ONO-7300243 |
Catalog No.GC12362
One-Click Copy Product Info
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ONO-7300243 es un nuevo y potente antagonista del receptor 1 del Ácido lisofosfatÍdico (LPA1) con IC50 de 0,16 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 638132-34-0
Sample solution is provided at 25 µL, 10mM.
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IC50: 160 nM
ONO-7300243 is a LPA1 antagonist.
Lysophosphatidic acids (LPAs), a bioactive class of phospholipids, are produced by autotaxin from lysophosphatidylcholine in blood. LPAs have a wide range of cellular responses, such as cell proliferation, intracellular Ca2+ mobilization, cell survival, and cell motility. Based on their specific properties, LPAs have been involved in various complex physiological responses, such as the contraction of smooth muscle, wound healing, coagulation, demyelization, as well as immunological competence.
In vitro: ONO-7300243 was identified as a novel and potent LPA1 antagonist. Importantly, it was found that ONO-7300243 showed equal potency to the α1 adrenoceptor antagonist tamsulosin that is clinically used for the treatment of dysuria with benign prostatic hyperplasia (BPH) [1].
In vivo: Animal study reported that although ONO-7300243 showed only modest in vitro activity (IC50 = 0.16 μM), the oral dosing of ONO-7300243 to rats resulted in much stronger effects on reducing intraurethral pressure (88% inhibition at 10 mg/kg i.d., 62% inhibition at 3 mg/kg i.d.). When compared with tamsulosin, ONO-7300243 had no effect on the mean blood pressure at this dose, which suggested that LPA1 antagonists could be used to treat BPH without affecting the blood pressure [1].
Clinical trial: Up to now, ONO-7300243 is still in the preclinical development stage.
Reference:
[1] Terakado M et al. Discovery of ONO-7300243 from a Novel Class of Lysophosphatidic Acid Receptor 1 Antagonists: From Hit to Lead. ACS Med Chem Lett. 2016 Aug 19;7(10):913-918. eCollection 2016.
Animal experiment: | Rats[1] The oral administration of ONO-7300243 (30 mg/kg, p.o.) is investigated to determine its effect on rat IUP. ONO-7300243 is studied in an LPA-induced rat intraurethral pressure (IUP) model. |
References: [1]. Terakado M, et al. Discovery of ONO-7300243 from a Novel Class of Lysophosphatidic Acid Receptor 1 Antagonists: From Hit to Lead. ACS Med Chem Lett. 2016 Aug 19;7(10):913-918. | |
| Cas No. | 638132-34-0 | SDF | |
| Chemical Name | 2-(4-((3,5-dimethoxy-4-methyl-N-(3-phenylpropyl)benzamido)methyl)phenyl)acetic acid | ||
| Canonical SMILES | O=C(O)CC1=CC=C(CN(C(C2=CC(OC)=C(C)C(OC)=C2)=O)CCCC3=CC=CC=C3)C=C1 | ||
| Formula | C28H31NO5 | M.Wt | 461.22 |
| Solubility | ≥ 46.1mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1682 mL | 10.8408 mL | 21.6816 mL |
| 5 mM | 433.6 μL | 2.1682 mL | 4.3363 mL |
| 10 mM | 216.8 μL | 1.0841 mL | 2.1682 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)