ONO 1301

Names

[ Name ]:
ONO 1301

[Synonym ]:
2-((5-(2-(((phenyl(pyridin-3-yl)methylene)amino)oxy)ethyl)-7,8-dihydronaphthalen-1-yl)oxy)acetic acid
Acetic acid, ((7,8-dihydro-6-methyl-5-(2-(((phenyl-3-pyridinylmethylene)amino)oxy)ethyl)-1-naphthalenyl)oxy)-
7,8-Dihydro-5-[(E/Z)-[[α-(3-pyridyl)benzylidene]aminooxy]ethyl]-1-naphthyloxy]acetic acid

Biological Activity

[Description]:

ONO 1301 (ONO-AP 500-02), a prostaglandin (PG) I2 mimetic, is an orally active, long-acting prostacyclin agonist with thromboxane-synthase inhibitory activity. ONO 1301 promotes production of hepatocyte growth factor (HGF) from various cell types and ameliorates ischemia-induced left ventricle dysfunction in the mouse, rat and pig[1][2][3].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> GPCR/G Protein >> Prostaglandin Receptor

[In Vitro]

ONO 1301 (ONO-AP 500-02) inhibits collagen-induced aggregation in a concentration-dependent manner, with an IC50 value of 460 nM[3]. ONO-1301 (0-1000 nM) significantly increases alkaline phosphatase (ALP) activity in the primary osteoblasts and ST2 cells[3].

[In Vivo]

ONO-1301 (6 mg/kg; p.o.; /daily for 4 weeks) improves the hemodynamic status of rats with dilated cardiomyopathy after experimental autoimmune myocarditis[1]. Animal Model: Eight-week-old male Lewis rats (rat model of myosin-induced experimental autoimmune myocarditis)[1] Dosage: 6 mg/kg Administration: Orally; /daily for 4 weeks Result: Hemodynamic parameters and plasma brain natriuretic peptide (BNP) level were significantly improved.

[References]

[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.

Chemical & Physical Properties

[ Melting Point ]:
147-158 °C

[ Molecular Formula ]:
C₂₆H₂₄N₂O₄

[ Molecular Weight ]:
428.48000

[ Exact Mass ]:
428.17400

[ PSA ]:
81.01000

[ LogP ]:
4.73390

[ Storage condition ]:
-20° C

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

Articles

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...