.
[5]. Liu X, et al. Palmatine induces G2/M phase arrest and mitochondrial-associated pathway apoptosis in colon cancer cells by targeting AURKA. Biochem Pharmacol. 2020 May;175:113933.
[6]. Long J, et al. Palmatine: A review of its pharmacology, toxicity and pharmacokinetics. Biochimie. 2019 Jul;162:176-184.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H22CLNO4
Molecular Weight
387.86
CAS #
10605-02-4
Related CAS #
Palmatine hydroxide;131-04-4;Palmatine;3486-67-7
Appearance
Typically exists as solids (or liquids in special cases) at room temperature
SMILES
[Cl-].O(C([H])([H])[H])C1=C(C([H])=C2C(=C1[H])C([H])([H])C([H])([H])[N+]1C([H])=C3C(=C(C([H])=C([H])C3=C([H])C=12)OC([H])([H])[H])OC([H])([H])[H])OC([H])([H])[H]
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ≥ 32 mg/mL (~82.50 mM)
H2O : ~5 mg/mL (~12.89 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.45 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (6.45 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: 2.5 mg/mL (6.45 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C).


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.5782 mL 12.8912 mL 25.7825 mL
5 mM 0.5157 mL 2.5782 mL 5.1565 mL
10 mM 0.2578 mL 1.2891 mL 2.5782 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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