Structure of Stachydrine HCl
CAS No.: 4136-37-2
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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.
Stachydrine HCl is a naturally occuring anti-metastatic agent in vitro which is isolated from seed husk and the pulp of the fruit of C. Leonurus.
Synonyms: Stachydrine hydrochloride
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| CAS No. : | 4136-37-2 |
| Formula : | C7H14ClNO2 |
| M.W : | 179.64 |
| SMILES Code : | C[N+]1(C)[C@H](C(O)=O)CCC1.[Cl-] |
| Synonyms : |
Stachydrine hydrochloride
|
| MDL No. : | MFCD21609192 |
| InChI Key : | DUNMULOWUUIQIL-RGMNGODLSA-N |
| Pubchem ID : | 44150282 |
| GHS Pictogram: |
|
| Signal Word: | Warning |
| Hazard Statements: | H315-H319-H335 |
| Precautionary Statements: | P261-P305+P351+P338 |
In Vitro:
|
Cell Line
|
Concentration | Treated Time | Description | References |
| Adult mouse cardiac myocytes (AMCMs) | 10 µM | 1 hour | STA decreased Ca2+ content, enhanced contractility, inhibited Ca2+ overload, and strengthened sarcomere contractility in cardiomyocytes under oxidative stress. | Int J Mol Sci. 2023 Sep 21;24(18):14369 |
| Bovine aorta endothelial cells (BAECs) | 10 µM | 12 hours | To evaluate the effect of STA on Hcy-induced reduction in NO production, results showed that STA pretreatment effectively attenuated the detrimental effect of Hcy on NO production. | Mol Med. 2018 Mar 19;24(1):10 |
| Bovine aorta endothelial cells (BAECs) | 0-10 µM | 24 hours | To evaluate the effect of STA on cell viability, results showed that STA had no significant effect on BAECs viability at concentrations of 0-20μM. | Mol Med. 2018 Mar 19;24(1):10 |
| HUVEC cells | 10 µM | 24 hours | To evaluate the inhibitory effect of Stachydrine on M2-TAMs-induced migration, invasion, and tube formation of HUVEC cells. Results showed that Stachydrine significantly inhibited M2-TAMs-induced migration, invasion, and tube formation of HUVEC cells. | Front Pharmacol. 2025 Feb 5;16:1514158 |
| THP-1 cells | 10 µM | 24 hours | To evaluate the inhibitory effect of Stachydrine on M2-TAMs-induced migration and invasion of CRC cells. Results showed that Stachydrine significantly inhibited M2-TAMs-induced migration and invasion of CRC cells. | Front Pharmacol. 2025 Feb 5;16:1514158 |
| Rat H9c2 cardiomyocytes | 10 µM | 24 hours | STA decreased the expression of phosphorylated CaMKII (T286), oxidized CaMKII, and phosphorylated RyR2 (S2814) proteins. | Int J Mol Sci. 2023 Sep 21;24(18):14369 |
| HK-2 cells | 20 or 40 µM | 36 hours | To evaluate the effects of stachydrine on HK-2 cell viability and oxidative stress. Results showed that stachydrine significantly reduced ROS levels and enhanced the expression of antioxidant enzymes. | Foods. 2025 May 12;14(10):1718 |
| Neonatal rat cardiomyocytes (NRCMs) | 10 µM | 48 hours | STA reduced ROS production, downregulated NOX2 protein expression, and regulated the translocation of its regulatory subunits in hypertrophic cardiomyocytes. | Int J Mol Sci. 2023 Sep 21;24(18):14369 |
| Bone marrow-derived macrophages (BMMs) | 0, 12.5, 25, 50, 100, 200 µM | 5 days | STA inhibited RANKL-induced osteoclast formation in a dose-dependent manner | J Cell Mol Med. 2019 Oct;23(10):6730-6743 |
| PC12 cells | 10 mM | 6 hours | To investigate the protective effect of stachydrine on oxygen-glucose deprivation (OGD)-induced injury in PC12 cells, results showed that stachydrine improved the survival rate of PC12 cells and reduced the release of inflammatory factors | Front Pharmacol. 2020 Feb 18;11:64 |
