墨蝶呤

墨蝶呤用途

L-Sepiapterin (Sepiapterin) 是内皮型一氧化氮合酶 (eNOS) 辅因子四氢生物喋呤 (BH4) 的前体。L-Sepiapterin 改善 db/db 小鼠肠系膜小动脉内皮功能障碍,诱导血管生成。L-Sepiapterin 通过下调 p70S6K 依赖性 VEGFR-2 表达抑制卵巢癌细胞增殖和迁移。

墨蝶呤名称

[ CAS 号 ]:
17094-01-8

[ 中文名 ]:
L-墨蝶呤

[ 英文名 ]:
L-Sepiapterin

[中文别名 ]:

墨蝶呤

[英文别名 ]:

MFCD00210214
Sepiapterine
L-Sepiapterin
Sepiapterin
2-Amino-6-L-lactoyl-7,8-dihydro-3H-pteridin-4-on
2-amino-6-L-lactoyl-7,8-dihydro-3H-pteridin-4-one

墨蝶呤生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

[ 靶点 ]

Human Endogenous Metabolite

[体外研究]

L-海藻氨酸(sepiapertein)(0.1-10μM；24hpurs)以剂量依赖的方式诱导细胞增殖[1]。L-海藻氨酸(1-50μM；20分钟)显著抑制VEGF-A诱导的(50 ng/ml)p70S6K的磷酸化[1]。L-海藻氨酸通过非独立机制抑制VEGF-A诱导的细胞增殖和迁移[1]。细胞增殖试验[1]细胞系：SKOV-3细胞浓度：0.1,1,10μM孵育时间：24h结果：诱导细胞增殖呈剂量依赖性。

[体内研究]

sepiapertein(10mg/kg；p.o.(powder chow)；每日或8周)显著改善db/db小鼠肠系膜小动脉(SMA)对Ach的舒张作用[2]。动物模型：雄性C57BL/KsJ糖尿病小鼠(db/db)[2]剂量：10mg/kg给药：P.o.(粉周)；每日或8周结果：db/db小鼠SMA对Ach的舒张作用明显改善。

[参考文献]

[1]. Pannirselvam M, et al. Chronic oral supplementation with sepiapterin prevents endothelial dysfunction and oxidative stress in small mesenteric arteries from diabetic (db/db) mice. Br J Pharmacol. 2003;140(4):701‐706.

[2]. Cho YR, et al. Sepiapterin inhibits cell proliferation and migration of ovarian cancer cells via down-regulation of p70S6K-dependent VEGFR-2 expression. Oncol Rep. 2011;26(4):861‐867.

墨蝶呤物理化学性质

[ 密度 ]:
1.9±0.1 g/cm3

[ 沸点 ]:
448.1ºC at 760 mmHg

[ 熔点 ]:
> 275 °C (lit.)

[ 分子式 ]:
C₉H₁₁N₅O₃

[ 分子量 ]:
237.215

[ 闪点 ]:
224.8ºC

[ 精确质量 ]:
237.086182

[ PSA ]:
133.46000

[ LogP ]:
-3.93

[ 外观性状 ]:
黄色固体

[ 蒸汽压 ]:
6.54E-10mmHg at 25°C

[ 折射率 ]:
1.822

[ 储存条件 ]:
20°C

墨蝶呤MSDS

详细MSDS(安全技术说明书)

墨蝶呤安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 安全声明 (欧洲) ]:
24/25

[ 危险品运输编码 ]:
NONH for all modes of transport

[ 海关编码 ]:
2933990090

墨蝶呤上下游产品

墨蝶呤上游产品

墨蝶呤下游产品

墨蝶呤海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

墨蝶呤文献

Bone Morphogenic Protein 4 Mediates NOX1-Dependent eNOS Uncoupling, Endothelial Dysfunction, and COX2 Induction in Type 2 Diabetes Mellitus.

Mol. Endocrinol. 29 , 1123-33, (2015)

We have recently shown that angiotensin II-mediated uncoupling of endothelial nitric oxide synthase (eNOS) contributes to endothelial dysfunction in streptozotocin-induced type 1 diabetes mellitus. Ho...

Sulfa drugs inhibit sepiapterin reduction and chemical redox cycling by sepiapterin reductase.

J. Pharmacol. Exp. Ther. 352(3) , 529-40, (2015)

Sepiapterin reductase (SPR) catalyzes the reduction of sepiapterin to dihydrobiopterin (BH2), the precursor for tetrahydrobiopterin (BH4), a cofactor critical for nitric oxide biosynthesis and alkylgl...

Stromal cell-derived factor 2 is critical for Hsp90-dependent eNOS activation.

Sci. Signal. 8 , ra81, (2015)

Endothelial nitric oxide synthase (eNOS) catalyzes the conversion of l-arginine and molecular oxygen into l-citrulline and nitric oxide (NO), a gaseous second messenger that influences cardiovascular ...

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墨蝶呤