| Size | Price | Stock | Qty |
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| 5mg |
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| 50mg |
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| Targets |
KS370G targets multiple signaling pathways involved in metabolism and cardiovascular function. It lowers the phosphorylation of high-stress myocardial ERK, AKT, and GSK3β in pressure-overloaded mice hearts, indicating its role in modulating these stress-activated pathways. By inhibiting GSK-3β, KS370G is also being studied for its potential to treat neurodegenerative diseases such as Alzheimer's and Parkinson's, where GSK-3β activity contributes to disease progression. This multi-targeted approach allows KS370G to exert its protective effects in various tissues.
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| ln Vitro |
In vitro, KS370G's activity is primarily characterized by its ability to modulate key signaling pathways. It inhibits the phosphorylation of ERK, AKT, and GSK3β, which are critical mediators of cellular stress responses, survival, and metabolism. Its activity as an inhibitor of GSK-3β is of particular interest, as this enzyme is a key regulator of glycogen synthesis, insulin signaling, and neurodegeneration. These in vitro activities confirm its potential as a multi-targeted therapeutic agent for metabolic, cardiovascular, and neurodegenerative diseases.
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| ln Vivo |
By lowering the phosphorylation of high-stress myocardial ERK, AKT, and GSK3β, KS370G (1 mg/kg; oral; once daily for 8 weeks) enhances left ventricular function and prevents cardiac hypertrophy [1]. By decreasing neuronal and oxidative stress, oral medication (once daily for 13 days) mitigates unilateral ureteral blockage-induced kidney fibrosis in mice [2].
In vivo, KS370G demonstrates significant oral bioavailability and efficacy in various disease models. In diabetic models, it improves glucose homeostasis. At a dose of 1 mg/kg administered orally once daily for 8 weeks, KS370G enhances left ventricular function and prevents cardiac hypertrophy in pressure-overloaded mice. It also inhibits UUO-induced renal fibrosis marker expression and reduces collagen deposition in obstructed kidneys. These in vivo activities confirm its potential as a therapeutic agent for cardiovascular, metabolic, and renal diseases. |
| Enzyme Assay |
Non-cell-based assays for KS370G are not typical, as its mechanism involves the modulation of signaling pathways. However, its activity as a GSK-3β inhibitor can be assessed using in vitro kinase assays with purified GSK-3β enzyme. The compound is incubated with the enzyme, a peptide substrate, and ATP at varying concentrations. Kinase activity is measured by quantifying substrate phosphorylation. IC₅₀ values for GSK-3β inhibition can be determined.
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| Cell Assay |
Cellular assays for KS370G are performed using various cell lines to study its effects on signaling pathways. Cells are treated with the compound, and the phosphorylation of ERK, AKT, and GSK3β is assessed by Western blotting. Its effects on cell survival, proliferation, and metabolism are measured. These assays confirm the compound's ability to modulate these key signaling pathways.
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| Animal Protocol |
Animal/Disease Models: Pressure overload ICR mouse model [1]
Doses: 1 mg/kg Route of Administration: po (oral gavage), one time/day for 8 weeks. Experimental Results: Inhibited cardiac hypertrophy caused by pressure overload and improved cardiac function. Decreases plasma levels of atrial natriuretic peptide and lactate dehydrogenase. Dramatically diminished pressure overload-induced increases in α-SMA and ERK, AKT, and GSK3β phosphorylation. Collagen accumulation in the heart is diminished. Animal/Disease Models: Male ICR mouse, unilateral ureteral obstruction (UUO) model [2] Doses: 10 mg/kg Route of Administration: Orally, one time/day for 13 days Experimental Results: Dramatically attenuated collagen deposition in the obstructed kidney, and inhibited UUO-induced expression of renal fibrosis markers, including fibronectin, type I collagen, vimentin, and α-smooth muscle actin (α-SMA). Dramatically diminished renal expression of inflammatory chemokines/adhesion molecules and monocyte markers (MCP-1, VCAM-1, ICAM-1 and CD11b). diminished renal malondialdehyde l In vivo animal models for KS370G include pressure-overloaded mice for studying cardiac hypertrophy and function, and UUO (unilateral ureteral obstruction) models for studying renal fibrosis. The compound is administered orally at doses such as 1 mg/kg once daily for several weeks. Efficacy is assessed by measuring left ventricular function, cardiac hypertrophy, collagen deposition, and markers of inflammation and fibrosis. These studies confirm the compound's in vivo efficacy and its potential for treating cardiovascular and renal diseases. |
| ADME/Pharmacokinetics |
KS370G has a molecular weight of 283.32 g/mol and a molecular formula of C₁₇H₁₇NO₃. Its CAS number is 105955-01-9. The compound is supplied as a solid with a purity of >98%. It is soluble in DMSO. Storage conditions: -20°C. The compound demonstrates oral bioavailability, making it suitable for oral administration in animal studies. Detailed pharmacokinetic parameters such as half-life, Cmax, and volume of distribution are not extensively reported in the available literature.
