| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
The primary target of Collagen proline hydroxylase inhibitor-1 is prolyl 4-hydroxylase. This enzyme catalyzes the hydroxylation of proline residues in collagen, a post-translational modification essential for the stability of the collagen triple helix. By inhibiting this enzyme, the compound disrupts collagen synthesis and stabilization, leading to antifibroproliferative effects.
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|---|---|
| ln Vitro |
In vitro, Collagen proline hydroxylase inhibitor-1 exhibits antifibroproliferative activity. By inhibiting prolyl 4-hydroxylase, it reduces collagen production and deposition, which is a key process in fibrosis. This makes it a valuable tool for studying fibrotic diseases and for developing potential anti-fibrotic therapies. Its activity is typically assessed by measuring collagen synthesis in cell-based assays or by using purified enzyme.
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| ln Vivo |
In vivo efficacy data for Collagen proline hydroxylase inhibitor-1 are not extensively detailed. As an inhibitor of collagen synthesis, it is expected to have potential in animal models of fibrosis, such as pulmonary fibrosis, liver fibrosis, or skin scarring. However, specific in vivo studies with this compound have not been widely reported. It is intended for research use only.
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| Enzyme Assay |
For prolyl 4-hydroxylase inhibition assays, the enzymatic activity of recombinant prolyl 4-hydroxylase is measured. The enzyme is incubated with varying concentrations of the inhibitor in a reaction buffer containing a peptide substrate, ascorbate, 2-oxoglutarate, and Fe²⁺. The reaction is stopped, and the hydroxylated product is quantified using HPLC or a coupled enzyme assay. IC50 values are calculated.
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| Cell Assay |
For cellular studies, fibroblasts or other collagen-producing cells are cultured in appropriate medium. The compound is dissolved in DMSO and diluted in culture medium. Cells are treated with the compound, and collagen synthesis is assessed by measuring hydroxyproline content or by using radiolabeled proline incorporation. Cell proliferation is assessed by MTT or cell counting.
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| Animal Protocol |
For in vivo efficacy studies, animal models of fibrosis could be used. The compound would be formulated in vehicle and administered orally or intraperitoneally. Fibrosis would be assessed by measuring collagen content in tissues using hydroxyproline assay or by histopathological examination (e.g., Masson's trichrome staining). Inflammatory and fibrotic markers would also be analyzed.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Collagen proline hydroxylase inhibitor-1 are not extensively reported. As a small molecule with a molecular weight of 443.45, it is expected to have moderate oral bioavailability. Its metabolism likely involves hepatic CYP450 enzymes. A comprehensive PK study would be needed to determine its half-life, Cmax, and AUC for any potential therapeutic development.
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| Toxicity/Toxicokinetics |
Toxicological data for Collagen proline hydroxylase inhibitor-1 are limited. No acute toxicity, organ-specific toxicity, or mutagenicity data have been reported. As with all research chemicals, appropriate safety precautions should be taken during handling.
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| Additional Infomation |
Collagen proline hydroxylase inhibitor-1 (CAS 223663-32-9) is an antifibroproliferative agent that inhibits prolyl 4-hydroxylase. It has the molecular formula C₂₄H₂₁N₅O₄ and a molecular weight of 443.45. It is a research tool for studying fibrosis and is strictly for research use.
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| Molecular Formula |
C24H21N5O4
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|---|---|
| Molecular Weight |
443.455
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| Exact Mass |
443.159
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| CAS # |
223663-32-9
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| PubChem CID |
9911272
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
3.341
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
33
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| Complexity |
797
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1C([N+]([O-])=O)=CNC2=C1C=CC3=C2N=CC(C(N4CCN(CC4)CC5=CC=CC=C5)=O)=C3
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| InChi Key |
HPDVDDAVQSIBPH-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
8-(4-benzylpiperazine-1-carbonyl)-3-nitro-1H-1,10-phenanthrolin-4-one
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2550 mL | 11.2750 mL | 22.5499 mL | |
| 5 mM | 0.4510 mL | 2.2550 mL | 4.5100 mL | |
| 10 mM | 0.2255 mL | 1.1275 mL | 2.2550 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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