ONO-7300243|cas:638132-34-0|西域试剂

ONO-7300243,98.46%

产品编号：Bellancom-100882| CAS NO：638132-34-0| 分子式：C₂₈H₃₁NO₅| 分子量：461.55

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货号	价格	库存与货期
Bellancom-100882	￥900.00	杭州北京（现货）
Bellancom-100882	￥1600.00	杭州北京（现货）
Bellancom-100882	￥3500.00	杭州北京（现货）
Bellancom-100882	￥6200.00	杭州北京（现货）

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ONO-7300243

产品介绍

ONO-7300243 是一种新型有效的溶血磷脂酸受体 1 (LPA1) 拮抗剂，IC₅₀ 为 0.16 μM。

生物活性

ONO-7300243 is a novel, potent lysophosphatidic acid receptor 1 (LPA1) antagonist with IC₅₀ of 0.16 μM.

体外研究

ONO-7300243 shows modest in vitro activity (IC₅₀=0.16 μM). ONO-7300243 exhibits almost identical levels of antagonist activity in vitro.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

ONO-7300243 shows good efficacy in vivo. The oral dosing of 17a at 30 mg/kg leads to reduced intraurethral pressure in rats. ONO-7300243 shows stronge effects in vivo (88% inhibition at 10 mg/kg i.d., 62% inhibition at 3 mg/kg i.d.) compared with compound 12g. The results reveal that ONO-7300243 shows good membrane permeability and good metabolic stability against rat liver microsomes (MS). ONO-7300243 exhibits good selectivity towards LPAl over LPA2, most likely because low molecular weight and low lipophilicity lead to reduced compound promiscuity and increased selectivity. ONO-7300243 inhibits the LPA-induced IUP increase in a dose dependent manner (ID₅₀=11.6 mg/kg p.o.) up to 1 h after dosing. Significant effects are observed at 10 and 30 mg/kg (p<0.05 vs.vehicle). ONO-7300243 (30 mg/kg, p.o.) leads to a significant decrease in the IUP in conscious rats without LPA stimulation compared with the vehicle without affecting the mean blood pressure (MBP). The results of a rat pharmacokinetic study of ONO-7300243 show that this material had a rapid clearance (CLtot=15.9 mL/min/kg at 3 mg/kg i.v.) and a short half-life (0.3 h).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (216.66 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1666 mL	10.8331 mL	21.6661 mL
5 mM	0.4333 mL	2.1666 mL	4.3332 mL
10 mM	0.2167 mL	1.0833 mL	2.1666 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 3 mg/mL (6.50 mM); Clear solution

此方案可获得 ≥ 3 mg/mL (6.50 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 3 mg/mL (6.50 mM); Clear solution

此方案可获得 ≥ 3 mg/mL (6.50 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。