2. Immunology/Inflammation GPCR/G Protein Apoptosis Membrane Transporter/Ion Channel Metabolic Enzyme/Protease
  3. PGE synthase Prostaglandin Receptor MDM-2/p53 Amino acid Transporter Glutathione Peroxidase Ferroptosis
  4. SZ0232

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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SZ0232

SZ0232 화학구조

CAS No. : 924851-91-2

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg   견적 받기  
200 mg   견적 받기  

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고객리뷰

Based on 1 Customer Validation

SZ0232 Related Antibodies

Top Publications Citing Use of Products

View All Prostaglandin Receptor Isoform Specific Products:

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DP EP FP IP TXA2/TP TXB2

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GPX1 GPX4

  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

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[1][2][3][4].

IC50 & Target[2]

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.

SZ0232 Related Antibodies
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.
분자량

518.58

화학식

C24H30N4O7S
CAS No.
Appearance

Solid

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
선적

Room temperature in continental US; may vary elsewhere.
보관
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
용액&용해도
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9283 mL 9.6417 mL 19.2834 mL
5 mM 0.3857 mL 1.9283 mL 3.8567 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 몰농도 계산기

  • 농도 희석 계산기

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 2.5 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.

    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: ≥ 2.5 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.

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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).
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.
순도&문서

Purity: 99.25%

SDS (252 KB)

COA (250 KB)

Handling Instructions (2659 KB)
References

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. 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 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:

SZ0232924851-91-2SZ 0232SZ-0232PGE synthaseProstaglandin ReceptorMDM-2/p53Amino acid TransporterGlutathione PeroxidaseFerroptosisProstaglandin E synthase氨基酸转运蛋白p53/SLC7A11/GPX4 axisferroptosisCOX-2renal tubular cellstype 2 diabetes mellitusmPGES-1prostaglandin E2PGE2-EP3 pathwaymicrosomal prostaglandin E synthase-2β-cellInhibitorinhibitorinhibit

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상품명:
SZ0232
Cat. No.:
HY-179041
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