CPA inhibitor
Based on 3 publication(s) in Google Scholar
CPA inhibitor (Compound 5) (Carboxypeptidase inhibitor) is an orally active competitive carboxypeptidase A (CPA) inhibitor with a Ki value of 0.32 μM. CPA inhibitor blocks the activity of carboxypeptidase A3 (CPA3). CPA activator activates the Wnt/Lrp6/β-catenin signaling pathway. CPA inhibitor reduces epithelial damage. CPA inhibitor is applicable to research related to inflammatory bowel disease, including ulcerative colitis and Crohn's disease.
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- Pureté : 99.78%
- CAS No.: 223532-02-3
- Formule: C18H19NO4
- Masse moléculaire:313.35
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) CPA inhibitor
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Activité biologique
Description
IC50 & Target
Ki: 0.32 μM (CPA)[1]
In Vitro
CPA inhibitor potently inhibits purified carboxypeptidase A (CPA) as a competitive inhibitor with a Ki of 0.32 μM[1].
CPA inhibitor (10 μM; 3 days) treatment partially rescues activated bone marrow-derived mast cell-induced inhibition of mouse small intestinal organoid growth and function by restoring intestinal stem cell activity, reactivating the Wnt/Lrp6/β-catenin signaling pathway, and reducing apoptosis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 6 to 8 weeks old, 2.5% dextran sulfate sodium-induced acute colitis)[2]
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Dosage:200 mg/kg
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Administration:p.o.; initiated 6 days after DSS withdrawal; until day 12
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Result:Significantly promoted recovery, including increased body weight, improved Disease Activity Index (DAI), and attenuated colon shortening.
Alleviated epithelial damage as confirmed by histological evaluation.
Reversed DSS-induced downregulation of intestinal stem cell marker Lgr5 and stemness-associated gene Dek.
Partially restored Wnt signaling pathway activity, as indicated by elevated mRNA levels of Lrp6 and Ctnnb1, increased expression and nuclear translocation of total and active ß-catenin in colonic epithelial cells, and upregulated protein levels of Lrp6 and Lgr5.
Chemical Information
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CAS No. 223532-02-3
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Appearance Solid
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Masse moléculaire 313.35
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Formule C18H19NO4
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Color White to off-white
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SMILES
O=C(N(CC(C(O)=O)CC1=CC=CC=C1)O)CC2=CC=CC=C2
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Synonyms
Carboxypeptidase inhibitor
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Cell Mol Gastroenterol Hepatol
Mast Cells Inhibit Stem Cell-driven Epithelial Repair in Inflammatory Bowel Disease via Suppressing Wnt/lrp6/β-Catenin Signaling Pathway. [Abstract]2026;20(5):101741. PMID: 41616821 -
Int Immunopharmacol
First-line therapies analysis in advanced/metastatic urothelial carcinoma: prognostic insights in ADCs combined therapy with propensity score analysis and RNA-Seq. [Abstract]2026 Jan 15:169:116060. PMID: 41411730 -
Insect Biochem Mol Biol
Trypsin-type serine protease p37k hydrolyzes CPAP3-type cuticle proteins in the molting fluid of the silkworm Bombyx mori. [Abstract]2021 Oct:137:103610. PMID: 34182106
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (319.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.98 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.98 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
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DSS-Induced Colitis
Dextran sulfate sodium (DSS)-induced colitis is generated by administering DSS in mouse drinking water, producing epithelial injury, barrier disruption, weight loss, diarrhea, fecal blood, colon shortening, histologic mucosal damage, and inflammatory mediator changes; the model is mainly used to study acute or chronic intestinal inflammation resembling selected features of ulcerative colitis. DSS injury is interpreted through clinical and tissue readouts rather than a single molecular endpoint: daily body weight, stool consistency, and bleeding are combined into a disease activity index, while colon length, histology, cytokines, myeloperoxidase activity, intestinal permeability, and tight-junction markers provide complementary measures of inflammation and barrier damage.
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TNBS-Induced Colitis
TNBS-induced colitis is produced by intrarectal delivery of 2,4,6-trinitrobenzene sulfonic acid in ethanol, where ethanol disrupts the mucosal barrier and TNBS haptenates colonic proteins, generating immune-mediated colonic inflammation with weight loss, diarrhea, ulceration, transmural injury, inflammatory-cell infiltration, and cytokine responses. The model is used as an experimental intestinal inflammation model with Crohn’s disease–like features, especially when Th1-type responses, IL-12–dependent inflammation, chronic relapsing inflammation, or fibrosis-related endpoints are studied.
Pureté et documentation
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Fiche technique (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Kim DH, et al. First hydroxamate inhibitors for carboxypeptidase A. N-acyl-N-hydroxy-beta-phenylalanines. Bioorg Med Chem Lett. 1999;9(5):691-696. [Content Brief]
[2]. Zhang T, et al. Mast Cells Inhibit Stem Cell-driven Epithelial Repair in Inflammatory Bowel Disease via Suppressing Wnt/lrp6/β-Catenin Signaling Pathway. Cell Mol Gastroenterol Hepatol. 2026;20(5):101741. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1913 mL | 15.9566 mL | 31.9132 mL | 79.7830 mL |
| 5 mM | 0.6383 mL | 3.1913 mL | 6.3826 mL | 15.9566 mL | |
| 10 mM | 0.3191 mL | 1.5957 mL | 3.1913 mL | 7.9783 mL | |
| 15 mM | 0.2128 mL | 1.0638 mL | 2.1275 mL | 5.3189 mL | |
| 20 mM | 0.1596 mL | 0.7978 mL | 1.5957 mL | 3.9891 mL | |
| 25 mM | 0.1277 mL | 0.6383 mL | 1.2765 mL | 3.1913 mL | |
| 30 mM | 0.1064 mL | 0.5319 mL | 1.0638 mL | 2.6594 mL | |
| 40 mM | 0.0798 mL | 0.3989 mL | 0.7978 mL | 1.9946 mL | |
| 50 mM | 0.0638 mL | 0.3191 mL | 0.6383 mL | 1.5957 mL | |
| 60 mM | 0.0532 mL | 0.2659 mL | 0.5319 mL | 1.3297 mL | |
| 80 mM | 0.0399 mL | 0.1995 mL | 0.3989 mL | 0.9973 mL | |
| 100 mM | 0.0319 mL | 0.1596 mL | 0.3191 mL | 0.7978 mL |
CPA inhibitor Related Classifications
HY-70005 Related Classifications
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Keywords
- CPA inhibitor
- 223532-02-3
- Carboxypeptidase inhibitor
- Carboxypeptidase
- Wnt
- β-catenin
- ulcerative colitis
- crohn’s disease
- Wnt/lrp6/β-catenin signaling
- CPA Arg-145
- carboxypeptidase A3
- carboxypeptidase A
- CPA S1 hydrophobic pocket
- CPA active site zinc
- intestinal stem cell
- inflammatory bowel disease
- Inhibitor
- inhibitor
- inhibit