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Collagen proline hydroxylase inhibitor-1

CAS# 223663-32-9

Collagen proline hydroxylase inhibitor-1

Catalog No. BCC1495----Order now to get a substantial discount!

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Chemical structure

Collagen proline hydroxylase inhibitor-1

3D structure

Chemical Properties of Collagen proline hydroxylase inhibitor-1

Cas No. 223663-32-9 SDF Download SDF
PubChem ID 9911272 Appearance Powder
Formula C24H21N5O4 M.Wt 443.45
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO
Chemical Name 8-(4-benzylpiperazine-1-carbonyl)-3-nitro-1H-1,10-phenanthrolin-4-one
SMILES C1CN(CCN1CC2=CC=CC=C2)C(=O)C3=CN=C4C(=C3)C=CC5=C4NC=C(C5=O)[N+](=O)[O-]
Standard InChIKey HPDVDDAVQSIBPH-UHFFFAOYSA-N
Standard InChI InChI=1S/C24H21N5O4/c30-23-19-7-6-17-12-18(13-25-21(17)22(19)26-14-20(23)29(32)33)24(31)28-10-8-27(9-11-28)15-16-4-2-1-3-5-16/h1-7,12-14H,8-11,15H2,(H,26,30)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Collagen proline hydroxylase inhibitor-1

DescriptionCollagen proline hydroxylase inhibitor-1 is an antifibroproliferative agents.

Collagen proline hydroxylase inhibitor-1 Dilution Calculator

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Preparing Stock Solutions of Collagen proline hydroxylase inhibitor-1

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.255 mL 11.2752 mL 22.5505 mL 45.1009 mL 56.3761 mL
5 mM 0.451 mL 2.255 mL 4.5101 mL 9.0202 mL 11.2752 mL
10 mM 0.2255 mL 1.1275 mL 2.255 mL 4.5101 mL 5.6376 mL
50 mM 0.0451 mL 0.2255 mL 0.451 mL 0.902 mL 1.1275 mL
100 mM 0.0226 mL 0.1128 mL 0.2255 mL 0.451 mL 0.5638 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Collagen proline hydroxylase inhibitor-1

Collagen proline hydroxylase inhibitor-1 is an antifibroproliferative agents.

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References on Collagen proline hydroxylase inhibitor-1

Specific inhibition of eIF-5A and collagen hydroxylation by a single agent. Antiproliferative and fibrosuppressive effects on smooth muscle cells from human coronary arteries.[Pubmed:7860726]

J Clin Invest. 1995 Feb;95(2):446-55.

Restenosis occurs in 35% of patients within months after balloon angioplasty, due to a fibroproliferative response to vascular injury. These studies describe a combined fibrosuppressive/antiproliferative strategy on smooth muscle cells cultured from human primary atherosclerotic and restenotic coronary arteries and from normal rat aortas. L-Mimosine suppressed the posttranslational hydroxylation of the precursors for collagen and for eukaryotic initiation factor-5A (eIF-5A) by directly inhibiting the specific protein hydroxylases involved, prolyl 4-hydroxylase (E.C. 1.14.11.2) and deoxyhypusyl hydroxylase (E.C. 1.14.99.29), respectively. Inhibition of deoxyhypusyl hydroxylation correlated with a dose-dependent inhibition of DNA synthesis. Inhibition of prolyl hydroxylation caused a dose-dependent reduction in the secretion of hydroxyproline-containing protein and decreased the formation of procollagen types I and III. The antifibroproliferative action could not be attributed to nonspecific or toxic effects of mimosine, appeared to be selective for the hydroxylation step in the biosynthesis of the procollagens and of eIF-5A, and was reversible upon removal of the compound. The strategy of targeting these two protein hydroxylases has important implications for the pathophysiology of restenosis and for the development of agents to control fibroproliferative diseases.

Induction of plasminogen activator inhibitor I gene expression by intracellular calcium via hypoxia-inducible factor-1.[Pubmed:15328163]

Blood. 2004 Dec 15;104(13):3993-4001.

The plasminogen activator inhibitor-1 (PAI-1) expression can be enhanced by hypoxia and other stimuli leading to the mobilization of intracellular calcium. Thus, it was the aim of the present study to investigate the role of calcium in the hypoxia-dependent PAI-1 expression. It was shown that the Ca(2+)-ionophore A23187 and the cell permeable Ca(2+)-chelator BAPTA-am (1,2-bis(2-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid-acetoxymethyl ester) induced PAI-1 mRNA and protein expression under normoxia and hypoxia in HepG2 cells. Transfection experiments with wild-type and hypoxia response element (HRE)-mutated PAI promoter constructs revealed that the HRE binding hypoxiainducible factor-1 (HIF-1) mediated the response to A23187 and BAPTA-am. Although A23187 induced a striking and stable induction of HIF-1alpha, BAPTA-am only mediated a fast and transient increase. By using actinomycin D and cycloheximide we showed that A23187 induced HIF-1alpha mRNA expression, whereas BAPTA-am acted after transcription. Although A23187 activated extracellular signal-regulated kinase (ERK), Jun N-terminal kinase (JNK), and p38 mitogen-activated protein kinase (MAPK), as well as protein kinase B, it appeared that the enhancement of HIF-1alpha by A23187 was only mediated via the ERK pathway. By contrast, BAPTA-am exerted its effects via inhibition of HIF-prolyl hydroxylase activity and von Hippel-Lindau tumor repressor protein (VHL) interaction. Thus, calcium appeared to have a critical role in the regulation of the HIF system and subsequent activation of the PAI-1 gene expression.

Description

Collagen proline hydroxylase inhibitor-1 is an antifibroproliferative agents.

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