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

Cilomilast  (Synonyms: SB-207499)

Cat. No.: HY-10790 Purity: 99.89%
COA Handling Instructions

Cilomilast (SB-207499) is a potent, selective and orally active inhibitor of Phosphodiesterase 4 (PDE4), with IC50s of ~100 and 120 nM for LPDE4 and HPDE4, respectively. Cilomilast shows selectivity for PDE4 over PDE1, PDE2, PDE3 and PDE5 (IC50=74, 65, >100, and 83 µM, respectively). Cilomilast has anti-inflammatory and immunomodulatory effects and can be used for thr research of asthma and chronic obstructive pulmonary disease (COPD).

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

Cilomilast Chemical Structure

Cilomilast Chemical Structure

CAS No. : 153259-65-5

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10 mM * 1 mL in DMSO USD 117 In-stock
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10 mg USD 185 In-stock
50 mg USD 607 In-stock
100 mg USD 1069 In-stock
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Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Cilomilast

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Cilomilast (SB-207499) is a potent, selective and orally active inhibitor of Phosphodiesterase 4 (PDE4), with IC50s of ~100 and 120 nM for LPDE4 and HPDE4, respectively. Cilomilast shows selectivity for PDE4 over PDE1, PDE2, PDE3 and PDE5 (IC50=74, 65, >100, and 83 µM, respectively). Cilomilast has anti-inflammatory and immunomodulatory effects and can be used for thr research of asthma and chronic obstructive pulmonary disease (COPD)[1][2][3].

IC50 & Target[1]

LPDE4

~100 nM (IC50)

HPDE4

120 nM (IC50)

In Vitro

Cilomilast (0.1 nM-10 μM; 5 min) inhibits human neutrophil functions[2].
Cilomilast (0.1 nM-10 μM; 5 min) inhibits eosinophil chemiluminescence response[2].
Cilomilast (0.001-100 μM; 30 min) inhibits the synthesis of TNFα in human monocytes and in human whole blood[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo

SB-207499 (1-100 mg/kg; p.o.) significantly inhibits the production of human TNFα in a dose-dependent manner in mice[1].
SB-207499 (0.1-100 mg/kg; oral gavage) reverses reserpine-induced hypothermia in mice, with an ED50 of 2.3 mg/kg[1].
SB-207499 (500 μg/ear; b.i.d. for 6 d) inhibits the chronic oxazolone-induced inflammatory response and intralesional IL-4 concentrations in mice[1].

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

Animal Model: Male Balb/c mice (18-25 g) are injected with human monocytes and LPS[1]
Dosage: 1, 5, 10, 50, 100 mg/kg
Administration: P.o. after the injection of human monocytes and before LPS challenge
Result: Inhibited the production of human TNFα, with an ED50 of 4.9 mg/kg.
Clinical Trial
Molecular Weight

343.42

Appearance

Solid

Formula

C20H25NO4
CAS No.
SMILES

O=C([[email protected]]1CC[[email protected]@](C#N)(CC1)C2=CC=C(OC)C(OC3CCCC3)=C2)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 (291.19 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9119 mL 14.5594 mL 29.1189 mL
5 mM 0.5824 mL 2.9119 mL 5.8238 mL
10 mM 0.2912 mL 1.4559 mL 2.9119 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (7.28 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (7.28 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.28 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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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.

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

Cilomilast153259-65-5SB-207499SB207499SB 207499Phosphodiesterase (PDE)PhosphodiesterasePDE4anti-inflammatoryimmunomodulatoryasthmachronicobstructivepulmonarydiseaseCOPDInhibitorinhibitorinhibit

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