Art. -Nr.: HY-148808

Zelasudil

(Synonyms: RXC007)

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Based on 1 Customer Validation

Zelasudil (RXC007) is an orally active, highly selective small molecule Rho-associated coiled-coil containing protein kinase 2 (ROCK2) inhibitor with anti-fibrotic efficacy. Zelasudil elicits positive immunomodulatory effects in metastatic pancreatic tumors with increase of CD8+ and CD4+ T cell infiltrate into the tumor cortex and reduction in immunosuppressive FOXP3+ regulatory T cells at the tumor border. Zelasudil is promising for research of pancreatic ductal adenocarcinoma.

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Reinheit: 99.48%
CAS. Nr.: 2365193-22-0
Formel: C₂₂H₂₁F₂N₇O
Molecular Weight:437.45

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Zelasudil Chemical Structure

CAS. Nr.: 2365193-22-0

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Biologische Aktivität
- Beschreibung
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle ROCK Isoform-spezifische Produkte anzeigen :

In Vivo

Zelasudil (5-100 mg/kg, p.o., a single dose for 21 days) reduces fibrosis and collagen deposition, suppresses the expression of a number of genes strongly associated with fibrosis in a murine Bleomycin (HY-108345)-induced lung fibrosis model^[4].

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

Animal Model:

Bleomycin (HY-108345)-induced lung fibrosis mouse model^[4]
Dosage:

5-100 mg/kg
Administration:

p.o., a single dose for 21 days
Result:

Significantly reduced fibrosis and collagen deposition and picrosirius red in the lung.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2365193-22-0
Appearance Solid
Molecular Weight 437.45
Formel C₂₂H₂₁F₂N₇O
Color Off-white to light brown
SMILES

O=C(C1=CC=C(C2=NN(C)C(NC3=CC=C4NN=CC4=C3C5CC5)=N2)C=C1)NCC(F)F
Synonyms

RXC007
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (228.60 mM; Need ultrasonic; 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

2.2860 mL

11.4299 mL

22.8598 mL

5 mM

0.4572 mL

2.2860 mL

4.5720 mL

10 mM

0.2286 mL

1.1430 mL

2.2860 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. 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)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.5 mg/mL (5.71 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (5.71 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 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]. Lee E, et al. Selective ROCK2 inhibition for treatment of edema and associated conditions: World Intellectual Property Organization, WO2022169946. 2022-08-11.

[2]. WHO Drug Information-World Health Organization (WHO).

[3]. Pajic M, et al. Combining zelasudil, a small molecule ROCK2 inhibitor, with chemotherapy or immunotherapy improves response in preclinical models of pancreatic cancer[J]. Cancer Research, 2024, 84(6_Supplement): 720-720.

[4]. Gambardella A, et al. Effects of RXC007, a highly potent and selective ROCK2 inhibitor, in ex-vivo and in vivo models of pulmonary fibrosis[C]//European Respiratory Journal. 442 GLOSSOP RD, SHEFFIELD S10 2PX, ENGLAND: EUROPEAN RESPIRATORY SOC JOURNALS LTD, 2022, 60.

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

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	2.2860 mL	11.4299 mL	22.8598 mL	57.1494 mL
	5 mM	0.4572 mL	2.2860 mL	4.5720 mL	11.4299 mL
	10 mM	0.2286 mL	1.1430 mL	2.2860 mL	5.7149 mL
	15 mM	0.1524 mL	0.7620 mL	1.5240 mL	3.8100 mL
	20 mM	0.1143 mL	0.5715 mL	1.1430 mL	2.8575 mL
	25 mM	0.0914 mL	0.4572 mL	0.9144 mL	2.2860 mL
	30 mM	0.0762 mL	0.3810 mL	0.7620 mL	1.9050 mL
	40 mM	0.0571 mL	0.2857 mL	0.5715 mL	1.4287 mL
	50 mM	0.0457 mL	0.2286 mL	0.4572 mL	1.1430 mL
	60 mM	0.0381 mL	0.1905 mL	0.3810 mL	0.9525 mL
	80 mM	0.0286 mL	0.1429 mL	0.2857 mL	0.7144 mL
	100 mM	0.0229 mL	0.1143 mL	0.2286 mL	0.5715 mL

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Zelasudil

Reprogramming Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Transcription Factor-Targeted Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Extracellular Vesicles (EVs) Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Stem Cell Signaling Compound Library

TGF-beta/Smad Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Alle ROCK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Zelasudil

Reprogramming Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Transcription Factor-Targeted Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Extracellular Vesicles (EVs) Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Stem Cell Signaling Compound Library

TGF-beta/Smad Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Alle ROCK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Zelasudil Related Classifications

HY-148808 Related Classifications