Art. -Nr.: HY-117960

Orismilast

(Synonyms: LEO-32731)

Kundenbewertung

Based on 1 Customer Validation

Orismilast (LEO-32731) is an orally active and selective PDE4 inhibitor used for the research of inflammatory diseases. Orismilast demonstrates potent inhibition of PDE4B and PDE4D subtype splice variants.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.88%
CAS. Nr.: 1353546-86-7
Formel: C₁₉H₁₅Cl₂F₂NO₇S
Molecular Weight:510.29

Speicherung:

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

Orismilast Chemical Structure

CAS. Nr.: 1353546-86-7

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Verfügbarkeit

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[2].

PDE4B3

3 nM (IC₅₀)

PDE4D7

3 nM (IC₅₀)

PDE4D5

3 nM (IC₅₀)

PDE4B2

6 nM (IC₅₀)

PDE4D3

8 nM (IC₅₀)

PDE4D4

8 nM (IC₅₀)

PDE4D1

9 nM (IC₅₀)

PDE4D2

9 nM (IC₅₀)

PDE4A4

11 nM (IC₅₀)

PDE4B1

16 nM (IC₅₀)

PDE4A1

16 nM (IC₅₀)

PDE4A10

52 nM (IC₅₀)

PDE4C2

104 nM (IC₅₀)

Alle Phosphodiesterase (PDE) Isoform-spezifische Produkte anzeigen :

In Vitro

Orismilast inhibits tumour necrosis factor α (TNFα), and the secretion of T-helper (Th)1 (TNFα and IFNγ), Th17 (IL-22 and IL-23), and Th2 (IL-4, IL-5, and IL-13) related cytokines in PBMC^[2].

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

Cell Viability Assay^[2].

Cell Line:

PBMC.
Concentration:

0-30 nM.
Incubation Time:

72 h.
Result:

Inhibited pro-inflammatory TNFα release.
Inhibited the secretion of cytokines across all investigated T-helper cell sublineages, with most the profound effect on Th1-cell effector cytokines but also demonstrates potent inhibition on Th17 cells and Th2 cells related cytokines.

In Vivo

Orismilast (10 and 30mg/kg) significantly reduces ear thickness and inflammation markers (p<0.0001, respectively)^[2].

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

Animal Model:

Female BALB/cABomTac mice (sensitized to oxazolone on the right ear with a single application of 10 μl oxazolone (0.8% in acetone) on Day 7)^[2].
Dosage:

10 and 30mg/kg.
Administration:

Orally.
Result:

Both the 10 mg/kg and 30mg/kg doses of oral orismilast resulted in a significant reduction in ear thickness over time (p<0.0001, respectively;) with no impact on bodyweight during the treatment period.

Clinical Trial

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

Chemical Information

CAS. Nr. 1353546-86-7
Appearance Solid
Molecular Weight 510.29
Formel C₁₉H₁₅Cl₂F₂NO₇S
Color White to off-white
SMILES

O=S1(CCC2(OC3=C(C=CC(C(CC4=C(C=[N+](C=C4Cl)[O-])Cl)=O)=C3O2)OC(F)F)CC1)=O
Synonyms

LEO-32731
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 (195.97 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

1.9597 mL

9.7983 mL

19.5967 mL

5 mM

0.3919 mL

1.9597 mL

3.9193 mL

10 mM

0.1960 mL

0.9798 mL

1.9597 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)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 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]. Nielsen,et al.Preparation of benzodioxole or benzodioxepine heterocyclic compounds as phosphodiesterase inhibitors.WO2011160632A1.

[2]. Jonathan I Silverberg, et al. Pharmacology of orismilast, a potent and selective PDE4 inhibitor. J Eur Acad Dermatol Venereol. 2023 Apr;37(4):721-729. [Content Brief]

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	1.9597 mL	9.7983 mL	19.5967 mL	48.9917 mL
	5 mM	0.3919 mL	1.9597 mL	3.9193 mL	9.7983 mL
	10 mM	0.1960 mL	0.9798 mL	1.9597 mL	4.8992 mL
	15 mM	0.1306 mL	0.6532 mL	1.3064 mL	3.2661 mL
	20 mM	0.0980 mL	0.4899 mL	0.9798 mL	2.4496 mL
	25 mM	0.0784 mL	0.3919 mL	0.7839 mL	1.9597 mL
	30 mM	0.0653 mL	0.3266 mL	0.6532 mL	1.6331 mL
	40 mM	0.0490 mL	0.2450 mL	0.4899 mL	1.2248 mL
	50 mM	0.0392 mL	0.1960 mL	0.3919 mL	0.9798 mL
	60 mM	0.0327 mL	0.1633 mL	0.3266 mL	0.8165 mL
	80 mM	0.0245 mL	0.1225 mL	0.2450 mL	0.6124 mL
	100 mM	0.0196 mL	0.0980 mL	0.1960 mL	0.4899 mL

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Orismilast

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

Anti-Alzheimer's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Colorectal Cancer Compound Library

Antidepressant Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Multi-Target 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

Alle Phosphodiesterase (PDE) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Orismilast

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

Anti-Alzheimer's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Colorectal Cancer Compound Library

Antidepressant Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Multi-Target 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

Alle Phosphodiesterase (PDE) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Orismilast Related Classifications

HY-117960 Related Classifications