Cilomilast (SB207499; Ariflo)

Alias: Cilomilast; SB 207499; SB207499; Ariflo; SB-207499;
Cat No.:V0779 Purity: ≥98%
Cilomilast (also known asSB-207,499; SB207499; trade name Ariflo)is a novel, potent andorally bioactive phosphodiesterase 4/PDE4 inhibitorwith potential anti-inflammatory and immunomodulatory activity.
Cilomilast (SB207499; Ariflo) Chemical Structure CAS No.: 153259-65-5
Product category: PDE
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Cilomilast (also known as SB-207,499; SB207499; trade name Ariflo) is a novel, potent and orally bioactive phosphodiesterase 4/PDE4 inhibitor with potential anti-inflammatory and immunomodulatory activity. It inhibits PDE4 with an IC50 of ~110 nM, it has anti-inflammatory activity and low central nervous system activity. It has the potential to be used for the treatment of asthma and chronic obstructive obstructive pulmonary (COPD).

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Human neutrophil functions are inhibited by cipolast (0.1 nM–10 μM; 5 min)[2]. A 5-minute exposure to cipomalost (0.1 nM–10 μM) inhibits the eosinophil chemiluminescence response[2]. Cilomilast (0.001-100 μM; 30 min) prevents human monocytes and human whole blood from synthesizing TNFα[2].
ln Vivo
In mice, SB-207499 (1-100 mg/kg; po) substantially and dose-dependently suppresses human TNFα production[1]. With an ED50 of 2.3 mg/kg, SB-207499 (0.1-100 mg/kg; oral gavage) restores reserpine-induced hypothermia in mice[1]. In mice, intralesional IL-4 concentrations and the chronic oxazolone-induced inflammatory response are inhibited by SB-207499 (500 μg/ear; bid for 6 d)[1].
Animal Protocol
Animal/Disease Models: Male balb/c (Bagg ALBino) mouse (18-25 g) are injected with human monocytes and LPS[1]
Doses: 1, 5, 10, 50, 100 mg/kg
Route of Administration: Po after the injection of human monocytes and before LPS challenge
Experimental Results: Inhibited the production of human TNFα, with an ED50 of 4.9 mg/kg.
References
[1]. Griswold DE, et, al. SB 207499 (Ariflo), a second generation phosphodiesterase 4 inhibitor, reduces tumor necrosis factor alpha and interleukin-4 production in vivo. J Pharmacol Exp Ther. 1998 Nov;287(2):705-11.
[2]. Hatzelmann A, et, al. Anti-inflammatory and immunomodulatory potential of the novel PDE4 inhibitor roflumilast in vitro. J Pharmacol Exp Ther. 2001 Apr;297(1):267-79.
[3]. Barnette MS, et, al. SB 207499 (Ariflo), a potent and selective second-generation phosphodiesterase 4 inhibitor: in vitro anti-inflammatory actions. J Pharmacol Exp Ther. 1998 Jan;284(1):420-6.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C20H25NO4
Molecular Weight
343.42
CAS #
153259-65-5
SMILES
O=C([C@H]1CC[C@](C2=CC=C(OC)C(OC3CCCC3)=C2)(C#N)CC1)O
InChi Key
CFBUZOUXXHZCFB-LDTOLXSISA-N
InChi Code
InChI=1S/C20H25NO4/c1-24-17-7-6-15(12-18(17)25-16-4-2-3-5-16)20(13-21)10-8-14(9-11-20)19(22)23/h6-7,12,14,16H,2-5,8-11H2,1H3,(H,22,23)/t14-,20+
Chemical Name
cis-4-Cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]cyclohexanecarboxylic acid
Synonyms
Cilomilast; SB 207499; SB207499; Ariflo; SB-207499;
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 69 mg/mL (200.9 mM)
Water:<1 mg/mL
Ethanol: 50 mg/mL (145.6 mM)
Solubility (In Vivo)
5% DMSO+95% Corn oil:30 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
  • Cilomilast

    Inhibition of human TNFα by orally administered SB 207499 (Cilomilast)(A) or R-rolipram (B).J Pharmacol Exp Ther.1998 Nov;287(2):705-11.
  • Cilomilast

    Reversal of reserpine-induced hypothermia by R-rolipram (○) or SB 207499 (•).J Pharmacol Exp Ther.1998 Nov;287(2):705-11.
  • Cilomilast

    Pharmacokinetic/pharmacodynamic relationship for SB 207499.J Pharmacol Exp Ther.1998 Nov;287(2):705-11.
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