Product Details
| Product Name:
ONO-8430506 |
CAS No.:
1354805-08-5 |
| Purity:
97.05% |
Supply Ability:
10g |
| Release date:
2024/11/19 |
Product Introduction
Bioactivity
| Name | ONO-8430506 |
| Description | ONO-8430506 is an orally available, potent autotaxin (ATX)/ENPP2 inhibitor (IC90: 100 nM) that inhibits ATX activity in mouse plasma. |
| In vitro | The IC50 values of ONO-8430506 against the lysophospholipase D (LysoPLD) activity of recombinant human ATX/ENPP2 are 5.1 nM and 4.5 nM, determined using synthetic fluorescent substrate (FS-3) and a natural substrate (16:0-LPC) assay, respectively.[2]
ONO-8430506 exhibits effective inhibition of lysophosphatidic acid (LPA) formation, demonstrating IC50 values of approximately 10 nM with both recombinant and plasma-derived ATX/ENPP2 derived from diverse animal species.[2] |
| In vivo | ONO-8430506 (10 mg/kg/day; gavage; for 21 days) initially slows tumor growth and limits lung metastasis, with tumor size comparable to the vehicle group by day 13. It reduces the initial phase of breast tumor growth and lung metastases by ~60% in a syngeneic orthotopic mouse model. ONO-8430506 (oral; 30 mg/kg) demonstrates good pharmacokinetics and persistently inhibits plasma lysophosphatidic acid formation in rats. Additionally, ONO-8430506 (30 or 100 mg/kg) enhances the antitumor effect of Paclitaxel in a breast cancer model. The compound exhibits moderate oral bioavailability (rat 51.6%, dog 71.1%, monkey 30.8%) and Cmax (rat 261, dog 1670, monkey 63 ng/mL) following oral administration (rat 1, dog 1, and monkey 1 mg/kg). |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 90.0 mg/mL (195.0 mM), Sonication is recommended.
|
| Keywords | ONO-8430506 | ONO 8430506 | ONO8430506 |
| Inhibitors Related | Theophylline monohydrate | Diphylline | Acefylline | Roflumilast | Theobromine | Apremilast | Isoprenaline hydrochloride | Indomethacin | Icariin | Theophylline | Vardenafil hydrochloride | Doxofylline |
| Related Compound Libraries | Bioactive Compound Library | Inhibitor Library | Bioactive Compounds Library Max |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
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$2800.00/100mg |
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United States