IN-1130|cas:868612-83-3|西域试剂

IN-1130,99.79%

产品编号：Bellancom-18758| CAS NO：868612-83-3| 分子式：C₂₅H₂₀N₆O| 分子量：420.47

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-18758	￥1000.00	杭州北京（现货）
Bellancom-18758	￥1700.00	杭州北京（现货）
Bellancom-18758	￥3500.00	杭州北京（现货）
Bellancom-18758	￥5500.00	杭州北京（现货）
Bellancom-18758	￥9500.00	杭州北京（现货）

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IN-1130

产品介绍

N-1130 是一种高度选择性的转化生长因子-β I 型受体激酶 (ALK5) 抑制剂，对 ALK5 介导的 Smad3 磷酸化的 IC₅₀ 为 5.3 nM。IN-1130 抑制酪蛋白的 ALK5 磷酸化 (IC₅₀=36 nM)，抑制 p38α 丝裂原活化的蛋白激酶 (IC₅₀=4.3 μM)。IN-1130 可抑制阻塞性肾病中的肾纤维化，阻止乳腺癌的肺转移。

生物活性

IN-1130 is a highly selective transforming growth factor-β type I receptor kinase (ALK5) inhibitor with an IC₅₀ of 5.3 nM for ALK5-mediated Smad3 phosphorylation. IN-1130 inhibits ALK5 phosphorylation of casein (IC₅₀=36 nM) and p38α mitogen-activated protein kinase (IC₅₀=4.3 μM). IN-1130 suppresses renal fibrosis in obstructive nephropathy and blocks breast cancer lung metastasis.

体外研究

IN-1130 (0.5, 1 μM; for 2 hours) inhibits TGF-β-stimulated Smad2 phosphorylation and subsequent nuclear translocation in HepG2 and 4T1 cells.
IN-1130 (1 μM; for 72 hours) restores the TGF-β-mediated decrease in E-cadherin protein expression. IN-1130 (1 μM; for 72 hours) inhibits TGF-β-induced MMPs mRNA expression and the gelatinolytic activity of secreted MMPs in MCF10A cells.
IN-1130 (1 μM; pretreated for 30 min) inhibits TGF-β-induced MDA-MB-231 cells, NMuMG, and MCF10A cells mobility and invasion.

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

Western Blot Analysis

Cell Line:	HepG2 and 4T1 cells
Concentration:	0.5, 1 μM
Incubation Time:	For 2 hours
Result:	Inhibited TGF-β-stimulated Smad2 phosphorylation.

RT-PCR

Cell Line:	MCF10A cells
Concentration:	1 μM
Incubation Time:	For 72 hours
Result:	Inhibited TGF-β-induced MMPs mRNA expression and the gelatinolytic activity of secreted MMPs.

体内研究
(In Vivo)

IN-1130 (10, 20 mg/kg/day; IP; for 7 and 14 days) reduces the extent of interstitial nephritis and fibrosis (arrowheads) with 10 mg/kg and significantly reduces or absent histopathological changes with 20 mg/kg in unilateral ureteral obstruction (UUO) rats.
IN-1130 (10, 20 mg/kg/day; for 14 days) dose-dependently decreases levels of TGF-β1 mRNA and suppresses phosphorylation of Smad2, α-SMA, myofibroblasts in rat UUO kidneys.
IN-1130 (40 mg/kg; IP; 3 times per week for 3 weeks) inhibits in vivo breast cancer metastasis to the lungs in MMTV/c-Neu mice (Eight-week-old female BALB/c mice).

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

Animal Model:	Six-week-old male Sprague–Dawley rats weighing 180-200 g
Dosage:	10 and 20 mg/kg
Administration:	IP; daily; for 7 and 14 days
Result:	Reduced the extent of interstitial nephritis and fibrosis (arrowheads) with 10 mg/kg.

体内研究

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

Animal Model:	Six-week-old male Sprague–Dawley rats weighing 180-200 g
Dosage:	10 and 20 mg/kg
Administration:	IP; daily; for 7 and 14 days
Result:	Reduced the extent of interstitial nephritis and fibrosis (arrowheads) with 10 mg/kg.

体内研究

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

Animal Model:	Six-week-old male Sprague–Dawley rats weighing 180-200 g
Dosage:	10 and 20 mg/kg
Administration:	IP; daily; for 7 and 14 days
Result:	Reduced the extent of interstitial nephritis and fibrosis (arrowheads) with 10 mg/kg.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (237.83 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3783 mL	11.8915 mL	23.7829 mL
5 mM	0.4757 mL	2.3783 mL	4.7566 mL
10 mM	0.2378 mL	1.1891 mL	2.3783 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: ≥ 1.43 mg/mL (3.40 mM); Clear solution

此方案可获得 ≥ 1.43 mg/mL (3.40 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 14.3 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