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| ln Vitro |
Snail IN-1 (compound S29) (0.1-10 μM; 48 h) significantly downregulated the expression level of Snail protein in HUVEC cells in an in vitro concentration-dependent manner without affecting Snail mRNA levels, indicating that its regulatory effect occurs in the post-transcriptional stage [1]. Snail IN-1 (5-60 μM; 48 h) did not show significant cytotoxicity to HUVEC cells even at concentrations as high as 60 μM after 48 hours of incubation [1]. Snail IN-1 (5 μM; 0-240 min) accelerated the degradation of Snail protein and reduced its stability in HUVEC cells [1]. Snail IN-1 (2.5-20 μM; 48 h) specifically downregulated the expression level of Snail protein in HUVEC cells without affecting the protein or mRNA levels of other EMT transcription factors (Zeb1, Slug, Twist) [1]. Snail IN-1 (5 μM; 24 h) promotes the degradation of Snail by disrupting the interaction between Snail and CBP, reducing the acetylation level of Snail, and increasing the polyubiquitination of Snail in human umbilical vein endothelial cells (HUVECs) [1]. Snail IN-1 (2.5 μM; 24 h) significantly downregulated the mRNA levels of pro-atherosclerotic factors (CCL5, CXCL10, MMP-9, MMP-2) in TNF-α-stimulated HUVECs [1]. Snail IN-1 (1.25–5 μM; 24 h) inhibited the expression of CCL5 and CXCL10 proteins in TNF-α-stimulated HUVECs in a concentration-dependent manner [1]. Snail IN-1 (2.5 μM; 24 h) inhibited monocyte recruitment by altering the secretory properties of TNF-α-stimulated HUVECs [1].
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| ln Vivo |
Snail IN-1 (25-50 mg/kg; gavage; once daily; for 4 weeks) showed dose-dependent anti-atherosclerotic effects in ApoE-/- mice fed a high-fat diet, reducing plaque burden by decreasing the levels of inflammatory chemokines (CCL5, CXCL10) and matrix degrading enzymes (MMP2, MMP9) while increasing the levels of plaque stabilizing factors (collagen, α-SMA) [1]. Snail IN-1 (2000 mg/kg; gavage; single dose) was well tolerated in C57BL/6 mice without causing acute organ damage or dysfunction [1].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: Human umbilical vein endothelial cells (HUVECs) Tested Concentrations: 0.1, 1.25, 2.5, 5, 10 μM Incubation Duration: 48 hours Experimental Results: At a concentration of 10 μM, the Snail protein level (with β-actin as an internal control) decreased to 0.27 relative to the solvent control group. Snail protein levels were significantly reduced at concentrations of 0.1, 1.25, 2.5, and 5 μM. No significant changes were observed in Snail mRNA levels at any of the tested concentrations. Cytotoxicity assay [1] Cell Types: Human umbilical vein endothelial cells (HUVEC) Tested Concentrations: 5, 10, 20, 40, 60 μM Incubation Duration: 48 hours Experimental Results: At all test concentrations, the viability of HUVEC cells was not significantly reduced, and the cell viability remained above 90% relative to the solvent control group. Western Blot Analysis [1] Cell Types: Human umbilical vein endothelial cells (HUVECs) Tested Concentrations: 5 μM; containing cyclohexylimide (CHX) Incubation Duration: 0, 30, 60, 120, 240 minutes Experimental Results: Compared with cells treated with the vector, the degradation rate of Snail protein increased. After the addition of CHX, the relative level of Snail protein decreased at all time points, and the decrease was more significant over time.
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| Animal Protocol |
Animal/Disease Models:ApoE-/- mice (high-fat diet-induced atherosclerosis model; 4 weeks of treatment after modeling) [1]
Doses: 25 mg/kg; 50 mg/kg Route of Administration: Gavage; daily; 4 weeks Experimental Results: Compared with the control group, the aortic plaque area was reduced to 11.33% in the 25 mg/kg dose group and to an even lower but undetermined value in the 50 mg/kg dose group. The CCL5 area in the plaque was reduced to about 2% in the 50 mg/kg dose group (about 15% in the control group), and the CXCL10 area was reduced to about 1.5% (about 5% in the control group). At the 50 mg/kg dose, the collagen area in the plaque increased to about 45% (about 40% in the control group), and the α-SMA area increased to about 10% (about 3% in the control group). At a dose of 50 mg/kg, the area of MMP2 in the plaque was reduced by 64.2%, and the area of MMP9 was reduced by 60% (compared to the control group). Animal/Disease Models:C57BL/6 mice [1] Doses: 2000 mg/kg Route of Administration: Gavage; single dose Experimental Results: No adverse reactions, weight changes or organ weight abnormalities were observed. Histopathological analysis showed that the tissue structure of the heart, liver, spleen, lungs, kidneys and brain was normal, and no pathological changes were observed. The serum levels of liver injury markers (ALT, AST), kidney function markers (BUN, Scr) and metabolic indicators (Glu, LAC) were comparable to those of the solvent control group, with no statistically significant differences. |
| References |
| Molecular Formula |
C21H23N5O2S
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|---|---|
| Molecular Weight |
409.50
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| CAS # |
3083216-69-4
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| Appearance |
Off-white to light yellow solid
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| SMILES |
CC1=C(C=CN=C1CSC2=NC3=CC(N4C=CC=N4)=CC=C3N2)OCCCOC
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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 |
| 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 Vitro) |
DMSO : ~100 mg/mL (~244.20 mM; with sonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.11 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 canAdd 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of physiological saline: Dissolve 0.9 g of sodium chloride in double-distilled water and dilute to 100 mL to obtain clear physiological saline. 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 (6.11 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), Suspended solution. For example, if 1 mL of working solution is to be prepared, you canAdd 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD saline (4°C, store for one week): Dissolve 2 g of SBE-β-CD powder in 10 mL of saline until completely dissolved and clear. 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.11 mM)(saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4420 mL | 12.2100 mL | 24.4200 mL | |
| 5 mM | 0.4884 mL | 2.4420 mL | 4.8840 mL | |
| 10 mM | 0.2442 mL | 1.2210 mL | 2.4420 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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