AM095
目录号 : KM9802 CAS No. : 1345614-59-6 纯度 : 98%

AM095 是一种选择性的 LPA1 受体拮抗剂。作用于人和鼠 转染 LPA1 的 CHO 细胞,AM095 拮抗 LPA 诱导的钙流动,IC50 分别为 0.025 和 0.023 μM。

规格 价格 是否有货 数量
5mg
In-stock
10mg
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50mg
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100mg
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200mg
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500mg 询价 In-stock
1g 询价 In-stock

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生物活性

AM095 is a selective LPA1 receptor antagonist. The IC50 for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA1-transfected CHO cells is 0.025 and 0.023 μM, respectively.

体外研究

AM095 is a potent LPA1 receptor antagonist because it inhibits GTPγS binding to Chinese hamster ovary (CHO) cell membranes overexpressing recombinant human or mouse LPA1 with IC50 values of 0.98 and 0.73 μM, respectively. AM095 inhibits LPA-driven chemotaxis of CHO cells overexpressing mouse LPA1 (IC50=778 nM) and human A2058 melanoma cells (IC50=233 nM). The IC50 of AM095 in the human LPA1 GTPγS binding assay is comparable with that of our previously published compound AM966 (IC50=0.98±0.17 μM) and the Debio-0719 compound (IC50=0.60±0.04 μM). AM095 inhibits the LPA-induced calcium flux of CHO cells stably transfected with human or mouse LPA1. The IC50 for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA1-transfected CHO cells is 0.025 and 0.023 μM, respectively.

体内研究

AM095 has high oral bioavailability and a moderate half-life and is well tolerated at the doses tested in rats and dogs after oral and intravenous dosing. After oral (10 mg/kg) dosing in rats, AM095 plasma concentrations peaked at 2 h with a Cmax of 41 μM, thereafter decreasing to 10 nM by 24 h. After intravenous (2 mg/kg) dosing, a Cmax of 12 μM is observed within 15 min, which also decreased to approximately 10 nM by 24 h, yielding a t1/2 of 1.79 h. In dogs, a single oral dose of 5 mg/kg yielded a peak plasma concentration of 21 μM within 15 min of dosing, which then decreased to 10 nM by 24 h. In contrast, an intravenous dose of 2 mg/kg resulted in a Cmax of 11 μM within 15 min and decreased to 15 nM by 8 h, yielding a t1/2 of 1.5 h.

分子式
C27H23N2NaO5
分子量
478.47
CAS号
1345614-59-6
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 83.33 mg/mL (174.16 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0900 mL 10.4500 mL 20.9000 mL
5 mM 0.4180 mL 2.0900 mL 4.1800 mL
10 mM 0.2090 mL 1.0450 mL 2.0900 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: Saline

    Solubility: 5 mg/mL (10.45 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.35 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.35 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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。

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.35 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.35 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

  • 4.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.35 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.35 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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