Referencia número: HY-179041

SZ0232

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SZ0232 is a selective mPGES-2 inhibitor. SZ0232 binds to the active site of mPGES-2 via hydrogen bonds and π-π stacking, reduces the production of prostaglandin E₂ (PGE₂) and blocks the PGE₂-EP3 pathway. SZ0232 regulates Ferroptosis by activating the heme-dependent p53/SLC7A11/GPX4 axis, inhibits lipid peroxidation, and protects renal tubules. SZ0232 enhances glucose-stimulated insulin secretion, inhibits β-cell senescence, and improves glucose homeostasis. SZ0232 reduces renal lipid accumulation, alleviates fibrosis, and ameliorates renal dysfunction in diabetic mice. SZ0232 inhibits renal cyst growth in polycystic kidney disease models. SZ0232 exhibits an insulinotropic effect that strengthens with the increase of animal age. SZ0232 can be used in studies related to type 2 diabetes, acute kidney injury, diabetic kidney disease, and autosomal dominant polycystic kidney disease.

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Pureza: 99.25%
No. CAS: 924851-91-2
Fòrmula: C₂₄H₃₀N₄O₇S
Peso molecular:518.58

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

SZ0232 Chemical Structure

No. CAS: 924851-91-2

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[2]

GPX4

Ver todos los productos específicos de isoformas Prostaglandin Receptor :

Ver todos los productos específicos de isoformas Glutathione Peroxidase :

GPX1
GPX4

In Vitro

SZ0232 (10^-9 to 10^-3; 10 min pre-incubation, 100 s assay incubation) potently inhibits mPGES-2 enzymatic activity via specific binding to the enzyme's active site, and reduces PGE₂ production in cell-free biochemical assays^[1].
SZ0232 (0.01-100 μM) shows no significant cytotoxicity in MIN6 mouse pancreatic islet β cells^[1].
SZ0232 inhibits β-cell senescence induced by mPGES-2 overexpression in INS-1 rat pancreatic islet β-cells^[1].
SZ0232 upregulates the expression of ferroptosis protective markers GPX4 and SLC7A11 in renal tubular epithelial cells HK-2^[2].
SZ0232 (40-160 μM; 8 days) inhibits Forskolin (HY-15371)-induced cyst growth in MDCK cells in a dose-dependent manner, with the maximum reduction in cyst diameter observed at the concentration of 160 μM^[4].
SZ0232 (0.1-1000 μM) shows no effect on the viability of normal MDCK cells^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

SZ0232 (i.p.; once daily; for 8 consecutive weeks; dose of 0.5 mg/kg) improves glucose tolerance, enhances the expression of β-cell identity markers and reduces β-cell senescence in db/db mice, with no systemic toxicity observed^[1].
SZ0232 (1 mg/kg; i.p.; once daily for 7 consecutive days) protects male C57BL/6 J mice against cisplatin-induced acute kidney injury (AKI), alleviating renal dysfunction, tubular injury, lipid peroxidation and cell death without altering PGE₂ levels^[2].
SZ0232 (1 mg/kg; i.p.; once daily; for 7 consecutive days) protects male C57BL/6 J mice against ischemia/reperfusion-induced acute kidney injury (AKI), and alleviates renal dysfunction, renal tubular injury, lipid peroxidation and cell death^[2].
SZ0232 (0.5 mg/kg; i.p.; once every two days; for 8 weeks) inhibits mPGES-2, improves renal lipid metabolism, alleviates renal function injury, podocyte injury and tubulointerstitial fibrosis, thereby blocking the progression of diabetic kidney disease (DKD)^[3].
SZ0232 (2 mg/kg/day; subcutaneous injection; daily, for 7 consecutive days) significantly reduces the kidney weight/body weight ratio, renal cyst index, and proliferation level of renal epithelial cells in ADPKD mouse models^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C57BKS-db/db (male, 8-week-old, mixed C57BKS and C57BL/6J background, type 2 diabetes genetic model)^[1]
Dosage:

0.5 mg/kg
Administration:

i.p.; daily; 8 weeks
Result:

Improved glucose tolerance relative to vehicle control, as shown by lower blood glucose levels at 15, 30, 60, 90, and 120 minutes during IPGTT, and a reduced area under the curve (AUC) for glucose (P=0.0414).
Increased relative expression of β-cell identity markers MafA (P=0.0125), Pdx1 (P=0.0445), Glut2 (P=0.0130), and NR4A1 (P=0.0368) in islets.
Significantly reduced relative expression of senescence markers p16 (P=0.0206), IGF1R (P=0.0311), and β-galactosidase (β-Gal) (P=0.0306) in islets.
Caused no significant changes in body weight, serum liver/kidney function indices, or histomorphology of liver, kidney, muscle, or white fat relative to control group.

