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9,11-二脱氧基-9α,11α-亚甲基环氧前列腺素 F2α溶液

用途

U-46619 (9,11-Methanoepoxy PGH2) 是一种稳定的血栓素 A2 (TXA2) 的类似物,也是一种有效的 TXA2 激动剂。

名称

[ CAS 号 ]:
56985-40-1

[ 中文名 ]:
9,11-二脱氧基-9α,11α-亚甲基环氧前列腺素 F2α溶液

[ 英文名 ]:
U-46619

[英文别名 ]:

MFCD00135238

生物活性

[ 描述 ]:

U-46619 (9,11-Methanoepoxy PGH2) 是一种稳定的血栓素 A2 (TXA2) 的类似物,也是一种有效的 TXA2 激动剂。

[ 相关类别 ]:

研究领域 >> 心血管疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 前列腺素受体

[ 靶点 ]

TXA2[1]

[体外研究]

U-46619(1nm-10μM)引起血小板形状改变和聚集,且呈浓度依赖性,EC50s分别为0.58μM和0.013μM,用于聚集和形状改变[1]。U-46619(10nm-10μM)以类似浓度依赖性的浓度依赖性方式增加内部Ca2+浓度([Ca2+]i)并激活磷酸肌醇(PI)水解[1]。U-46619(3nm-10μM)还依赖于血小板膜中GTPase的浓度激活[1]。U-46619通过激活p38MAPK和ERK1/2信号通路提高人诱导多能干细胞向内皮细胞分化的效率[2]。

[体内研究]

U-46619(5μg/kg；静脉注射)使雄性自发性高血压大鼠(SHR)血压升高[3]。动物模型：12-15周龄雌雄SHR[2]剂量：5μg/kg给药：静脉注射结果：雄性SHR在注射1分钟后,MABP显著升高。

[参考文献]

[1]. Ohkubo S, et al. Thromboxane A2-mediated shape change: independent of Gq-phospholipase C--Ca2+ pathway in rabbit platelets. Br J Pharmacol. 1996 Mar;117(6):1095-104.

[2]. Su L, et al. The prostaglandin H2 analog U-46619 improves the differentiation efficiency of human induced pluripotent stem cells into endothelial cells by activating both p38MAPK and ERK1/2 signaling pathways. Stem Cell Res Ther. 2018 Nov 15;9(1):313.

[3]. Schirner M, et al. U 46619 induces different blood pressure effects in male and female spontaneously hypertensive rats (SHR). Prostaglandins Leukot Essent Fatty Acids. 1993 Jun;48(6):469-73.

物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
519.7±30.0 °C at 760 mmHg

[ 分子式 ]:
C₂₁H₃₄O₄

[ 分子量 ]:
350.492

[ 闪点 ]:
176.1±18.1 °C

[ 精确质量 ]:
350.245697

[ PSA ]:
66.76000

[ LogP ]:
3.90

[ 蒸汽压 ]:
0.0±3.1 mmHg at 25°C

[ 折射率 ]:
1.548

[ 储存条件 ]:
-20°C，密闭，干燥

MSDS

详细MSDS(安全技术说明书)

毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: MJ9681090

CHEMICAL NAME :: 5-Heptenoic acid, 7-(6-(3-hydroxy-1-octenyl)-2-oxabicyclo(2.2.1)hept-5- yl)-, (1R-(1-alpha, 4-alpha,5-beta(Z),6-alpha(1E,3S*)))-

CAS REGISTRY NUMBER :: 56985-40-1

LAST UPDATED :: 198306

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C21-H34-O4

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 66 ug/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - dyspnea Lungs, Thorax, or Respiration - other changes

REFERENCE :: JPETAB Journal of Pharmacology and Experimental Therapeutics. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1909/10- Volume(issue)/page/year: 224,369,1983

安全信息

[ 符号 ]:

GHS02, GHS07

[ 信号词 ]:
Danger

[ 危害声明 ]:
H225-H319-H336

[ 补充危害声明 ]:
Repeated exposure may cause skin dryness or cracking.

[ 警示性声明 ]:
P210-P280-P304 + P340 + P312-P305 + P351 + P338-P337 + P313-P403 + P235

[ 个人防护装备 ]:
Eyeshields;Faceshields;full-face respirator (US);Gloves;multi-purpose combination respirator cartridge (US);type ABEK (EN14387) respirator filter

[ 危害码 (欧洲) ]:
F;Xi

[ 风险声明 (欧洲) ]:
R11;R36;R66;R67

[ 安全声明 (欧洲) ]:
S16;S26

[ 危险品运输编码 ]:
UN 1231 3/PG 2

文献

P2X1-initiated p38 signalling enhances thromboxane A2-induced platelet secretion and aggregation.

Thromb. Haemost. 112(1) , 142-50, (2014)

ATP released by activated platelets can serve as a positive feedback machinery to amplify platelet responses by activating P2X1 receptors. It has, however, not been defined how P2X1 activities influen...

Thromboxane A(2) receptor stimulation promotes closure of the rat ductus arteriosus through enhancing neointima formation.

PLoS ONE 9(4) , e94895, (2014)

Ductus arteriosus (DA) closure follows constriction and remodeling of the entire vessel wall. Patent ductus arteriosus occurs when the DA does not close after birth, and this condition is currently tr...

A platelet P-selectin test predicts adverse cardiovascular events in patients with acute coronary syndromes treated with aspirin and clopidogrel.

Platelets 25(8) , 612-8, (2014)

There is wide variation in response to antiplatelet therapy and high on-treatment platelet reactivity is associated with adverse cardiovascular events. The objective here was to determine whether the ...

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