ONO 1301

ONO 1301用途

ONO 1301(ONO-AP 500-02)是一种前列腺素(PG)I2模拟物,是一种口服活性长效前列环素激动剂,具有血栓素合酶抑制活性。ONO 1301促进不同细胞类型肝细胞生长因子(HGF)的产生,并改善缺血诱导的小鼠、大鼠和猪的左心室功能障碍[1][2][3]。

点击显示

ONO 1301名称

[ CAS 号 ]:
176391-41-6

[ 英文名 ]:
ONO 1301

[英文别名 ]:

ONO 1301生物活性

[ 描述 ]:

[ 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

[体外研究]

ONO 1301(ONO-AP 500-02)以浓度依赖的方式抑制胶原诱导的聚集,IC50值为460nm[3]。ONO-1301(0-1000 nM)显著增加原代成骨细胞和ST2细胞中的碱性磷酸酶(ALP)活性[3]。

[体内研究]

ONO-1301(6 mg/kg；p.o.；/天,持续4周)改善实验性自身免疫性心肌炎后扩张型心肌病大鼠的血流动力学状态[1]。动物模型：8周龄雄性Lewis大鼠(肌球蛋白诱导的实验性自身免疫性心肌炎大鼠模型)[1]剂量：6mg/kg给药：口服/结果：血流动力学参数和血浆脑钠肽(BNP)水平均明显改善。

[参考文献]

[1]. Hirata Y, et al. Beneficial effect of a synthetic prostacyclin agonist, ONO-1301, in rat autoimmune myocarditis model. Eur J Pharmacol. 2013;699(1-3):81-87.

[2]. Kashiwagi H, et al. The novel prostaglandin I2 mimetic ONO-1301 escapes desensitization in an antiplatelet effect due to its inhibitory action on thromboxane A2 synthesis in mice. J Pharmacol Exp Ther. 2015;353(2):269-278.

[3]. Kanayama S, et al. ONO-1301 Enhances in vitro Osteoblast Differentiation and in vivo Bone Formation Induced by Bone Morphogenetic Protein. Spine (Phila Pa 1976). 2018;43(11):E616-E624.

ONO 1301物理化学性质

[ 熔点 ]:
147-158 °C

[ 分子式 ]:
C₂₆H₂₄N₂O₄

[ 分子量 ]:
428.48000

[ 精确质量 ]:
428.17400

[ PSA ]:
81.01000

[ LogP ]:
4.73390

[ 外观性状 ]:
固体

[ 储存条件 ]:
-20° C

ONO 1301安全信息

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

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

ONO 1301文献

Inhibition of cyclooxygenase-2 causes a decrease in coronary flow in diabetic mice. The possible role of PGE2 and dysfunctional vasodilation mediated by prostacyclin receptor.

J. Physiol. Biochem. 71 , 351-8, (2015)

Several lines of evidence suggest that cyclooxygenase-2 (COX-2) activity can have a beneficial role in the maintenance of vascular tone of the blood vessels in diabetes. Specifically, the increased pr...

Effect of prostaglandin I2 analogs on monocyte chemoattractant protein-1 in human monocyte and macrophage.

Clin. Exp. Med. 15 , 245-53, (2015)

Chemokines play essential roles during inflammatory responses and in pathogenesis of inflammatory diseases. Monocyte chemotactic protein-1 (MCP-1) is a critical chemokine in the development of atheros...

ONO-1301, a sustained-release prostacyclin analog, ameliorates the renal alterations in a mouse type 2 diabetes model possibly through its protective effects on mesangial cells.

Acta Med. Okayama 69(1) , 1-15, (2015)

Diabetic nephropathy is the most common pathological disorder predisposing patients to end-stage renal disease. Considering the increasing prevalence of type 2 diabetes mellitus worldwide, novel thera...

更多文献