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| Toxicity/Toxicokinetics |
Detailed toxicological data for KS370G are not extensively reported in the available literature. As a research compound, its safety profile would need to be established through standard preclinical toxicity assessments. The compound is intended for research use only and is not for human consumption. Standard laboratory safety precautions should be followed when handling the compound.
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| References |
[1]. Chuang ST, et al. KS370G, a caffeamide derivative, attenuates unilateral ureteral obstruction-induced renal fibrosis by the reduction of inflammation and oxidative stress in mice. Eur J Pharmacol. 2015 Mar 5;750:1-7.
[2]. Weng YC, et al. KS370G, a synthetic caffeamide derivative, improves left ventricular hypertrophy and function in pressure-overload mice heart. Eur J Pharmacol. 2012 Jun 5;684(1-3):108-15. [3]. Chuang ST, et al. KS370G, a caffeamide derivative, attenuates unilateral ureteral obstruction-induced renal fibrosis by the reduction of inflammation and oxidative stress in mice. Eur J Pharmacol. 2015 Mar 5;750:1-7. |
| Additional Infomation |
It has been reported that custard apple (Annona cherimola) contains caffeic acid phenylacetamide, and relevant data is available. See also: Water spinach (Ipomoea aquatica) leaves (partial).
KS370G is also known as caffeic acid phenethyl amide. It is an orally active hypoglycemic and cardiovascular protective agent. The compound improves left ventricular hypertrophy and function in pressure-overloaded mice and reduces collagen deposition in obstructed kidneys. By inhibiting GSK-3β, KS370G is also being studied for its potential to treat neurodegenerative diseases. Its mechanism involves lowering the phosphorylation of ERK, AKT, and GSK3β. KS370G is used in research for metabolic, cardiovascular, and neurodegenerative diseases. |
| Molecular Formula |
C17H17NO3
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| Molecular Weight |
283.32
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| Exact Mass |
283.121
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| Elemental Analysis |
C, 72.07; H, 6.05; N, 4.94; O, 16.94
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| CAS # |
105955-01-9
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| PubChem CID |
11391937
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| Appearance |
Solid powder
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| LogP |
3.31
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
21
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| Complexity |
350
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(/C=C/C1C=CC(=C(C=1)O)O)NCCC1C=CC=CC=1
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| InChi Key |
QOWABIXYAFJMQE-VQHVLOKHSA-N
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| InChi Code |
InChI=1S/C17H17NO3/c19-15-8-6-14(12-16(15)20)7-9-17(21)18-11-10-13-4-2-1-3-5-13/h1-9,12,19-20H,10-11H2,(H,18,21)/b9-7+
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| Chemical Name |
(E)-3-(3,4-dihydroxyphenyl)-N-(2-phenylethyl)prop-2-enamide
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| Synonyms |
KS 370 G; KS-370-G; KS370G
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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 (~352.96 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.82 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 can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.82 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5296 mL | 17.6479 mL | 35.2958 mL | |
| 5 mM | 0.7059 mL | 3.5296 mL | 7.0592 mL | |
| 10 mM | 0.3530 mL | 1.7648 mL | 3.5296 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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