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Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
Nitidine chloride (NC), a quaternary ammonium alkaloid, exhibits multiple biological activities, including antimalarial, antifungal, and antiangiogenesis. NC has been identified to suppress cell proliferation, stimulate apoptosis, and induce cell cycle arrest, retard migration, invasion and metastasis[3]. NC caused time- and concentration-dependent inhibition of CYP2D6, and more than 50% of CYP2D6 activity was suppressed after a 15-minute incubation with NC at 100 μM in the primary incubation mixtures, with KI of 4.36 μM, kinact of 0.052 minute-1, and a partition ratio of approximately 290[4]. NC led to the inhibition of cell growth, migration, and invasion and the induction of apoptosis, also inhibited the expression of SIN1 in osteosarcoma cells[5]. Nitidine chloride inhibited HaCaT proliferation and induced S phase cell cycle arrest. Nitidine chloride also significantly downregulated bcl-2 and upregulated bax, cleaved caspase-9 and cleaved caspase-3. In 12-O-tetradecanoyl-phorbol-13-acetate (TPA)- and imiquimod (IMQ)-induced epidermal hyperplasia and inflammation models, nitidine chloride inhibited topical edema in mouse ear and back skin, substantially reducing tissue thickness and weight[6].
Nitidine chloride/氯化两面针碱 细胞实验
Cell Line
Concentration
Treated Time
Description
References
MDCK-hOCT2/hMATE1 cells
2.5 µM
120 minutes
To evaluate the transcellular transport and intracellular accumulation of nitidine chloride in MDCK-hOCT2/hMATE1 cells, results showed that MATE1 plays a minor role in the transcellular transport of nitidine chloride
Br J Pharmacol. 2016 Aug;173(16):2543-54.
MDCK-hOCT2 cells
0.1 –4.0 µM
2 minutes
To evaluate the uptake kinetics of nitidine chloride in MDCK-hOCT2 cells, results showed that nitidine chloride is a high-affinity substrate of hOCT2 with a Km of 0.97 ± 0.10 μM and Vmax of 288.1 ± 12.8 pmol·mg-1·protein·min-1
Br J Pharmacol. 2016 Aug;173(16):2543-54.
Rat primary-cultured proximal tubular (rPCPT) cells
0.1 –50 µM
24 hours
To evaluate the cytotoxicity of nitidine chloride in rat primary-cultured proximal tubular cells and the effect of OCT2 inhibitors, results showed that nitidine chloride concentration-dependently decreased cell viability, and OCT2 inhibitors significantly attenuated its toxicity
Br J Pharmacol. 2016 Aug;173(16):2543-54.
RAW 264.7 cells
1 µM, 10 µM
24 hours
To evaluate the effect of NitC on LPS-induced inflammatory response. Results showed that NitC significantly inhibited the expression of iNOS, COX2, IL-1β, and NLRP3, indicating its ability to suppress NLRP3 inflammasome activation.
Front Pharmacol. 2022 Jul 22;13:919940.
Cardiac fibroblasts (CFs)
1.25, 2.5, 5, 10, 20, 40 µM
24 or 48 hours
To evaluate the effect of NC on cardiac fibroblasts, it was found that low concentrations of NC (1.25, 2.5, 5 μM) increased cell viability, while high concentrations (20, 40 μM) decreased cell viability
Acta Pharmacol Sin. 2023 Mar;44(3):561-572.
Li-7 hepatocellular carcinoma cells
10, 20, 40, 80 μg/mL
24, 48, 72 hours
Evaluate the cytotoxic effect of TPGS-FA/NC on Li-7 cells, results showed TPGS-FA/NC had better cytotoxicity than 5-Fu and NC
BMC Chem. 2022 Oct 9;16(1):75.
HUVECs
10 µM
36 hours
Nitidine chloride showed no significant effect on HUVECs
Mol Pharm. 2014 Jul 7;11(7):2022-9.
A549 cells
10 µM
36 hours
Nitidine chloride significantly inhibited the dispersion of A549 cancer cells, almost completely abolishing the spheroids' dispersion
Mol Pharm. 2014 Jul 7;11(7):2022-9.
HeLa
1-10 µM
48 hours
Inhibition of cancer cell proliferation
Cell Death Discov. 2025 Mar 22;11(1):116.
HCT116
1-10 µM
48 hours
Inhibition of cancer cell proliferation
Cell Death Discov. 2025 Mar 22;11(1):116.
A549
0.5 µM
48 hours
NC induced cell swelling and large bubbles emerging from the plasma membrane, showing typical pyroptotic features.
Chin Med. 2022 Sep 29;17(1):115.
NCI-H1688
0.5 µM
48 hours
NC induced cell swelling and large bubbles emerging from the plasma membrane, showing typical pyroptotic features.