Animal Model:

C57BL/6 J (8-week-old male, cisplatin-induced AKI)^[2]
Dosage:

1 mg/kg
Administration:

i.p.; daily; 7 days
Result:

Significantly reduced serum creatinine (SCr) levels (P=0.0451).
Significantly reduced blood urea nitrogen (BUN) levels (P=0.0007).
Reduced the tubular injury score (P<0.0001).
Increased renal glutathione (GSH) levels (P=0.0070).
Decreased renal malondialdehyde (MDA) levels (P=0.0005).
Reduced the percentage of TUNEL-positive renal cells (P=0.0001).
Did not alter renal prostaglandin E₂ (PGE₂) levels.

Animal Model:

C57BL/6 J (8-week-old male, ischemia/reperfusion-induced AKI)^[2]
Dosage:

1 mg/kg
Administration:

i.p.; daily; 7 days
Result:

Significantly reduced SCr levels (P=0.0498).
Significantly reduced BUN levels (P=0.0224).
Reduced the tubular injury score (P=0.0156).
Increased renal GSH levels (P=0.0185).
Decreased renal MDA levels (P=0.0015).
Reduced the percentage of TUNEL-positive renal cells (P=0.0013).

Animal Model:

db/db (leptin-receptor-deficient, 8-week-old)^[3]
Dosage:

0.5 mg/kg
Administration:

i.p.; once every two days; 8 weeks
Result:

Reduced urinary albumin-to-creatinine ratio and serum blood urea nitrogen levels.
Reduced tubular injury and glomerulosclerosis.
Decreased collagen deposition and tubulointerstitial fibrosis.
Reduced renal lipid accumulation.
Increased glomerular expression of podocyte markers WT-1, nephrin, and synaptopodin.
Reduced tubular expression of the injury marker KIM-1.
Decreased renal expression of ADRP and FABP5.

Animal Model:

C57BL/6 J mice (postnatal day 4 pups; Ksp-Cre; Pkd1flox/flox ADPKD model)^[4]
Dosage:

2 mg/kg/day
Administration:

s.c.; daily; 7 consecutive days
Result:

Reduced kidney weight-to-body weight ratio significantly compared with vehicle controls.
Reduced renal cyst index significantly compared with vehicle controls.
Decreased positive cell rates of proliferation markers PCNA and Ki67 significantly compared with vehicle controls.
Lowered PCNA protein expression relative to vehicle controls.

Chemical Information

No. CAS 924851-91-2
Appearance Solid
Peso molecular 518.58
Fòrmula C₂₄H₃₀N₄O₇S
Color White to off-white
SMILES

O=C(NCCOC1=CC=C(C=C1OCCNC(C)=O)NS(=O)(C2=CC=C(C=C2)N3CCCC3=O)=O)C
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (192.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9283 mL

9.6417 mL

19.2834 mL

5 mM

0.3857 mL

1.9283 mL

3.8567 mL

10 mM

0.1928 mL

0.9642 mL

1.9283 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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: ≥ 2.5 mg/mL (4.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (285 KB)
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)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Zhong D, et al. mPGES-2 blockade antagonizes β-cell senescence to ameliorate diabetes by acting on NR4A1. Nat Metab. 2022;4(2):269-283. [Content Brief]

[2]. Zhong D, et al. Targeting mPGES-2 to protect against acute kidney injury via inhibition of ferroptosis dependent on p53. Cell Death Dis. 2023;14(10):710. Published 2023 Oct 31. [Content Brief]

[3]. Zhong D, et al. Genetic or pharmacologic blockade of mPGES-2 attenuates renal lipotoxicity and diabetic kidney disease by targeting Rev-Erbα/FABP5 signaling. Cell Rep. 2024;43(4):114075. [Content Brief]

[4]. Zhong DD, et al. Inhibiting mPGES-2 impedes renal cyst growth in mice with polycystic kidney disease. Acta Pharmacol Sin. 2026;47(3):689-700. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	1.9283 mL	9.6417 mL	19.2834 mL	48.2086 mL
	5 mM	0.3857 mL	1.9283 mL	3.8567 mL	9.6417 mL
	10 mM	0.1928 mL	0.9642 mL	1.9283 mL	4.8209 mL
	15 mM	0.1286 mL	0.6428 mL	1.2856 mL	3.2139 mL
	20 mM	0.0964 mL	0.4821 mL	0.9642 mL	2.4104 mL
	25 mM	0.0771 mL	0.3857 mL	0.7713 mL	1.9283 mL
	30 mM	0.0643 mL	0.3214 mL	0.6428 mL	1.6070 mL
	40 mM	0.0482 mL	0.2410 mL	0.4821 mL	1.2052 mL
	50 mM	0.0386 mL	0.1928 mL	0.3857 mL	0.9642 mL
	60 mM	0.0321 mL	0.1607 mL	0.3214 mL	0.8035 mL
	80 mM	0.0241 mL	0.1205 mL	0.2410 mL	0.6026 mL
	100 mM	0.0193 mL	0.0964 mL	0.1928 mL	0.4821 mL

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SZ0232

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Ver todos los productos específicos de isoformas Prostaglandin Receptor

Ver todos los productos específicos de isoformas Glutathione Peroxidase

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

SZ0232 Related Classifications

HY-179041 Related Classifications