| ONO-7300243LPA1 antagonist |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.05%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
ONO-7300243 Dilution Calculator
calculate
ONO-7300243 Molarity Calculator
calculate
| Cas No. | 638132-34-0 | SDF | Download SDF |
| Synonyms | N/A | ||
| 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 |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
