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| 1mg |
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| 5mg |
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| Targets |
Collagen proline hydroxylase inhibitor targets collagen proline hydroxylase (CP4H), an enzyme that catalyzes the hydroxylation of proline residues in procollagen chains. This post-translational modification is essential for the formation of stable collagen triple helices. By inhibiting CP4H, the compound prevents proper collagen folding and secretion, thereby disrupting collagen maturation and extracellular matrix deposition.
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| ln Vitro |
In vitro, Collagen proline hydroxylase inhibitor demonstrates inhibitory activity against collagen proline hydroxylase. The compound's inhibitory effects are typically assessed in enzyme activity assays measuring prolyl hydroxylation. By blocking collagen maturation, the compound can be used as a research tool to study collagen metabolism, fibrotic diseases, and extracellular matrix remodeling. Its activity is relevant for antifibrotic research applications.
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| ln Vivo |
In vivo studies of Collagen proline hydroxylase inhibitor are focused on evaluating its antifibrotic effects in animal models of fibrotic diseases. By inhibiting collagen proline hydroxylase, the compound disrupts collagen maturation and may reduce fibrosis. Preclinical studies show potential antifibrotic effects. Further in vivo studies are needed to fully characterize its efficacy, safety, and pharmacokinetic profile.
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| Enzyme Assay |
For in vitro enzyme assays, Collagen proline hydroxylase inhibitor is evaluated using enzymatic activity assays that measure prolyl hydroxylation. The compound is incubated with recombinant CP4H enzyme, procollagen substrate, and cofactors (such as alpha-ketoglutarate, ascorbate, and Fe2+) at various concentrations. Hydroxylation is quantified by measuring the release of succinate or by using labeled substrates. IC₅0 values are determined from dose-response curves.
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| Cell Assay |
For in vitro cellular experiments, Collagen proline hydroxylase inhibitor is tested in fibroblast cell lines or other collagen-producing cells. Cells are cultured in appropriate media and treated with various concentrations of the compound. Collagen synthesis and secretion are assessed by measuring hydroxyproline content, collagen protein levels by Western blotting, or using radioactive proline incorporation assays. The compound's effects on cell viability and proliferation are monitored.
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| Animal Protocol |
For in vivo animal experiments, Collagen proline hydroxylase inhibitor can be administered to rodents via various routes including oral gavage, intravenous injection, or intraperitoneal injection. The compound's efficacy can be evaluated in models of fibrotic diseases such as pulmonary fibrosis, liver fibrosis, or skin fibrosis. Tissue samples are collected for histological analysis of collagen deposition and measurement of hydroxyproline content.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Collagen proline hydroxylase inhibitor are not extensively characterized in the literature. As a small molecule with a molecular weight of 354.36, it may have reasonable bioavailability and tissue distribution. The compound is soluble in DMSO at 13.15 mg/mL. Detailed parameters such as Cₘₐₓ, Tₘₐₓ, AUC, half-life, and clearance would need to be determined through comprehensive PK studies.
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| Toxicity/Toxicokinetics |
Toxicological data for Collagen proline hydroxylase inhibitor are limited, as it is primarily a research tool. As an inhibitor of collagen maturation, its toxicity would depend on the importance of collagen for normal tissue structure and function. Comprehensive toxicology studies including acute and repeated-dose toxicity, genotoxicity, and cardiotoxicity assessments would be needed for further development. Appropriate safety precautions should be taken when handling this compound.
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| Additional Infomation |
Collagen proline hydroxylase inhibitor is a research compound used to study collagen metabolism and fibrotic diseases. No clinical trials or regulatory approvals have been reported for this compound as a therapeutic agent. It is available from various chemical suppliers for research purposes only. The compound is useful for antifibrotic proliferative agents and is used as a research tool to study collagen metabolism and extracellular matrix remodeling.
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| Molecular Formula |
354.36
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|---|---|
| Molecular Weight |
C18H18N4O4
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| Exact Mass |
354.133
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| CAS # |
223666-07-7
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| PubChem CID |
9928521
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| Appearance |
White to gray solid powder
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| LogP |
3.379
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
615
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XUARBCHSPWMKRC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H18N4O4/c1-3-7-21(4-2)18(24)12-8-11-5-6-13-16(15(11)19-9-12)20-10-14(17(13)23)22(25)26/h5-6,8-10H,3-4,7H2,1-2H3,(H,20,23)
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| Chemical Name |
N-ethyl-8-nitro-7-oxo-N-propyl-10H-1,10-phenanthroline-3-carboxamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~13.15 mg/mL (~37.11 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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