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| ln Vitro |
ETTAC-2 (0-26 μM, 1-48 h) induced LRG1 degradation in a time-dependent manner, with a DC50 value of 8.38 μM. This degradation could persist for 6 hours in HK-2 cells via the ubiquitin-proteasome pathway [1]. ETTAC-2 alleviated cell fibrosis in vitro by inhibiting the TGF-β-Smad3 pathway in HK-2 cells [1].
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| ln Vivo |
ETTAC-2 (50 mg/kg, intravenous injection, once daily for five consecutive days) can protect the structure and function of kidney tissue, reduce renal fibrosis, degrade LRG1 to inhibit the TGF-β-Smad3 pathway, and has good safety in a mouse model of unilateral ureteral obstruction (UUO mice) [1].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: HK-2 cells Tested Concentrations: 0, 1.625, 3.25, 6.5, 8.38, 13 and 26 μM Incubation Duration: 0, 1, 3, 5, 8, 18 and 24 hours Experimental Results: LRG1 degradation was induced in a time-dependent manner. |
| Animal Protocol |
Animal/Disease Models:Male C57BL/6 mice (20 g) (with unilateral ureteral obstruction model) [1]
Doses: 50 mg/kg Route of Administration: Intravenous injection, once daily for 5 consecutive days Experimental Results: Blood urea nitrogen (BUN) and serum creatinine (SCR) levels were significantly reduced. Kidney morphology was similar with no significant differences. The weight increase of obstructed kidneys was effectively reduced by 16.6%. Tubular dilation and tubular epithelial cell vacuolation caused by unilateral ureteral obstruction (UUO) were significantly reduced. Kidney pathological damage was reduced by about 50%. Matrix deposition was reduced by 64.3%. The mRNA expression levels of α-SMA, collagen-1A1 and fibronectin were reduced by 79.4%, 74.2% and 58%, respectively. The expression areas of α-SMA, collagen-1A1, and fibronectin decreased by 64.4%, 73.4%, and 71.9%, respectively. Protein expression of α-SMA, collagen-1A1, and fibronectin decreased by 60.3%, 61.6%, and 53.3%, respectively. This resulted in a 46.9% reduction in LRG1 overexpression and a 62.9% decrease in LRG1 levels. This led to a significant decrease in fluorescence signal and a significant improvement in tubular structure. Phosphorylated Smad3 levels decreased by 57.1%. There was no significant effect on body weight, nor did it cause significant morphological changes in major organs (including the heart, liver, spleen, and lungs). |
| References |
| Molecular Formula |
C83H123N23O26S
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|---|---|
| Molecular Weight |
1891.07
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| Sequence |
Lenalidomide-(CC)-Gly-Gly-Glu-Ser-Tyr-Ser-Ala-Lys-His-Arg-Ile-Met-Leu-ThrLenalidomide-(CC)-GGESYSAKHRIMLT
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| SequenceShortening |
Lenalidomide-(CC)-GGESYSAKHRIMLT
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| Appearance |
White to off-white solid
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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: 请将本产品存放在密封保护的环境中，避免受潮。 |
| 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 (~52.88 mM; with sonication)
H2O : ~2 mg/mL (~1.06 mM; with sonication) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (1.32 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 (1.32 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), 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 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 (1.32 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 | 0.5288 mL | 2.6440 mL | 5.2880 mL | |
| 5 mM | 0.1058 mL | 0.5288 mL | 1.0576 mL | |
| 10 mM | 0.0529 mL | 0.2644 mL | 0.5288 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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