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

SH-11037 是一种强效的可溶性环氧化物水解酶 (sEH) 抑制剂，可与 sEH 水解酶结构域中的底物结合裂隙结合。SH-11037 呈剂量依赖性地抑制离体脉络膜血管生成实验中的血管生成，并抑制斑马鱼幼体眼部发育血管生成。SH-11037 可减少激光诱导的脉络膜新生血管 (CNV) 小鼠模型中的脉络膜新生血管病灶体积。SH-11037 在体外和体内均与抗 VEGF 治疗具有协同作用。SH-11037 可诱导 G2/M 期阻滞，并在有效浓度下维持视网膜内皮细胞的活力，且无明显毒性。SH-11037 可用于视网膜新生血管和眼部新生血管的研究。

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SH-11037

SH-11037 Chemical Structure

CAS No. : 1638153-78-2

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SH-11037 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

SH-11037 (14a) 可强效且选择性地抑制人视网膜微血管内皮细胞 (HRECs) 的增殖，其 GI50 为 0.055 μM，对 HUVECs 的选择性约为 14 倍，对 92-1 细胞的选择性超过 1000 倍，对 Y79 细胞的选择性约为 218 倍[1]。
SH-11037 可剂量依赖性地抑制人视网膜微血管内皮细胞 (HREC) 的增殖，且不会诱导凋亡性核改变[1]。
SH-11037 (30-600 nM) 呈剂量依赖性抑制划痕伤口实验中人视网膜微血管内皮细胞 (HRECs) 的迁移，在浓度≥300 nM 时可观察到显著抑制作用[1]。
SH-11037 (30-500 nM) 呈剂量依赖性抑制人视网膜微血管内皮细胞 (HRECs) 在基质胶上的管形成，当浓度≥100 nM 时可观察到显著抑制作用[1]。
SH-11037 (50-600 nM) 对人视网膜微血管内皮细胞 (HRECs) 仅诱导极少量细胞凋亡，在最高 600 nM 的浓度下，发生凋亡的细胞占比不足 10%[1]。
SH-11037 (30-1000 nM) 不会降低人视网膜微血管内皮细胞 (HRECs) 的存活率[1]。
SH-11037 (100-1000 nM; 48 h) 可在人视网膜微血管内皮细胞 (HRECs) 中引起剂量依赖性的 G2/M 期细胞周期阻滞，且无显著的细胞凋亡诱导作用[1]。
SH-11037 (1 μM; up to 2 h) 在 pH 7.4 磷酸盐缓冲液中稳定，但在小鼠血浆中会发生快速的定量酶解生成 SH-11008 (半衰期 0.018 min)，在犬血浆 (半衰期 69.1 min) 和人血浆 (半衰期 73.2 min) 中的水解速率较慢[2]。
SH-11037 (1 μM; up to 2 h) 在小鼠血浆和小鼠眼匀浆中，羧酸酯酶是介导其快速水解为 SH-11008 的主要酶；在犬血浆中，对氧磷酶 1 和丁酰胆碱酯酶介导较慢的水解，而在人血浆中仅对氧磷酶 1 介导该水解过程[2]。

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

SH-11037 相关抗体:

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.
体内研究
(In Vivo)

SH-11037 (5-10 mg/kg；静脉注射、口服；单次给药) 在雄性 ICR 小鼠中经静脉注射给药后会被快速且几乎完全转化为其代谢物 SH-11008 (fm = 102.7%)，而口服给药后血浆中未检测到 SH-11037 和 SH-11008[2]。
SH-11037 (1-10 μM；3 天) 抑制了斑马鱼幼虫的眼部血管生成[4]。
SH-11037 (0.1-100 μM；静脉注射；单次给药) 对视网膜无毒[4]。
SH-11037 (0.1-10 μM；静脉注射；单次给药) 呈剂量依赖性地抑制 CNV 病灶体积[4]。

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.
分子量

621.67

Formula

C34H39NO10
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

SH-11037 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

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Keywords:

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

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