Ki16425 Debio 0719|cas:355025-24-0|西域试剂

Ki16425 Debio 0719,98.10%

产品编号：Bellancom-13285| CAS NO：355025-24-0| 分子式：C₂₃H₂₃ClN₂O₅S| 分子量：474.96

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货号	价格	库存与货期
Bellancom-13285	￥810.00	杭州北京（现货）
Bellancom-13285	￥1252.00	杭州北京（现货）
Bellancom-13285	￥4687.00	杭州北京（现货）

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Ki16425 Debio 0719

产品介绍

Ki16425 (Debio 0719) 是一种亚型选择性，竞争性的 EDG 家族受体拮抗剂，对 LPA1 和 LPA3 的 K_i 值分别为 0.34 μM，0.93 μM。Ki16425 (Debio 0719) 降低 LPA 诱导的 p42/p44 MAPK 激活。Ki16425 还可抑制 LPA 诱导的 HEK293A 细胞中 YAP/TAZ 的去磷酸化。

生物活性

Ki16425 (Debio 0719) is a subtype-selective, competitive antagonist of the EDG-family receptors, LPA1 and LPA3 with K_is of 0.34 μM and 0.93 μM, respectively. Ki16425 (Debio 0719) reduces the LPA-induced activation of p42/p44 MAPK. Ki16425 can also inhibit LPA-induced dephosphorylation of Yes-associated protein (YAP)/TAZ in HEK293A cells.

体外研究

Ki16425 (10 μM; 1.5 hours; HEK293A cells) treatment blocks LPA-induced dephosphorylation of YAP/TAZ in HEK293A cells. Ki16425 partially inhibits the ability of serum to repress YAP/TAZ phosphorylation, particularly at low serum concentrations (0.2%).

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

Western Blot Analysis

Cell Line:	HEK293A cells
Concentration:	10 μM
Incubation Time:	1.5 hours
Result:	Blocked LPA-induced dephosphorylation of YAP/TAZ. Partially inhibited the ability of serum to repress YAP/TAZ phosphorylation.

体内研究
(In Vivo)

Ki16425 (Debio 0719) (1-30 mg/kg; i.p.; at 30 min prior to LPA injection) inhibits LPA-induced neuropathic pain-like behaviors^[4].

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

Animal Model:	20-24 g male standard ddY-strain mice^[4]
Dosage:	1-30 mg/kg
Administration:	Intraperitoneal injection; at 30 minutes prior to LPA injection
Result:	LPA-induced neuropathic pain behaviors were attenuated in a dose-dependent manner.

体内研究

Ki16425 (Debio 0719) (1-30 mg/kg; i.p.; at 30 min prior to LPA injection) inhibits LPA-induced neuropathic pain-like behaviors^[4].

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

Animal Model:	20-24 g male standard ddY-strain mice^[4]
Dosage:	1-30 mg/kg
Administration:	Intraperitoneal injection; at 30 minutes prior to LPA injection
Result:	LPA-induced neuropathic pain behaviors were attenuated in a dose-dependent manner.

体内研究

Ki16425 (Debio 0719) (1-30 mg/kg; i.p.; at 30 min prior to LPA injection) inhibits LPA-induced neuropathic pain-like behaviors^[4].

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

Animal Model:	20-24 g male standard ddY-strain mice^[4]
Dosage:	1-30 mg/kg
Administration:	Intraperitoneal injection; at 30 minutes prior to LPA injection
Result:	LPA-induced neuropathic pain behaviors were attenuated in a dose-dependent manner.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (210.54 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1054 mL	10.5272 mL	21.0544 mL
5 mM	0.4211 mL	2.1054 mL	4.2109 mL
10 mM	0.2105 mL	1.0527 mL	2.1054 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: ≥ 2.5 mg/mL (5.26 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.26 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.26 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.26 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.26 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.26 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。