DDR1-IN-4|cas:2125676-13-1|西域试剂

DDR1-IN-4,98.01%

产品编号：Bellancom-114173| CAS NO：2125676-13-1| 分子式：C₂₃H₂₀BrF₃N₆O₃| 分子量：565.34

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-114173		￥6500.00	杭州北京（现货）
Bellancom-114173		￥10500.00	杭州北京（现货）

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DDR1-IN-4

产品介绍

DDR1-IN-4 (Compound 2.45) 是有效、选择性的盘肽结构域受体 1 (DDR1) 自磷酸化的抑制剂，其对 DDR1 和 DDR2 的IC₅₀ 值分别为 29 nM 和 1.9 μM。

生物活性

DDR1-IN-4 (Compound 2.45) is a selective and potent Discoidin Domain Receptor 1 (DDR1) autophosphorylation inhibitor, with IC₅₀ values of 29 nM and 1.9 μM for DDR1 and DDR2, respectively.

体外研究

DDR1-IN-4 (Compound 2.45) shows a clear dose-dependent inhibition of DDR1 phosphorylation in HT1080 cells overexpressing DDR1, with greater than 70% inhibition of phosphorylation at a concentration of 1 μM, and retaining selectivity over inhibition of DDR2.

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

体内研究

DDR1-IN-4 (Compound 2.45, ip, 90 mg/kg) preserves renal function and reduces tissue damage in Col4a3^–/– mice (the preclinical mouse model of Alport syndrome) when employing a therapeutic dosing regime, indicating the real therapeutic value of selectively inhibiting DDR1 phosphorylation in vivo.

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

Animal Model:	Col4a3^–/– mice, a mouse model phenocopying Alport syndrome.
Dosage:	90 mg/kg.
Administration:	Injected intraperitoneally daily.
Result:	Resulted in a significant reduction of fibrosis evaluated by Picro Sirius Red, smooth muscle actin staining, and collagen I accumulation. Significantly reduces the levels of pDDR1 in Col4a3 knockout mice compared to controls.

体内研究

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

Animal Model:	Col4a3^–/– mice, a mouse model phenocopying Alport syndrome.
Dosage:	90 mg/kg.
Administration:	Injected intraperitoneally daily.
Result:	Resulted in a significant reduction of fibrosis evaluated by Picro Sirius Red, smooth muscle actin staining, and collagen I accumulation. Significantly reduces the levels of pDDR1 in Col4a3 knockout mice compared to controls.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (442.21 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7688 mL	8.8442 mL	17.6885 mL
5 mM	0.3538 mL	1.7688 mL	3.5377 mL
10 mM	0.1769 mL	0.8844 mL	1.7688 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 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (3.68 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.68 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。
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
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.68 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.68 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。