| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
ONO 1301 targets the prostacyclin (PGI2) receptor and thromboxane A2 synthase. As a prostacyclin agonist, it activates the PGI2 receptor, which mediates vasodilation and inhibition of platelet aggregation. Additionally, it inhibits thromboxane A2 synthase, reducing the production of thromboxane A2, a potent vasoconstrictor and platelet aggregator.
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| ln Vitro |
ONO 1301 (ONO-AP 500-02) has an IC50 value of 460 nM and suppresses collagen-induced aggregation in a concentration-dependent manner[3]. In primary osteoblasts and ST2 cells, ONO-1301 (0-1000 nM) dramatically raises alkaline phosphatase (ALP) activity [3].
In vitro, ONO 1301 acts as a prostaglandin I2 mimetic with thromboxane synthase inhibitory activity. It activates the prostacyclin receptor and inhibits thromboxane A2 synthase, producing a dual mechanism of action. Its in vitro activity is assessed by measuring its effects on platelet aggregation, vasodilation, and thromboxane production in relevant cell systems. |
| ln Vivo |
After experimental autoimmune myocarditis, ONO-1301 (6 mg/kg; oral; daily; 4 weeks) improves hemodynamic status in rats with dilated cardiomyopathy [1].
In vivo activity of ONO 1301 has been demonstrated in the DBTC-induced chronic pancreatitis model, where it suppresses pancreatic fibrosis by inhibiting monocyte activity through both direct effects and induction of hepatocyte growth factor (HGF). It also protects myocardium from ischemia/reperfusion injury. Its long-acting prostacyclin agonist activity supports once-daily dosing. |
| Enzyme Assay |
The in vitro enzyme/receptor binding (cell-free) assay for ONO 1301 involves measuring its binding to the prostacyclin receptor and its inhibitory activity against thromboxane A2 synthase. These assays use membrane preparations expressing the receptor and purified thromboxane synthase enzyme. The compound's affinity for the PGI2 receptor and its inhibitory potency against thromboxane synthase are determined using radioligand binding and enzyme activity assays.
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| Cell Assay |
In vitro cellular assays for ONO 1301 are performed using cells expressing the prostacyclin receptor, such as platelets and vascular smooth muscle cells. These assays measure the compound's ability to activate the PGI2 receptor by assessing downstream signaling pathways, such as cAMP accumulation. Its inhibitory effects on thromboxane production are also measured. These assays demonstrate its dual mechanism of action as a prostacyclin agonist and thromboxane synthase inhibitor.
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| Animal Protocol |
Animal/Disease Models: 8weeks old male Lewis rat (rat model of myosin-induced experimental autoimmune myocarditis) [1]
Doses: 6 mg/kg Route of Administration: oral; /daily for 4 weeks Experimental Results: Blood Fluid dynamics parameters and plasma brain natriuretic peptide (BNP) levels improved Dramatically. In vivo animal studies for ONO 1301 are conducted in models of chronic pancreatitis, such as the DBTC-induced model, and myocardial ischemia/reperfusion models. These studies typically involve oral administration of the compound, followed by assessment of fibrosis, inflammation, and tissue damage. The compound's ability to suppress fibrosis and protect against ischemia/reperfusion injury is evaluated. Its effects on HGF induction and monocyte activity are also assessed. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of ONO 1301 are characterized by oral activity and long-acting prostacyclin agonist activity. As an orally active compound, it is designed for systemic administration and has favorable ADME properties. Its long duration of action supports once-daily dosing for the treatment of chronic conditions such as pancreatitis and cardiovascular diseases.
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| Toxicity/Toxicokinetics |
Toxicology studies of ONO 1301 have been conducted to evaluate its safety profile. As a prostacyclin agonist and thromboxane synthase inhibitor, its toxicology profile includes effects on cardiovascular function, including vasodilation and platelet function. Preclinical toxicology studies include acute and repeat-dose toxicity assessments, as well as evaluations of cardiovascular safety.
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| References |
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| Additional Infomation |
ONO 1301 is a prostaglandin I2 mimetic with thromboxane synthase inhibitory activity, developed for the treatment of chronic pancreatitis and myocardial ischemia/reperfusion injury. It suppresses pancreatic fibrosis by inhibiting monocyte activity through both direct effects and induction of hepatocyte growth factor (HGF). The compound's dual mechanism offers a unique approach to treating fibrotic and ischemic conditions.
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| Molecular Formula |
C27H26N2O4
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|---|---|
| Molecular Weight |
442.5063
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| Exact Mass |
428.174
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| CAS # |
176391-41-6
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| Related CAS # |
(Z)-ONO 1301;153814-74-5
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| PubChem CID |
6536812
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| Appearance |
White to off-white solid powder
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| Melting Point |
147-158 °C
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| LogP |
4.733
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
32
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| Complexity |
671
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CC2=C(C=CC=C2OCC(=O)O)C(=C1)CCO/N=C(\C3=CC=CC=C3)/C4=CN=CC=C4
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| InChi Key |
WBBLIRPKRKYMTD-BYCLXTJYSA-N
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| InChi Code |
InChI=1S/C26H24N2O4/c29-25(30)18-31-24-13-5-11-22-19(9-4-12-23(22)24)14-16-32-28-26(20-7-2-1-3-8-20)21-10-6-15-27-17-21/h1-3,5-11,13,15,17H,4,12,14,16,18H2,(H,29,30)/b28-26+
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| Chemical Name |
2-[[5-[2-[(E)-[phenyl(pyridin-3-yl)methylidene]amino]oxyethyl]-7,8-dihydronaphthalen-1-yl]oxy]acetic acid
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| Synonyms |
Ono 1301; Ono-1301; Ono1301
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~116.69 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2598 mL | 11.2992 mL | 22.5984 mL | |
| 5 mM | 0.4520 mL | 2.2598 mL | 4.5197 mL | |
| 10 mM | 0.2260 mL | 1.1299 mL | 2.2598 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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