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Cilomilast PDE inhibitor

Name: Cilomilast
Brand: Selleck Chemicals
SKU: S1455
Availability: InStock
Rating: 5 (8 reviews)

Cat.No.S1455

Cilomomilast (SB-207499) is a potent PDE4 inhibitor with IC50 of about 110 nM, has anti-inflammatory activity and low central nervous system activity. Phase 3.

Chemical Structure

Molecular Weight: 343.42

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.94%

99.94

Related Targets	P450 (e.g. CYP17) Dehydrogenase phosphatase PPAR HSP (HSP90) Vitamin Transferase Carbohydrate Metabolism Mitochondrial Metabolism Casein Kinase Serine/threonin kinase Lipoxygenase Phospholipase (e.g. PLA) Retinoid Receptor DPP ACE Peroxidases Fatty Acid Synthase FXR HMG-CoA Reductase Carbonic Anhydrase Lipase Decarboxylase DHFR IDO/TDO Hydroxylase PCSK9 OXPHOS ROR Acyltransferase
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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Activity Description
Sf9 cells	Function assay	Inhibition of human Phosphodiesterase 4A isoform using construct representing the common region of spliced variants expressed as GST-fusion proteins in Sf9 cells, IC50=0.038 μM
sf21 cells	Function assay	Inhibition of human full length PDE4A4 expressed in baculovirus infected sf21 cells, IC50=0.062 μM
human peripheral blood mononuclear cells	Function assay	Inhibition of TNF-alpha release from human peripheral blood mononuclear cells, IC50=3.467 μM
U937 cells	Function assay	Arbitary maximal response for cAMP elevation from baseline level was evaluated in Human U-937 cells, EC50=3.63 μM
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	343.42	Formula	C₂₀H₂₅NO₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	153259-65-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	SB-207499			Smiles	COC1=C(C=C(C=C1)C2(CCC(CC2)C(=O)O)C#N)OC3CCCC3

Solubility

In vitro
Batch:

DMSO : 69 mg/mL ( (200.92 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 50 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.45mg/ml (10.05mM)	Taking the 1 mL working solution as an example, add 50 μL of 69 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.49mg/ml (1.43mM)	Taking the 1 mL working solution as an example, add 50 μL of 9.8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Features	Cilomilast has been used to treat chronic obstructive pulmonary disease (COPD) for many years.
Targets/IC₅₀/Ki	LPDE4 ^[1] (Cell-free assay) 100 nM HPDE4 ^[1] (Cell-free assay) 120 nM
In vitro	Cilomilast produces a concentration-dependent increase in cAMP content in U937 cells. This compound produces a concentration-dependent increase in cAMP content in U937 cells. ^[2] In isolated human monocytes, it and (R)-rolipram are equipotent at suppressing LPS-induced TNF-α formation with -log (IC50) of 7.0 and 7.2, respectively. Both this compound and (R)-rolipram produces a modest prevention of fMLP-induced degranulation of human neutrophils. It and (R)-rolipram are equipotent at suppressing neutrophil activation with -log (IC50) of 7.1 and 6.4, respectively. ^[2] This chemical significantly decreases the expression of TNF-α in the cornea and IL-1α, IL-1β, and TNF-α in the conjunctivaas compared to vehicle control. Its treatment markedly decreases the presence of CD11b+ antigen-presenting cells in the central and peripheral cornea, and leads to decreased conjunctival expression of cytokines IL-6, IL-23, and IL-17. Moreover, it decreases the expression of IL-17 and IL-23 in the draining lymph nodes. ^[3] It reduces TLR4 expression, IL-8 release and neutrophil chemotactic activity as well as it increased IP-10 release and lymphocyte chemotactic activity. ^[4]
In vivo	Cilomilast inhibits human TNFα production with oral ED50 of 4.9 mg/kg. In contrast to their equipotent activity against TNFα production, this compound (ED50 = 2.3 mg/kg, p.o.) is 10-fold less potent than R-rolipram (ED50 = 0.23 mg/kg, p.o.) in reversing reserpine-induced hypothermia, a model of antidepressant activity. ^[1] In time course studies, this chemical (30 mg/kg, p.o.) suppresses TNFα production for at least 10 hour. The ability of this compound to modulate interleukin-4 productionin vivo is assessed in a chronic oxazolone-induced contact sensitivity model in Balb/c mice. Topical administration of this chemical (1000 μg) inhibits intralesional concentrations of interleukin-4. ^[1] Orally administered cilomilast dose-dependently inhibits production of interleukin-4, TNF-α, and cysteinyl leukotrienes, as well as leukocyte infiltration in bronchoalveolar lavage fluid from the airways of ovalbumin-sensitized Brown Norway rats ^[5].
References	https://pubmed.ncbi.nlm.nih.gov/9808700/ https://pubmed.ncbi.nlm.nih.gov/9435206/ https://pubmed.ncbi.nlm.nih.gov/22577075/ https://pubmed.ncbi.nlm.nih.gov/21382614/ https://pubmed.ncbi.nlm.nih.gov/21315169/

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