Description
ONO-7300243 is a novel, potent LPA1(Lysophosphatidic Acid Receptor) antagonist with an IC50 of 160 nM.
Product information
CAS Number: 638132-34-0
Molecular Weight: 461.55
Formula: C28H31NO5
Chemical Name: 2-(4-{[1-(3,5-dimethoxy-4-methylphenyl)-N-(3-phenylpropyl)formamido]methyl}phenyl)acetic acid
Smiles: CC1C(=CC(=CC=1OC)C(=O)N(CC1C=CC(CC(O)=O)=CC=1)CCCC1C=CC=CC=1)OC
InChiKey: WGABOZPQOOZAOI-UHFFFAOYSA-N
InChi: InChI=1S/C28H31NO5/c1-20-25(33-2)17-24(18-26(20)34-3)28(32)29(15-7-10-21-8-5-4-6-9-21)19-23-13-11-22(12-14-23)16-27(30)31/h4-6,8-9,11-14,17-18H,7,10,15-16,19H2,1-3H3,(H,30,31)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Solubility (25°C). 92 mg/mL(199.32 mM). Insoluble.
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Although ONO-7300243 showed only modest in vitro activity (IC50 = 0.16 μM), it showed much stronger effects in vivo (88% inhibition at 10 mg/kg i.d., 62% inhibition at 3 mg/kg i.d.). ONO-7300243 showed good membrane permeability and good metabolic stability against rat liver microsomes.
In Vivo:
Although ONO-7300243 showed only modest in vitro activity (IC50 = 0.16 μM), it showed much stronger effects in vivo (88% inhibition at 10 mg/kg i.d., 62% inhibition at 3 mg/kg i.d.). ONO-7300243 showed good membrane permeability and good metabolic stability against rat liver microsomes.
References:
- 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.
Products are for research use only. Not for human use.
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