DFP00173 |
Catalog No.GC38769
One-Click Copy Product Info
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DFP00173 is an aquaporin-3 (AQP3) inhibitor that inhibits mouse and human AQP3 with an IC50 value of approximately 0.1-0.4μM, exhibiting antitumor activity.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 672286-03-2
Sample solution is provided at 25 µL, 10mM.
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DFP00173 is an aquaporin-3 (AQP3) inhibitor that inhibits mouse and human AQP3 with an IC50 value of approximately 0.1-0.4μM, exhibiting antitumor activity[1, 2]. DFP00173 effectively inhibits intracellular H2O2 uptake[3].
In vitro, treatment of multiple myeloma cell lines (RPMI8226, KMS-11, U266, KMS-27) with DFP00173 (1μM) for 1-6 days significantly reduced the survival rate of all four cell lines, but did not significantly increase the rate of apoptosis, and inhibited cellular mitochondrial respiration[4]. Treatment of HCT8 cells with DFP00173 (5μM) for 45min reduced cell viability and glycerol uptake[5].
In vivo, DFP00173 (20mg/kg) administered via intradiscal injection for 5 weeks in a rat model of intervertebral disc degeneration (IVDD) induced by annular puncture (AFP) restored the intervertebral disc space in IVDD rats[6].
References:
[1] Sonntag Y, Gena P, Maggio A, et al. Identification and characterization of potent and selective aquaporin-3 and aquaporin-7 inhibitors[J]. Journal of Biological Chemistry, 2019, 294(18): 7377-7387.
[2] Pimpão C, da Silva I V, Soveral G. The expanding role of aquaporin-1, aquaporin-3 and aquaporin-5 as transceptors: Involvement in cancer development and potential druggability[J]. International Journal of Molecular Sciences, 2025, 26(3): 1330.
[3] Mu K, Kitts D D. Application of a HyPer-3 sensor to monitor intracellular H2O2 generation induced by phenolic acids in differentiated Caco-2 cells[J]. Analytical Biochemistry, 2022, 659: 114934.
[4] Tanaka M, Yasui M, Hara-Chikuma M. Aquaporin 3 inhibition suppresses the mitochondrial respiration rate and viability of multiple myeloma cells[J]. Biochemical and Biophysical Research Communications, 2023, 676: 158-164.
[5] Angelini I, Centrone M, Caponio G R, et al. MOMAST® Downregulates AQP3 Expression and Function in Human Colon Cells[J]. Antioxidants, 2024, 14(1): 26.
[6] Sang Y, Zhao H, Wu J, et al. Downregulation of aquaporin 3 promotes hyperosmolarity-induced apoptosis of nucleus pulposus cells through PI3K/Akt/mTOR pathway suppression[J]. arXiv preprint arXiv:2507.02231, 2025.
| Cell experiment [1]: | |
Cell lines | RPMI8226, KMS-11, U266, KMS-27 cells |
Preparation Method | Cells were incubated with anti-AQP3 mAb (1µg/mL), an equal concentration of control IgG (mouse IgG2a isotype control), DFP00173 (1µM), or vehicle (0.01% DMSO) for 1-6 days. Cell viability was quantified using the CellTiter-Glo Luminescent Cell Viability assay. |
Reaction Conditions | 1µM; 1-6 days |
Applications | Both anti-AQP3 mAb (1µg/mL) and DFP00173 (1µM) significantly reduced the numbers of viable RPMI8226, KMS-11, U266, and KMS-27 cells compared to corresponding controls treated with IgG. |
| Animal experiment [2]: | |
Animal models | Sprague-Dawley rats |
Preparation Method | Rats were randomly allocated into four experimental groups using stratified randomization based on body weight: Control, Annulus fibrosus puncture (AFP), AFP+AQP3 inhibitor DFP00173, AFP+AAV-AQP3. Animals were anesthetized via intraperitoneal injection of sodium pentobarbital (40mg/kg) and positioned prone on a warming pad. Under fluoroscopic guidance (C-arm Ziehm Vision RFD 3D), the caudal intervertebral disc (Co6/7 level) was exposed through a posterolateral approach. A 26-gauge spinal needle was inserted perpendicular to the annulus fibrosus at 5mm depth, followed by 360° rotation with 30-second dwell timeto induce controlled annular injury. DFP00173 (20mg/kg) or AAV-AQP3 solution were intradiscally injected using a microsyringe. Postoperative analgesia was maintained with meloxicam for 72h. Weekly booster injections were administered under isoflurane anesthesia. |
Dosage form | 20mg/kg; 5 weeks; intradiscally injected |
Applications | After 5 weeks of treatment with DFP00173, micro-CT imaging showed that the intervertebral disc space width was restored in rats. |
References: | |
| Cas No. | 672286-03-2 | SDF | |
| Canonical SMILES | O=C(NC1=CSC([N+]([O-])=O)=C1)NC2=C(Cl)C=CC=C2Cl | ||
| Formula | C11H7Cl2N3O3S | M.Wt | 332.16 |
| Solubility | DMSO: 125 mg/mL (376.32 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.0106 mL | 15.053 mL | 30.106 mL |
| 5 mM | 602.1 μL | 3.0106 mL | 6.0212 mL |
| 10 mM | 301.1 μL | 1.5053 mL | 3.0106 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)