Drpitor1a
Based on 1 Customer Validation
Drpitor1a is an orally active DRP1 GTPase inhibitor. Drpitor1a blocks mitochondrial fission, inhibits DRP1 GTPase activity, and reduces ROS levels. Drpitor1a induces mitochondrial fusion and mitochondria-dependent apoptosis by elevating Bak and Smac/Diablo and inhibiting Bcl-2. Drpitor1a inhibits proliferation in pulmonary arterial hypertension hPASMC and induces necrosis and autophagy mediators. Drpitor1a causes regression of non-small cell lung cancer tumors in mouse xenograft models and exhibits higher accumulation and efficacy in females. Drpitor1a can be used in research related to non-small cell lung cancer, myocardial ischemia-reperfusion injury, and pulmonary arterial hypertension.
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- Pureté : 96.95%
- CAS No.: 73326-98-4
- Formule: C15H8N2O2
- Masse moléculaire:248.24
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
Activité biologique
Description
IC50 & Target
[4]|
Bcl-2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.057 μM
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Inhibition of mitochondrial fragmentation in human A549 cancer cells.
Inhibition of mitochondrial fragmentation in human A549 cancer cells.
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PMC10378656 |
In Vitro
Drpitor1a effectively inhibits mitochondrial fragmentation in A549 cancer cells, with an IC50 of 0.057 μM[2].
Drpitor1a directly inhibits the GTPase activity of recombinant and endogenous Drp1 from PAH hPASMCs[4].
Drpitor1a (0.1 μM; 4-5 h) inhibits mitochondrial fission in PAH hPASMCs but does not alter mitochondrial morphology in normal hPASMCs; it reverses the fragmented mitochondrial network in PAH BOECs but does not change mitochondrial morphology in control human BOECs[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PAH hPASMC, normal hPASMC
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Concentration:0.1 μM
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Incubation Time:5 hours
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Result:Increased the accumulation of endogenous Drp1 on mitochondria in PAH hPASMC.
Did not alter total Drp1 expression in PAH hPASMC.\nIncreased the accumulation of exogenous Drp1 on mitochondria in PAH hPASMC.
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Cell Line:PAH hPASMC, normal hPASMC
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Concentration:1 μM
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Incubation Time:48 hours
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Result:Reduced cell proliferation in PAH hPASMC without significantly reducing the much lower proliferation rate of control hPASMC.
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Cell Line:PAH hPASMC
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Concentration:5 μM
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Incubation Time:48 hours
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Result:Increased unstimulated apoptosis in 2 of 3 PAH hPASMC cell lines, with an accompanying significant increase in the expression of the apoptosis mediators Bak, Smac/Diablo, and suppression of the anti-apoptosis mediator, Bcl-2.
Slightly increased the expression of receptor-interacting protein and the LC3B II/I ratio.
Parmacokinetics
| Species | Dose | Route | AUC0-t | AUC0-∞ | MRT | T1/2 (Elimination) | Tmax | Cmax | CLplasma | Vd | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat[4] | 1 mg/kg | i.v. | 552.5 nM·h | 844.3 nM·h | 7.2 h | 6.5 h | 0.08 h | 617.7 nM | 23.9 mL/min | 10.2 L | 26.0 % |
| Rat[4] | 1 mg/kg | i.v. | 1288.2 nM·h | 1433.8 nM·h | 2.4 h | 3.4 h | 0.08 h | 3250.4 nM | 13.1 mL/min | 1.9 L | 12.6 % |
| Rat[4] | 5 mg/kg | i.v. | 2496.9 nM·h | 3211.9 nM·h | 10.4 h | 9.9 h | 0.08 h | 2332.3 nM | 39.8 mL/min | 20.3 L | 21.1 % |
| Rat[4] | 5 mg/kg | i.v. | 5306.6 nM·h | 8577.4 nM·h | 27.5 h | 24.3 h | 0.08 h | 3425.0 nM | 13.7 mL/min | 14.3 L | 19.7 % |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
- Annexin V plus membrane-impermeant dye apoptosis staining
- ROS/oxidative-stress fluorescent staining
- Research Protocol for Cardiovascular Diseases
- Cell Viability Determination by MTT Colorimetric Assay
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Autophagy
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Lysosome and acidic-vesicle live-cell staining
- Subcutaneous Cell-Line-Derived Xenograft
- Macroautophagy Solutions
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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CAS No. 73326-98-4
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Appearance Solid
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Masse moléculaire 248.24
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Formule C15H8N2O2
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Color Light brown to brown
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SMILES
O=C1C2=C(C(C=CC=C3)=C3N2)C(C4=CN=CC=C41)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
In Vitro:
DMSO : 5 mg/mL (20.14 mM; ultrasonic and warming and heat to 60°C; 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (294 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
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.0284 mL | 20.1418 mL | 40.2836 mL | 100.7090 mL |
| 5 mM | 0.8057 mL | 4.0284 mL | 8.0567 mL | 20.1418 mL | |
| 10 mM | 0.4028 mL | 2.0142 mL | 4.0284 mL | 10.0709 mL | |
| 15 mM | 0.2686 mL | 1.3428 mL | 2.6856 mL | 6.7139 mL | |
| 20 mM | 0.2014 mL | 1.0071 mL | 2.0142 mL | 5.0354 mL |
Drpitor1a Related Classifications
HY-161119 Related Classifications
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Keywords
- Drpitor1a
- 73326-98-4
- Dynamin
- Reactive Oxygen Species (ROS)
- Bcl-2 Family
- Apoptosis
- non-small cell lung cancer
- DRP1 GTPase inhibitor
- mitochondrial-dependent apoptosis
- MCT-PAH rats
- mitochondrial fission
- cardiac ischemia/reperfusion injury
- pulmonary arterial hypertension hPASMC
- A549 cells
- reactive oxygen species
- PAH BOEC
- Inhibitor
- inhibitor
- inhibit