Basic information Safety Supplier Related

Piclamilast

Basic information Safety Supplier Related

Piclamilast Basic information

Product Name:
Piclamilast
Synonyms:
  • 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
CAS:
144035-83-6
MF:
C18H18Cl2N2O3
MW:
381.25
Product Categories:
  • Aromatics
  • Heterocycles
  • Inhibitors
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
Mol File:
144035-83-6.mol
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Piclamilast Chemical Properties

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 Information

Hazard Codes 
Xi
Risk Statements 
36/37/38
Safety Statements 
26
WGK Germany 
3
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Piclamilast Usage And Synthesis

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

PiclamilastSupplier

J & K SCIENTIFIC LTD.
Tel
18210857532; 18210857532
Email
jkinfo@jkchemical.com
ZHIWE CHEMTECH CO LTD
Tel
021-20221225 13917446399
Email
zwchem@163.com
Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070
Email
info@chemlin.com.cn
Shanghai Hekang Biotechnology Co., Ltd.
Tel
18939837085
Email
youchemicals@gmail.com
AN PharmaTech Co Ltd
Tel
86(21)68097365
Email
sales@anpharma.net
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Piclamilast(144035-83-6)Related Product Information