Art. -Nr.: HY-161119

Drpitor1a

Name: Drpitor1a
Brand: MedChemExpress
SKU: HY-161119
Price: 650.00 USD
Availability: InStock
Rating: 5 (1 reviews)

Kundenbewertung

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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 96.95%
CAS. Nr.: 73326-98-4
Formel: C₁₅H₈N₂O₂
Molecular Weight:248.24

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Drpitor1a Chemical Structure

CAS. Nr.: 73326-98-4

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

HY-150031
MFI8

Mitochondrial Fusion Inhibitor

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[4]

Bcl-2

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC50	0.057 μM	Inhibition of mitochondrial fragmentation in human A549 cancer cells. Inhibition of mitochondrial fragmentation in human A549 cancer cells.	PMC10378656

In Vitro

Anti-cancerRegulation of Cardiac Pump FunctionMitochondrial FunctionOthersApoptosis

Anti-cancer

Regulation of Cardiac Pump Function

Drpitor1a is an inhibitor of DRP1 GTPase activity, exhibits cardioprotective properties in cardiac I/R injury, and has antiproliferative effects in lung cancer cells^[1].

Mitochondrial Function

Drpitor1a fused the mitochondrial network in A549 cells expressing wild-type Drp1; moreover, it had no effect on the already fused mitochondrial network in A549 cells expressing the loss-of-function Drp1 K38A mutant^[2].
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].

Others

Drpitor1a (1 μM; 48 h) inhibits the proliferation of PAH hPASMCs, but has no significant effect on the proliferation of normal hPASMCs^[4].

Apoptosis

Drpitor1a (5 μM; 48 h) induces apoptosis in PAH hPASMCs through a mitochondria-dependent apoptotic pathway^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Immunofluorescence^[4]

Cell Line:

PAH hPASMC, normal hPASMC
Concentration:

0.1 μM
Incubation Time:

5 hours
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.

Cell Proliferation Assay^[4]

Cell Line:

PAH hPASMC, normal hPASMC
Concentration:

1 μM
Incubation Time:

48 hours
Result:

Reduced cell proliferation in PAH hPASMC without significantly reducing the much lower proliferation rate of control hPASMC.

Apoptosis Analysis^[4]

Cell Line:

PAH hPASMC
Concentration:

5 μM
Incubation Time:

48 hours
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	AUC_0-t	AUC_0-∞	MRT	T_1/2 (Elimination)	T_max	C_max	CL_plasma	V_d	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

Oxidative StressCardiovascular RegulationRegulation of Cardiac Pump FunctionOthers

Oxidative Stress

Cardiovascular Regulation

Drpitor1a inhibits mitochondrial fission and reduces ROS levels in a rat myocardial ischemia-reperfusion injury model^[3].

Cardiovascular Regulation

Regulation of Cardiac Pump Function

Drpitor1a (1 mg/kg; intravenous injection; once every 48 hours; from day 17 to day 27) regressed Monocrotaline (HY-N0750)-induced PAH in female rats by reversing adverse pulmonary vascular remodeling and RV hypertrophy, improved right heart function, and had no systemic vascular effects or toxicity^[4].

Others

Drpitor1a (0.1-1.0 mg/kg; i.v.; every 48 hours) showed a trend toward efficacy in female but not male MCT-PAH rats^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Related Protocols :

Chemical Information

CAS. Nr. 73326-98-4
Appearance Solid
Molecular Weight 248.24
Formel C₁₅H₈N₂O₂
Color Light brown to brown
SMILES

O=C1C2=C(C(C=CC=C3)=C3N2)C(C4=CN=CC=C41)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.0284 mL

20.1418 mL

40.2836 mL

5 mM

0.8057 mL

4.0284 mL

8.0567 mL

10 mM

0.4028 mL

2.0142 mL

4.0284 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (294 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Chen R, et al. Targeting mitochondrial dynamics proteins for the treatment of doxorubicin-induced cardiotoxicity. Frontiers in molecular biosciences. 2023;10:1241225.

[2]. Colpman P, et al. The Role of Mitochondrial Dynamics and Mitotic Fission in Regulating the Cell Cycle in Cancer and Pulmonary Arterial Hypertension: Implications for Dynamin-Related Protein 1 and Mitofusin2 in Hyperproliferative Diseases. Cells. 2023 Jul 20;12(14):1897.

[3]. Rozich E, et al. Mitochondrial oxidative stress, calcium and dynamics in cardiac ischaemia-reperfusion injury. The Journal of physiology. 2026 Aug;604(16):6659-6674.

[4]. Wu D, et al. Novel Drp1 GTPase Inhibitor, Drpitor1a: Efficacy in Pulmonary Hypertension. Hypertension (Dallas, Tex. : 1979). 2024 Oct;81(10):2189-2201.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

Drpitor1a

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen