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Structure of Nitidine chloride
CAS No.: 13063-04-2
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Nitidine Chloride can inhibit proliferation and induce apoptosis via the Akt pathway, derived from genus Zanthoxylum.
Synonyms: Nitidine (chloride); NSC 146397
4.5
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CAS No. : | 13063-04-2 |
Formula : | C21H18ClNO4 |
M.W : | 383.82 |
SMILES Code : | C[N+]1=CC2=CC(OC)=C(OC)C=C2C(C=CC3=C4)=C1C3=CC5=C4OCO5.[Cl-] |
Synonyms : |
Nitidine (chloride); NSC 146397
|
MDL No. : | MFCD01659688 |
InChI Key : | QLDAACVSUMUMOR-UHFFFAOYSA-M |
Pubchem ID : | 25659 |
GHS Pictogram: |
![]() |
Signal Word: | Danger |
Hazard Statements: | H300 |
Precautionary Statements: | P264-P270-P301+P310-P321-P330-P405-P501 |
Class: | 6.1 |
UN#: | 2811 |
Packing Group: | Ⅱ |
In Vitro:
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. |
In Vivo:
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. | Chin Med. 2022 Sep 29;17(1):115. |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.61mL 0.52mL 0.26mL |
13.03mL 2.61mL 1.30mL |
26.05mL 5.21mL 2.61mL |
Tags: Nitidine | Parasite | Apoptosis | STAT | Topoisomerase | ERK | FAK | p38 MAPK | NF-κB | Extracellular signal regulated kinases | PTK2 protein tyrosine kinase 2 | Zanthoxylum nitidum DC | Nitidine chloride | anticancer | anti-malarial | apoptosis | STAT3 inhibition | MAPK | NF-kB | DNA topoisomerase | ERK | c-Src/FAK | Focal adhesion kinase | Nuclear factor-κB | Nuclear factor-kappaB | 13063-04-2
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