|2-((4-氯-1-胍基异喹啉)-7-磺酰胺)-2-甲基丙酸盐酸盐|CsnPharm

CAS No.: 256476-36-5

2-((4-Chloro-1-guanidinoisoquinoline)-7-sulfonamido)-2-methylpropanoic acid hydrochloride Catalog No. CSN23329

Synonyms: UK-371804 HCl

UK-371804 HCl is a potent and selective urokinase-type plasmogen activator (uPA) inhibitor with excellent enzyme potency (Ki=10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin).

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400-920-2911

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实验方案

技术信息

生物活性

描述Urokinase plasminogen activator (uPA) is one of the activators in Urokinase plasminogen activator system (uPAS). uPA converts the proenzyme plasminogen into proteolytically active form (plasmin), which are important for tumour growth and metastases（https://www.ncbi.nlm.nih.gov/pubmed/26834522）. UK-371804 HCl, a geminal dimethyl based on 1-Isoquinolinylguanidines, is a potent and selective uPA inhibitor with excellent enzyme potency (Ki=10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin), which can inhibit exogenous uPA in human chronic wound fluid with IC50 value of 0.89 µMin vitro. In vivo , Two female pigs were subjected to eight excisional wounds. The wounds were dressed and treated daily for 10 days with either 1 mL of a 10 mg/mL formulation of UK-371804 in hydrogel vehicle, or hydrogel vehicle alone (control), inhibit exogenous uPA activity was inhibited by 82.3±7.6% with the concentration of 41.8±9.0 μM by penetrating into pig wounds with no adverse effect on wound healing parameters. is of an acceptable size (as measured by MW) and reasonable lipophilicity (Log D7.4) and is within our target range for topical delivery. The ionization constant of the guanidine group is somewhat lower than usual and warrants additional comment^[1].
动物研究
剂量
Pig: 1 ml of a 10 mg/ml formulation^[1]
参考文献

动物研究
剂量	Pig: 1 ml of a 10 mg/ml formulation^[1]

[1] Fish PV. Selective urokinase-type plasminogen activator inhibitors. 4. 1-(7-sulfonamidoisoquinolinyl)guanidines. J Med Chem. 2007 May 17;50(10):2341-51. doi: 10.1021/jm061066t. Epub 2007 Apr 21.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3681 mL
- 11.8403 mL
- 23.6806 mL
- 5 mM
- 0.4736 mL
- 2.3681 mL
- 4.7361 mL
- 10 mM
- 0.2368 mL
- 1.1840 mL
- 2.3681 mL

技术信息

CAS号

256476-36-5

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H17Cl2N5O4S

运输

蓝冰

分子量

422.29

别名

UK-371804 HCl

溶解度

DMSO	30.0 mg/mL (71.0 mM) warming
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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2-((4-Chloro-1-guanidinoisoquinoline)-7-sulfonamido)-2-methylpropanoic acid hydrochloride Catalog No. CSN23329

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