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Piclamilast

Product Name
Piclamilast
CAS No.
144035-83-6
Chemical Name
Piclamilast
Synonyms
RP 73401;RPR 73401;piclamilas;Piclamilast;Piclamilast, 10 mM in DMSO;N-(3,5-Dichloropyrid-4-yl)-3-cyclopentyloxy-4-methoxybenzamide;3-(cyclopentyloxy)-N-(3,5-dichloro-4-pyridyl)-4-methoxybenzamide;3-(Cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-methoxybenzamide;3-(Cyclopentyloxy)-N-(3,5-dichloro-4-pyridinyl)-4-methoxybenzamide;Benzamide,3-(cyclopentyloxy)-N-(3,5-dichloro-4-pyridinyl)-4-methoxy-
CBNumber
CB51328847
Molecular Formula
C18H18Cl2N2O3
Formula Weight
381.25
MOL File
144035-83-6.mol
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Piclamilast Property

Boiling point:
447.8±45.0 °C(Predicted)
Density 
1.370
storage temp. 
2-8°C
solubility 
DMSO: soluble20mg/mL, clear
pka
10.10±0.70(Predicted)
form 
powder
color 
white to beige
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Safety

Hazard Codes 
Xi
Risk Statements 
36/37/38
Safety Statements 
26
WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML0585
Product name
Piclamilast
Purity
≥98% (HPLC)
Packaging
5mg
Price
$112
Updated
2025/07/31
Sigma-Aldrich
Product number
SML0585
Product name
Piclamilast
Purity
≥98% (HPLC)
Packaging
25mg
Price
$434
Updated
2025/07/31
Cayman Chemical
Product number
29170
Product name
Piclamilast
Packaging
1mg
Price
$39
Updated
2024/03/01
Cayman Chemical
Product number
29170
Product name
Piclamilast
Packaging
5mg
Price
$127
Updated
2024/03/01
Cayman Chemical
Product number
29170
Product name
Piclamilast
Packaging
10mg
Price
$233
Updated
2024/03/01
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Piclamilast Chemical Properties,Usage,Production

Uses

Piclamilast is a potent and selective phosphodiesterase-4 (PDE4) inhibitor. Piclamilast may offer therapeutic strategies in respiratory diseases, including asthma and chronic obstructive pulmonary disease. Piclamilast may also provide a treatment option for pre-term infants with bronchopulmonary dysplasia (BPD).

Definition

ChEBI: A monocarboxylic acid amide resulting from the formal condensation of the carboxy group of 3-(cyclopentyloxy)-4-methoxybenzoic acid with the primary amino group of 3,5-dichloropyridin-4-amine.

Biological Activity

Piclamilast is a potent and selective cyclic AMP phosphodiesterase-4 inhibitor th at exhibits equal, high affinity for both the PDE4 high- and low-affinity rolipram binding states (HARBS and LARBS). Recent studies shown th at piclamilast inhibits Trypanosoma brucei PDEB1 (TbrPDEB1) and TbrPDEB2.', 'Piclamilast is also known as N-(3,5-dichloropyrid-4-yl)-3-cyclopentyloxy-4-methoxybenzamide. Piclamilast regulates the cAMP (cyclic adenosine monophosphate) signaling pathway. It increases the retinoid-dependent transactivation and the degradation of retinoic acid receptor α (RARα).

in vivo

Piclamilast (RP 73401, 10 mg/kg, 30 min) alone does not affect the MST of leukemia-bearing animals. Piclamilast combined with ATRA (HY-14649) significantly more effective than ATRA alone in increasing the MST (40 days; interval 34–45 days) of leukemia-bearing animals[3].

Animal Model:SCID mice[3].
Dosage:10 mg/kg (combined with ATRA (HY-14649)).
Administration:Injection daily.
Result:Significantly more effective than ATRA alone in increasing the MST (40 days; interval 34–45 days) of leukemia-bearing animals.

IC 50

PDE4: 16 nM (IC50, in pig aorta); PDE4: 2 nM (IC50, in eosinophil soluble); PDE1: >100 μM (IC50); PDE2: 40 μM (IC50); PDE3: >100 μM (IC50); PDE5: 14 μM (IC50)

storage

Store at RT

Piclamilast Preparation Products And Raw materials

Raw materials

Preparation Products

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Piclamilast Suppliers

Canada 1 China 44 India 1 United Kingdom 1 United States 10 USA 1 Global 58
Toronto Research Chemicals
Tel
--
Fax
--
Email
info@trc-canada.com
Country
Canada
ProdList
6038
Advantage
71

144035-83-6, PiclamilastRelated Search:

3-ISOPROPOXY-4-METHOXY-BENZALDEHYDE 4-Benzylaminopyridine 3-ETHOXY-4-METHOXY-BENZYLAMINE 3-BUTOXY-4-METHOXYBENZAMIDE N1-(4-PYRIDYL)BENZAMIDE 3-CYCLOPENTYLOXY-4-METHOXYBENZALDEHYDE CHEMBRDG-BB 9071037 (3,5-DICHLORO-PYRIDIN-4-YL)METHYLAMINE 3-ISOPROPOXY-BENZALDEHYDE Piclamilast BENZYL-PYRIDIN-4-YL-AMINE DIHYDROCHLORIDE 3-(SEC-BUTOXY)PHENYL]METHANAMINE 3-(CYCLOPENTYLOXY)-4-METHOXYBENZAMIDE 3-(CYCLOPENTYLOXY)BENZALDEHYDE CHEMBRDG-BB 5563263 1-(3-ISOPROPOXYPHENYL)METHANAMINE

  • Benzamide,3-(cyclopentyloxy)-N-(3,5-dichloro-4-pyridinyl)-4-methoxy-
  • RP 73401
  • RPR 73401
  • 3-(cyclopentyloxy)-N-(3,5-dichloro-4-pyridyl)-4-methoxybenzamide
  • 3-(Cyclopentyloxy)-N-(3,5-dichloro-4-pyridinyl)-4-methoxybenzamide
  • N-(3,5-Dichloropyrid-4-yl)-3-cyclopentyloxy-4-methoxybenzamide
  • Piclamilast
  • 3-(Cyclopentyloxy)-N-(3,5-dichloropyridin-4-yl)-4-methoxybenzamide
  • piclamilas
  • inhibit,Phosphodiesterase (PDE),RPR73401,AML,phosphodiesterase,PDE,RAR,RP-73401,Inhibitor,Piclamilast,RP73401,RPR-73401,ATRA,cAMP
  • Piclamilast, 10 mM in DMSO
  • 144035-83-6
  • Aromatics
  • Heterocycles
  • Inhibitors
  • Intermediates & Fine Chemicals
  • Pharmaceuticals