| Cardiac fibroblasts | 1-100 µM | 96 hours | Sta significantly inhibited AngII-induced proliferation and trans-differentiation of cardiac fibroblasts into myofibroblasts, and down-regulated the ACE/AngII/AT1R-TGFβ1 fibrogenic axis | Front Pharmacol. 2019 May 22;10:538 |
| Bone marrow-derived macrophages (BMMs) | 100 µM | Early stage (days 1-3) | STA significantly inhibited osteoclast formation in the early stage | J Cell Mol Med. 2019 Oct;23(10):6730-6743 |
In Vivo:
|
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
| C57BL/6 mice | LPS-induced inflammatory bone loss model | Intragastric administration | 10 mg/kg | Once daily for 7 days | STA alleviated LPS-induced bone loss and reduced osteoclast number | J Cell Mol Med. 2019 Oct;23(10):6730-6743 |
| Sprague-Dawley rats | Hyperhomocysteinemia-induced endothelial dysfunction model | Ex vivo organ culture | 10 μM | 12 hours | To evaluate the protective effect of STA on Hcy-induced endothelial dysfunction, results showed that STA effectively restored Hcy-impaired vascular relaxation. | Mol Med. 2018 Mar 19;24(1):10 |
| C57BL/6 mice | Pressure overload-induced cardiac fibrosis model | Oral gavage | 12 mg/kg | Once daily for 4 weeks | Sta significantly attenuated pressure overload-induced cardiac fibrosis, improved cardiac function and morphological remodeling, and down-regulated the ACE/AngII/AT1R-TGFβ1 fibrogenic axis | Front Pharmacol. 2019 May 22;10:538 |
| C57BL/6J mice | Colorectal cancer liver metastasis model | Oral | 15 mg/kg/d, 30 mg/kg/d, 60 mg/kg/d | Every other day for 3 weeks | To evaluate the inhibitory effect of Stachydrine on colorectal cancer liver metastasis. Results showed that Stachydrine significantly reduced the number and size of liver metastases and prolonged the survival of mice. | Front Pharmacol. 2025 Feb 5;16:1514158 |
| Sprague-Dawley rats | Middle Cerebral Artery Occlusion (MCAO) model | Caudal vein injection | 167.60 mM | Once daily for 24, 48, or 72 hours | To investigate the protective effect of stachydrine on cerebral ischemia-reperfusion injury, results showed that stachydrine significantly reduced the infarct volume, improved neurological deficit scores, and decreased the levels of inflammatory factors IL-1β and TNF-α | Front Pharmacol. 2020 Feb 18;11:64 |
| ICR mice | Hyperuricemia model induced by high-nucleoside diet | Intragastric administration | 20 or 40 mg/kg | Once daily for 4 weeks | To evaluate the effects of stachydrine on uric acid levels and renal injury in hyperuricemic mice. Results showed that stachydrine significantly reduced serum uric acid levels and alleviated renal inflammation and oxidative stress. | Foods. 2025 May 12;14(10):1718 |
| C57BL/6J mice | Transverse aortic constriction (TAC)-induced heart failure model | Gavage | 6 mg/kg/d or 12 mg/kg/d | Once daily for 6 weeks | STA improved cardiac function and morphology, reduced ROS production and NOX2 protein expression, inhibited NOX2-related calcium overload, and enhanced sarcomere contractility. | Int J Mol Sci. 2023 Sep 21;24(18):14369 |
| Bio Calculators | ||||
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1mg | 5mg | 10mg |
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1 mM 5 mM 10 mM |
5.57mL 1.11mL 0.56mL |
27.83mL 5.57mL 2.78mL |
55.67mL 11.13mL 5.57mL |
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| Dissolving Methods |
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:
in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day; The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
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Tags: Stachydrine | NF-κB | Endogenous Metabolite | Nuclear factor-κB | Nuclear factor-kappaB | 4136-37-2 |
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