2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. Orismilast

Orismilast  (Synonyms: LEO-32731)

Cat. No.: HY-117960 Purity: 99.37%
COA Handling Instructions

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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.

For research use only. We do not sell to patients.

Orismilast Chemical Structure

Orismilast Chemical Structure

CAS No. : 1353546-86-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 550 In-stock
Solution
10 mM * 1 mL in DMSO USD 550 In-stock
Solid
1 mg USD 200 In-stock
5 mg USD 500 In-stock
10 mg USD 850 In-stock
25 mg USD 1650 In-stock
50 mg USD 2600 In-stock
100 mg USD 4200 In-stock
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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Orismilast Related Antibodies

Top Publications Citing Use of Products

View All Phosphodiesterase (PDE) Isoform Specific Products:

View All Isoforms
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

  • Biological Activity

  • Purity & Documentation

  • References

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Description

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[1][2].

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)

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.

Orismilast Related Antibodies

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
Molecular Weight

510.29

Formula

C19H15Cl2F2NO7S
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9597 mL 9.7983 mL 19.5967 mL
5 mM 0.3919 mL 1.9597 mL 3.9193 mL
View the 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.37%

COA (254 KB) HNMR (288 KB) LCMS (268 KB)

Handling Instructions (2659 KB)
References

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. 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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Orismilast1353546-86-7LEO-32731LEO32731LEO 32731Phosphodiesterase (PDE)CISDincluding psoriasisADHSInhibitorinhibitorinhibit

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