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ONO-7300243 Sale

目录号 : GC12362

An LPA1 receptor antagonist

ONO-7300243 Chemical Structure

Cas No.:638132-34-0

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5mg
¥725.00
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25mg
¥2,678.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

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.

产品描述

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.

Chemical Properties

Cas No. 638132-34-0 SDF
化学名 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
分子式 C28H31NO5 分子量 461.22
溶解度 ≥ 46.1mg/mL in DMSO 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mM 2.1682 mL 10.8408 mL 21.6816 mL
5 mM 0.4336 mL 2.1682 mL 4.3363 mL
10 mM 0.2168 mL 1.0841 mL 2.1682 mL
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