Chin Med. 2022 Sep 29;17(1):115.
MCF-7 cells
1 or 2.5 µM
48 hours
NC inhibited the proliferation of MCF-7 cells in a dose-dependent manner and suppressed their migratory and invasive capabilities
Cell Biosci. 2016 Jun 16;6:44.
MDA-MB-468 cells
1 or 2.5 µM
48 hours
NC inhibited the proliferation of MDA-MB-468 cells in a dose-dependent manner and suppressed their migratory and invasive capabilities
Cell Biosci. 2016 Jun 16;6:44.
U2OS cells
8 µM
48 hours
To evaluate the effect of NC on U2OS cell apoptosis, results showed that NC treatment obviously induced cell apoptosis.
Mol Ther Oncolytics. 2019 Feb 5;12:224-234.
U2OS cells
4 µM
72 hours
To evaluate the effect of NC on U2OS cell proliferation, results showed that NC significantly inhibited cell growth in a dose-dependent manner.
Mol Ther Oncolytics. 2019 Feb 5;12:224-234.
MG63 cells
1.5 µM
72 hours
To evaluate the effect of NC on MG63 cell proliferation, results showed that NC significantly inhibited cell growth in a dose-dependent manner.
Mol Ther Oncolytics. 2019 Feb 5;12:224-234.
Nitidine chloride/氯化两面针碱 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Sprague-Dawley rats
Osteoarthritis model induced by destabilization of the medial meniscus (DMM) surgery
Intra-articular injection
10 μM
Once a week for 6 weeks
To evaluate the effect of NitC on DMM surgery-induced osteoarthritis model. Results showed that NitC significantly alleviated cartilage erosion, ECM degradation, and subchondral alterations.
Front Pharmacol. 2022 Jul 22;13:919940.
BALB/c nude mice
Liver cancer xenograft model
Intraperitoneal injection
10, 5, 2.5 mg/kg
Once daily for 14 days
To evaluate the antitumor effect of nitidine chloride on liver cancer xenograft models, results showed that nitidine chloride significantly inhibited tumor growth
Int J Oncol. 2018 Nov;53(5):1897-1912
Sprague-Dawley rats
Chronic nephrotoxicity model
Intravenous injection
2 mg/kg and 6 mg/kg
Once daily for 21 days
To evaluate the nephrotoxicity and underlying mechanisms of nitidine chloride. Results showed accumulation of NC in the inner cortex region of the kidney, leading to renal tubule damage and metabolic disturbances.
J Pharm Anal. 2024 Jul;14(7):100944
C57BL/6 mice
Cardiac hypertrophy model
Intraperitoneal injection
2.5, 5, 10 mg/kg
Once daily for 4 weeks
To evaluate the effect of NC on cardiac function, it was found that high-dose NC caused cardiac hypertrophy and dysfunction in mice, and cardiac autophagy levels were reduced
Acta Pharmacol Sin. 2023 Mar;44(3):561-572.
Zebrafish
HCC xenograft model
Yolk sac injection
3.0 ng
Every 24 hours
To validate the inhibitory effect of NC on HCC growth, metastasis, and angiogenesis in vivo, results showed that NC significantly inhibited the growth, metastasis, and angiogenesis of HCC
Mol Med. 2025 Feb 5;31(1):47
Sprague-Dawley rats
Healthy male rats
Intravenous injection
5 mg/kg
Once daily for 20 consecutive days
To evaluate the nephrotoxicity of nitidine chloride in rats after 20 days of successive intravenous administration, results showed that nitidine chloride caused increased levels of blood urea nitrogen (BUN) and lactate dehydrogenase (LDH), reduced levels of alkaline phosphatase (ALP), and pathological changes in the kidney
Br J Pharmacol. 2016 Aug;173(16):2543-54.
BALB/c nude mice
HCC xenograft model
Intraperitoneal injection
7 mg/kg
Every other day for 15 days
Significantly reduced tumor volume
Cell Death Dis. 2019 Sep 10;10(9):658
C57 mice
High-fat diet-induced NAFLD model
Gavage
8 mg/kg
Once daily for 4 weeks
To evaluate the therapeutic effect of NC-CS/PT-NPs on high-fat diet-induced NAFLD. Results showed that NC-CS/PT-NPs significantly inhibited weight gain, decreased serum AST, ALT and lipid levels, improved liver and intestinal inflammation, and altered the diversity of gut microbiota in mice.
Int J Nanomedicine. 2024 Mar 8;19:2409-2428
BALB/c mice
H1688 or A549 xenograft model
Intraperitoneal injection
8 mg/kg/week or 16 mg/kg/week
Twice a week for 21 days
NC significantly inhibited tumor growth and induced tumor cell pyroptosis by inhibiting the PI3K/Akt pathway.
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