EMD638683 (S-Form)
Based on 1 Customer Validation
EMD638683 (S-Form) (Compound 1a), the S-enantiomer of EMD638683 (HY-15193), is a SGK1 inhibitor with an IC50 value > 300 nM. EMD638683 is an orally active SGK1 inhibitor with an IC50 of 3 μM. EMD638683 exhibits strong inhibition against SGK1, moderate inhibition against SGK2 and SGK3, and shows excellent selectivity for other AGC kinase family members. EMD638683 has antihypertensive activity by inhibiting SGK1, and independently of the blood pressure-lowering effect, it effectively prevents heart inflammation and fibrosis caused by hypertension by inhibiting the cardiac NLRP3 inflammation body/ IL-1β axis. EMD638683 promotes apoptosis of colon cancer cells and sensitizes radiotherapy. EMD638683 (S-Form) can be used in research related to hypertension, hypertensive heart damage, and colon cancer.
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- Purity: 99.95%
- CAS No.: 1184940-46-2
- 화학식: C18H18F2N2O4
- 분자량:364.34
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Kinase Inhibitor Library
HY-L009
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Metabolism/Protease Compound Library
HY-L012
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Anti-Cancer Compound Library
HY-L025
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Anti-Cardiovascular Disease Compound Library
HY-L046
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Pyroptosis Compound Library
HY-L059
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Anti-Colorectal Cancer Compound Library
HY-L103
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Antidepressant Compound Library
HY-L108
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Pain-Related Compound Library
HY-L139
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Antihypertensive Compound Library
HY-L145
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Metabolic Enzyme Compound Library
HY-L146
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Inflammasomes related Compound Library
HY-L175
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Protein Kinase Compound Library
HY-L196
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High-Throughput Bioactive Compound Library
HY-L205
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Posttranslational Modification Library
HY-L226
Biological Activity
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SGK1 > 300 nM (IC50) |
EMD638683 (50 μM; 9-25 h) inhibits NLRP3 inflammasome activation and IL-1β secretion in mouse bone marrow-derived macrophages induced by angiotensin II (Ang II) by targeting NLRP3 expression[2].
EMD638683 (50 μM; 25-49 h) inhibits angiotensin II-induced transformation of primary mouse cardiac fibroblasts into myofibroblasts by reducing IL-1β secretion from macrophages[2].
EMD638683 (50 μM; 96 h) enhances radiation-induced apoptotic death of Caco-2 colon cancer cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Caco-2 cells
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Concentration:50 μM
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Incubation Time:24 h pre-incubation, 72 h post-radiation incubation
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Result:Enhanced radiation-induced apoptotic cell death in Caco-2 colon carcinoma cells, including augmented cell shrinkage, mitochondrial depolarization, caspase 3 activation, phosphatidylserine exposure, and late apoptosis.
EMD638683 (600 mg/kg, administered via mixed feed for 4 weeks) prevents hypertension in wild-type mice treated with 10% fructose in isotonic saline for 4 weeks[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SV129 original background backcrossed 4 generations to C57BL/6J sgk1+/+ wild type (mixed gender, 4 months old, hyperinsulinemic salt-loaded)[1]
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Dosage:600 mg/kg
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Administration:p.o.; continuous in chow; 4 days
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Result:Normalized systolic blood pressure from 111 mmHg to 87 mmHg.
Significantly increased urinary flow rate.
Significantly decreased body weight.
Caused no significant changes to fluid intake, food intake, or urinary Na+ and K+ excretion.
Increased blood pressure to 106 mmHg after returning to placebo food.
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Animal Model:SV129 original background backcrossed 4 generations to C57BL/6J sgk1+/+ wild type (mixed gender, 7 to 10 months old, fructose/salt-induced hypertension)[1]
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Dosage:600 mg/kg
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Administration:p.o.; continuous in chow; 4 weeks
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Result:Prevented the fructose/salt-induced rise in systolic blood pressure.
Resulted in significantly lower systolic blood pressure compared to placebo-treated mice.
Chemical Information
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CAS No. 1184940-46-2
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Appearance Solid
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분자량 364.34
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화학식 C18H18F2N2O4
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Color Off-white to pink
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SMILES
CC1=C(CC)C(C(NNC([C@@H](O)C2=CC(F)=CC(F)=C2)=O)=O)=CC=C1O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
DMSO : ≥ 100 mg/mL (274.47 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.75 mg/mL (7.55 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.75 mg/mL (7.55 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Ackermann TF, et al. EMD638683, a novel SGK inhibitor with antihypertensive potency. Cell Physiol Biochem. 2011;28(1):137-146. [Content Brief]
[2]. Towhid ST, et al. Inhibition of colonic tumor growth by the selective SGK inhibitor EMD638683. Cell Physiol Biochem. 2013;32(4):838-848. [Content Brief]
[3]. Gan W, et al. The SGK1 inhibitor EMD638683, prevents Angiotensin II-induced cardiac inflammation and fibrosis by blocking NLRP3 inflammasome activation. Biochim Biophys Acta Mol Basis Dis. 2018;1864(1):1-10. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7447 mL | 13.7234 mL | 27.4469 mL | 68.6172 mL |
| 5 mM | 0.5489 mL | 2.7447 mL | 5.4894 mL | 13.7234 mL | |
| 10 mM | 0.2745 mL | 1.3723 mL | 2.7447 mL | 6.8617 mL | |
| 15 mM | 0.1830 mL | 0.9149 mL | 1.8298 mL | 4.5745 mL | |
| 20 mM | 0.1372 mL | 0.6862 mL | 1.3723 mL | 3.4309 mL | |
| 25 mM | 0.1098 mL | 0.5489 mL | 1.0979 mL | 2.7447 mL | |
| 30 mM | 0.0915 mL | 0.4574 mL | 0.9149 mL | 2.2872 mL | |
| 40 mM | 0.0686 mL | 0.3431 mL | 0.6862 mL | 1.7154 mL | |
| 50 mM | 0.0549 mL | 0.2745 mL | 0.5489 mL | 1.3723 mL | |
| 60 mM | 0.0457 mL | 0.2287 mL | 0.4574 mL | 1.1436 mL | |
| 80 mM | 0.0343 mL | 0.1715 mL | 0.3431 mL | 0.8577 mL | |
| 100 mM | 0.0274 mL | 0.1372 mL | 0.2745 mL | 0.6862 mL |
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