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1,4-DPCA
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
1,4-DPCA图片
CAS NO:331830-20-7

1,4-DPCA,一种有效的选择性脯氨酰-4-羟化酶 (prolyl-4-hydroxylase) 抑制剂,也是人包皮成纤维细胞中的胶原蛋白羟基化抑制剂,IC50为 2.4 μM。1,4-DPCA 抑制脯氨酰-4-羟化酶 α 同工型,可稳定 HIF-1α 蛋白。1,4-DPCA 还抑制FIHIC50为 60 μM。
生物活性

1,4-DPCA, a potentprolyl-4-hydroxylaseinhibitor, is acollagen hydroxylationinhibitor in human foreskin fibroblasts with anIC50of 2.4 μM. 1,4-DPCA inhibits prolyl-4-hydroxylases α isoforms stabilizes HIF-1α protein. 1,4-DPCA also inhibitsfactor inhibiting HIF (FIH)with anIC50of 60 μM[1][2].

IC50& Target

IC50: 2.4 μM (Collagen hydroxylation); 60 μM (Factor inhibiting HIF (FIH))[2]

体外研究
(In Vitro)

1,4-DPCA (24 hours) treatment specifically increases the expression of multiple target genes, including the proangiogenic target genes Vegfa and Hmox1 and proglycolytic targets Ldh-a, Pgk1, Pdk1, and Glut1 in mouse B6 cells[1].
1,4-DPCA treatment significantly reduces the colony sizes of T4-2 (10 μM 1,4-DPCA) and ZR-75-1 cells (20 μM 1,4-DPCA). 1,4-DPCA-treated T4-2 cells form polarized spheroids in 3D culture. 1,4-DPCA treatment significantly reduces invasive branches in DA-MB-157 (20 μM 1,4-DPCA) and MDA-MB-231 (10 μM 1,4-DPCA) cells.1,4-DPCA inhibits the proliferation of T4-2, ZR-75-1, MDA-MB-157 and MDA-MB-231 cells[3].

体内研究
(In Vivo)

1,4-DPCA treatment suppresses connective tissue ingrowth in porous porous poly (lactic-co-glycolic acid) (PLGA) discs implanted in the peritoneal cavity for 28 days in mice. 1,4-DPCA is found to be effective at inhibiting collagen deposition within and on the outer surface of the disc, and also limited connective tissue ingrowth, but not to the extent of glucocorticoid inhibition[2].

分子量

240.21

性状

Solid

Formula

C13H8N2O3

CAS 号

331830-20-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 12.5 mg/mL(52.04 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM4.1630 mL20.8151 mL41.6302 mL
5 mM0.8326 mL4.1630 mL8.3260 mL
10 mM0.4163 mL2.0815 mL4.1630 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 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: 50%PEG300   50% saline

    Solubility: 10 mg/mL (41.63 mM); Suspended solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 0.92 mg/mL (3.83 mM); Clear solution

    此方案可获得 ≥ 0.92 mg/mL (3.83 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 9.2 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。
 
 
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