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

Cilomilast (Synonyms: SB-207499)

Cat. No.: HY-10790 Purity: 99.11%
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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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 106 In-stock
Estimated Time of Arrival: December 31
5 mg USD 96 In-stock
Estimated Time of Arrival: December 31
10 mg USD 168 In-stock
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50 mg USD 552 In-stock
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100 mg USD 972 In-stock
Estimated Time of Arrival: December 31
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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

Formula

C₂₀H₂₅NO₄

CAS No.

153259-65-5

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 provided by MCE.
References
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Keywords:

CilomilastSB-207499SB207499SB 207499Phosphodiesterase (PDE)PhosphodiesterasePDE4anti-inflammatoryimmunomodulatoryasthmachronicobstructivepulmonarydiseaseCOPDInhibitorinhibitorinhibit

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