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Merck

S8442

Sigma-Aldrich

SU 5416

≥98% (HPLC), powder, neuronal nitric oxide synthase inhibitor

别名:

1,3-二氢-3-[(3,5-二甲基-1H-吡咯-2-基)亚甲基]-2H-吲哚-2-酮

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About This Item

经验公式(希尔记法):
C15H14N2O
分子量:
238.28
MDL號碼:
分類程式碼代碼:
51111800
PubChem物質ID:
NACRES:
NA.77

product name

SU 5416, ≥98% (HPLC)

品質等級

化驗

≥98% (HPLC)

形狀

powder

顏色

yellow to yellow-orange

mp

221-222 °C

溶解度

DMSO: 20 mg/mL, clear (warmed)
H2O: insoluble

儲存溫度

−20°C

SMILES 字串

Cc1cc(C)c(C=C2C(=O)Nc3ccccc23)[nH]1

InChI

1S/C15H14N2O/c1-9-7-10(2)16-14(9)8-12-11-5-3-4-6-13(11)17-15(12)18/h3-8,16H,1-2H3,(H,17,18)/b12-8+

InChI 密鑰

WUWDLXZGHZSWQZ-XYOKQWHBSA-N

一般說明

SU 5416是一种血管内皮生长因子(VEGF)受体蛋白酪氨酸激酶1/2抑制剂。SU 5416可以抑制肿瘤生长和肿瘤血管新生。SU 5416抑制神经元型一氧化氮合酶活性,保护神经元细胞免遭一氧化氮介导的神经毒性伤害。也用作芳烃受体激动剂,还可能作为临床药物,有效治疗自身免疫疾病和移植排斥。

應用

SU 5416已用于在血管形成试验前处理人脐静脉内皮细胞(HUVEC),评估它对血管形成网络的影响。可诱发小鼠的肺动脉高压(PH)成为实验模型。

生化/生理作用

SU 516可抑制神经元一氧化氮合酶的活性并保护神经元细胞免受一氧化氮介导的神经毒性的影响。1 它还可作为芳烃受体的激动剂,是治疗自身免疫疾病和移植排斥的有效临床试剂。2
SU 5416是一种血管内皮生长因子(VEGF)受体蛋白酪氨酸激酶1/2抑制剂。

特點和優勢

该化合物是激酶磷酸酶生物学研究的推荐产品。点击这里 发现更多精选激酶磷酸酶生物学产品。了解更多有关用于其他研究领域的生物活性小分子的信息,请访问 sigma.com/discover-bsm

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

個人防護裝備

dust mask type N95 (US), Eyeshields, Gloves


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Joshua D Mezrich et al.
PloS one, 7(9), e44547-e44547 (2012-09-13)
The experimental compound SU5416 went as far as Phase III clinical trials as an anticancer agent, putatively because of its activity as a VEGFR-2 inhibitor, but showed poor results. Here, we show that SU5416 is also an aryl hydrocarbon receptor
Loredana Ciuclan et al.
American journal of respiratory and critical care medicine, 184(10), 1171-1182 (2011-08-27)
The complex pathologies associated with severe pulmonary arterial hypertension (PAH) in humans have been a challenge to reproduce in mice due to the subtle phenotype displayed to PAH stimuli. Here we aim to develop a novel murine model of PAH
Xiaowei Nie et al.
Journal of hypertension, 35(12), 2419-2435 (2017-07-14)
Similar to cancer, pulmonary arterial hypertension (PAH) is characterized by vascular remodeling, which leads to obliteration of the small pulmonary arteriole, with marked proliferation of pulmonary artery smooth muscle cells (PASMC) and/or endothelial cells dysfunction. Aberrant expression of tumor suppressor
Wei Cui et al.
PloS one, 7(9), e46253-e46253 (2012-10-11)
SU5416 was originally designed as a potent and selective inhibitor of vascular endothelial growth factor receptor-2 (VEGFR-2) for cancer therapy. In this study, we have found for the first time that SU5416 unexpectedly prevented 1-methyl-4-phenylpyridinium ion (MPP(+))-induced neuronal apoptosis in
Florian Ulrich et al.
Developmental biology, 357(1), 134-151 (2011-07-13)
The brain is made of billions of highly metabolically active neurons whose activities provide the seat for cognitive, affective, sensory and motor functions. The cerebral vasculature meets the brain's unusually high demand for oxygen and glucose by providing it with

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