| Size | Price | Stock | Qty |
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| 250mg |
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| 1g |
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| Other Sizes |
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| ln Vitro |
The effects of palmatin (0-100 μM; 42 h) include the inhibition of WNV (EC50 value: 3.6 μM) and the reduction of DENV-2 and YFV (EC50 values: 26.4 μM and 7.3 μM, respectively) viral titers [3]. The proliferation of colon cancer cells is inhibited by palmatin (0-1128 μM; 24-72 hours) [5]. Through pathways related to the mitochondria, palmatin (0-704 μM; 24 hours) can cause AURKA protein levels to drop, G2/M phase arrest, and apoptosis in colon cancer cells [5].
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| ln Vivo |
DSS (dextran sulfate sodium)-induced colitis is improved and inflammatory cell infiltration is prevented when palmatine (50 or 100 mg/kg; oral; taken daily for 7 days) is taken [1]. D-galactosamine/lipopolysaccharide-induced fulminant liver failure in mice can be reduced by palmatin (0-200 mg/kg; intraperitoneal injection; once) [2]. Memory-enhancing effects of palmatine (0–1 mg/kg; i.p.; 10 days) have been shown in mice [4]. Mice HCT-116 xenograft development is successfully inhibited by palmatine (33.75–135 mg/kg; oral; once daily for 26 days) [5].
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| 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. |
| Molecular Formula |
C21H22NO4
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|---|---|
| Molecular Weight |
352.4037
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| Exact Mass |
352.15
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| Elemental Analysis |
C, 71.57; H, 6.29; N, 3.97; O, 18.16
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| CAS # |
3486-67-7
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| Related CAS # |
Palmatine chloride; 10605-02-4; Palmatine hydroxide; 131-04-4; 4880-79-9 (iodide)
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| Appearance |
Solid powder
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| SMILES |
COC1=C(C2=C[N+]3=C(C=C2C=C1)C4=CC(=C(C=C4CC3)OC)OC)OC
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| InChi Key |
QUCQEUCGKKTEBI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H22NO4/c1-23-18-6-5-13-9-17-15-11-20(25-3)19(24-2)10-14(15)7-8-22(17)12-16(13)21(18)26-4/h5-6,9-12H,7-8H2,1-4H3/q+1
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| Chemical Name |
2,3,9,10-tetramethoxy-5,6-dihydroisoquinolino[2,1-b]isoquinolin-7-ium
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| Synonyms |
BRN-1555498; BRN1555498; BRN 1555498; Palmatine Free Base; Berbericinine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8377 mL | 14.1884 mL | 28.3768 mL | |
| 5 mM | 0.5675 mL | 2.8377 mL | 5.6754 mL | |
| 10 mM | 0.2838 mL | 1.4188 mL | 2.8377 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.
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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