EMD638683 (S-Form)

Name: EMD638683 (S-Form)
Brand: MedChemExpress
SKU: HY-15193B
Rating: 4.5 (0 reviews)

Cat. No.: HY-15193B Purity: 99.95%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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.

For research use only. We do not sell to patients.

EMD638683 (S-Form) Chemical Structure

CAS No. : 1184940-46-2

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Other Forms of EMD638683 (S-Form):

EMD638683 In-stock
EMD638683 (R-Form) In-stock

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SGK1 SGK3 SGK2

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[4]

SGK1

> 300 nM (IC₅₀)

In Vitro

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.

Apoptosis Analysis^[3]

Cell Line:	Caco-2 cells
Concentration:	50 μM
Incubation Time:	24 h pre-incubation, 72 h post-radiation incubation
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.

In Vivo

EMD638683 (600 mg/kg, administered via mixed diet for 4 consecutive days) normalizes systolic blood pressure in hyperinsulinemic, salt-loaded wild-type mice, reducing their blood pressure from 111 mmHg to 87 mmHg over the 4-day treatment period^[1].
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.

Animal Model:	SV129 original background backcrossed 4 generations to C57BL/6J sgk1+/+ wild type (mixed gender, 4 months old, hyperinsulinemic salt-loaded)^[1]
Dosage:	600 mg/kg
Administration:	p.o.; continuous in chow; 4 days
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.

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]
Dosage:	600 mg/kg
Administration:	p.o.; continuous in chow; 4 weeks
Result:	Prevented the fructose/salt-induced rise in systolic blood pressure. Resulted in significantly lower systolic blood pressure compared to placebo-treated mice.

Molecular Weight

364.34

Formula

C₁₈H₁₈F₂N₂O₄

CAS No.

1184940-46-2

Appearance

Solid

Color

Off-white to pink

SMILES

CC1=C(CC)C(C(NNC([C@@H](O)C2=CC(F)=CC(F)=C2)=O)=O)=CC=C1O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.7447 mL	13.7234 mL	27.4469 mL
5 mM	0.5489 mL	2.7447 mL	5.4894 mL
10 mM	0.2745 mL	1.3723 mL	2.7447 mL

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.75 mg/mL (7.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.95%

Select Batch:

Data Sheet (277 KB) SDS (252 KB)

COA (246 KB) LCMS (265 KB)

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]

[4]. Sgk1 inhibitors for the prophylaxis and/or therapy of viral diseases and/or carcinomas US 20110060050 A1

Complete Stock Solution Preparation Table

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

EMD638683 (S-Form) Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EMD638683 (S-Form)1184940-46-2SGKDrug IsomerSerum-glucocorticoid regulated kinaseSerum and glucocorticoid-regulated kinasemouse bone marrow-derived macrophagescolon carcinomacaspase-1IL-1βAng IICaco-2 colon carcinoma cellsSGK1hyperinsulinemic miceNLRP3 inflammasomeNDRG1Inhibitorinhibitorinhibit

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EMD638683 (S-Form)

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Complete Stock Solution Preparation Table

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