2. Metabolic Enzyme/Protease
  3. Epoxide Hydrolase
  4. SH-11037

SH-11037 is a potent inhibitor of soluble epoxide hydrolase (sEH) and docks to the substrate binding cleft in the sEH hydrolase domain. SH-11037 dose-dependently suppresses angiogenesis in the choroidal sprouting assay ex vivo and inhibited ocular developmental angiogenesis in zebrafish larvae. SH-11037 reduces choroidal neovascularisation lesion volume in the laser-induced CNV mouse model. SH-11037 synergises with anti-VEGF treatments in vitro and in vivo. SH-11037 induces G2/M phase blockade and retains retinal endothelial cell viability at active concentrations without overt toxicity. SH-11037 can be used for the research of retinal neovascularization and ocular neovascularization.

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SH-11037

SH-11037 Chemical Structure

CAS No. : 1638153-78-2

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SH-11037 Related Antibodies

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Description

SH-11037 is a potent inhibitor of soluble epoxide hydrolase (sEH) and docks to the substrate binding cleft in the sEH hydrolase domain. SH-11037 dose-dependently suppresses angiogenesis in the choroidal sprouting assay ex vivo and inhibited ocular developmental angiogenesis in zebrafish larvae. SH-11037 reduces choroidal neovascularisation lesion volume in the laser-induced CNV mouse model. SH-11037 synergises with anti-VEGF treatments in vitro and in vivo. SH-11037 induces G2/M phase blockade and retains retinal endothelial cell viability at active concentrations without overt toxicity. SH-11037 can be used for the research of retinal neovascularization and ocular neovascularization[1][2][3][4].

IC50 & Target[4]

sEH

 

In Vitro

SH-11037 (14a) potently and selectively inhibits the proliferation of human microvascular retinal endothelial cells (HRECs) with a GI50 of 0.055 μM, showing ~14-fold selectivity over HUVECs, >1000-fold selectivity over 92-1 cells, and ~218-fold selectivity over Y79 cells[1].
SH-11037 dose-dependently inhibits human microvascular retinal endothelial cell (HREC) proliferation without inducing apoptotic nuclear changes[1].
SH-11037 (30-600 nM) dose-dependently inhibits the migration of human microvascular retinal endothelial cells (HRECs) in a scratch wound assay, with significant inhibition observed at concentrations ≥300 nM[1].
SH-11037 (30-500 nM) dose-dependently inhibits the tube formation of human microvascular retinal endothelial cells (HRECs) on Matrigel, with significant inhibition observed at concentrations ≥100 nM[1].
SH-11037 (50-600 nM) induces minimal apoptosis in human microvascular retinal endothelial cells (HRECs), with <10% of cells undergoing apoptosis at concentrations up to 600 nM[1].
SH-11037 (30-1000 nM) does not reduce the viability of human microvascular retinal endothelial cells (HRECs)[1].
SH-11037 (100-1000 nM; 48 h) causes a dose-dependent G2/M phase cell cycle arrest in human microvascular retinal endothelial cells (HRECs) without significant induction of apoptosis[1].
SH-11037 (1 μM; up to 2 h) is stable in pH 7.4 phosphate buffer but undergoes rapid, quantitative enzymatic hydrolysis to SH-11008 in mouse plasma (half-life 0.018 min) and slower hydrolysis in dog (half-life 69.1 min) and human plasma (half-life 73.2 min)[2].
SH-11037 (1 μM; up to 2 h) has carboxylesterase as the predominant enzyme mediating rapid hydrolysis to SH-11008 in mouse plasma and mouse eye homogenate; paraoxonase 1 and butyrylcholinesterase mediate slower hydrolysis in dog plasma, while only paraoxonase 1 mediates hydrolysis in human plasma[2].

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

SH-11037 Related Antibodies

Cell Viability Assay[1]

Cell Line: human microvascular retinal endothelial cells
Concentration: 100 nM; 300 nM; 1000 nM
Incubation Time: 48 h
Result: Arrested HRECs at the G2/M phase of the cell cycle.
In Vivo

SH-11037 (5-10 mg/kg; i.v., p.o.; single dose) is rapidly and nearly completely converted to its metabolite SH-11008 (fm = 102.7%) following intravenous administration in male ICR mice, and neither SH-11037 nor SH-11008 are detectable in plasma following oral administration[2].
SH-11037 (1-10 μM) inhibits ocular angiogenesis in zebrafish larvae[4].
SH-11037 (0.1-100 μM; i.v.; single dose) has no toxic effects to eye[4].
SH-11037 (0.1-10 μM; i.v.; single dose) dose-dependently suppresses choroidal neovascularisation (CNV) lesion volume[4].

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

Animal Model: ICR (male, 8 weeks old, 30~35 g)[2]
Dosage: 5 mg/kg
Administration: i.v.; single dose
Result: Exhibited plasma levels below quantitation limit (<0.24 ng/mL) throughout 24-hour time course.
Produced hydrolytic metabolite with peak concentration (Cmax) of 738.1 ng/mL at 5 minutes, area under the curve (AUCinf) of 14,728.5 ng·min/mL, and half-life (t1/2) of 3.6 minutes, detected above quantitation limit up to 30 minutes.
Reached fraction converted to fm of 102.7%.
Animal Model: ICR (male, 8 weeks old, 30~35 g)[2]
Dosage: 10 mg/kg
Administration: p.o.; single dose
Result: Showed plasma levels below quantitation limit throughout 24-hour time course.
Animal Model: C57BL/6J (female, 6-8 weeks)[4]
Dosage: 0.1 μM; 1 μM; 10 μM; 100 μM
Administration: i.v.; single dose
Result: Showed no histological changes in retinal sections.
Showed no morphological changes to retinal thickness.
Showed no signs of retinal injury, apoptosis or inflammation.
Animal Model: C57BL/6J (female, 6-8 weeks)[4]
Dosage: 0.1 μM; 0.3 μM; 1 μM; 10 μM
Administration: i.v.; single dose
Result: Reduced CNV lesion size at 1 and 10 μM compared to vehicle controls.
Reduced leakiness of CNV lesions relative to the vehicle treatment.
Molecular Weight

621.67

Formula

C34H39NO10
CAS No.
SMILES

COC1=C2C(OCC(C2=O)CC3=CC(OC([C@@H](NC(OC(C)(C)C)=O)CC4=CC=CC=C4)=O)=C(C=C3)OC)=CC(OC)=C1OC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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SH-11037 Related Classifications

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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:

SH-110371638153-78-2SH11037SH 11037Epoxide Hydrolaseparaoxonase 1choroidal neovascularizationretinal neovascularizationG2/M phaseretinal endothelial cellshuman microvascular retinal endothelial cellsbutyrylcholinesteraseocular neovascularizationcarboxylesterasemouse plasmaInhibitorinhibitorinhibit

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