CHF-6001 - CAS 1239278-59-1
Catalog number: 1239278-59-1
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
Molecular Weight:
Phosphodiesterase (PDE)
This active molecular is a Type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor originated by Chiesi Farmaceutici with IC50 value of 0.026 ± 0.006 nM. CHF6001 inhibited PDE4 isoforms A to D with equal potency, showed an elevated ratio of high-affinity rolipram binding site versus low-affinity rolipram binding site and displayed >20,000-fold selectivity versus PDE4 compared with a panel of PDEs. In May 2016, Chiesi completed a phase I trial in Chronic Obstructive Pulmonary Disease (In volunteers) in United Kingdom (Inhalation). In Oct 2016, Phase-II clinical trials in Chronic obstructive pulmonary disease (Adjunctive treatment) in Hungary (Inhalation) was on-going.
CHF-6001; CHF 6001; CHF6001. UNII-0984EU6E2F; 0984EU6E2F; CHEMBL3113974; SCHEMBL12096092; CHF6001; VCFBPAOSTLMYIV-SANMLTNESA-N;[(1S)-1-[3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl]-2-(3,5-dichloro-1-oxidopyridin-1-ium-4-yl)ethyl] 3-(cyclopropylmethoxy)-4-(methanesulfonamido)benzoate
Soluble in DMSO
-20°C Freezer
Allergic asthma; Chronic obstructive pulmonary disease
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Canonical SMILES:
Current Developer:
Originator: Chiesi Farmaceutici
1.CHF6001 II: a novel phosphodiesterase 4 inhibitor, suitable for topical pulmonary administration--in vivo preclinical pharmacology profile defines a potent anti-inflammatory compound with a wide therapeutic window.
Villetti G;Carnini C;Battipaglia L;Preynat L;Bolzoni PT;Bassani F;Caruso P;Bergamaschi M;Pisano AR;Puviani V;Stellari FF;Cenacchi V;Volta R;Bertacche V;Mileo V;Bagnacani V;Moretti E;Puccini P;Catinella S;Facchinetti F;Sala A;Civelli M J Pharmacol Exp Ther. 2015 Mar;352(3):568-78. doi: 10.1124/jpet.114.220558. Epub 2015 Jan 9.
CHF6001 [(S)-3,5-dichloro-4-(2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)-2-(3-(cyclopropylmethoxy)-4-(methylsulfonamido)benzoyloxy)ethyl)pyridine 1-oxide] is a novel phosphodiesterase 4 (PDE4) inhibitor designed for use in pulmonary diseases by inhaled administration. Intratracheal administration of CHF6001 to ovalbumin-sensitized Brown-Norway rats suppressed the antigen-induced decline of lung functions (ED50 = 0.1 µmol/kg) and antigen-induced eosinophilia (ED50 = 0.03 µmol/kg) when administered (0.09 μmol/kg) up to 24 hours before antigen challenge, in agreement with CHF6001-sustained lung concentrations up to 72 hours after intratracheal treatment (mean residence time 26 hours). Intranasal, once daily administration of CHF6001 inhibited neutrophil infiltration observed after 11 days of tobacco smoke exposure in mice, both upon prophylactic (0.15-0.45 µmol/kg per day) or interventional (0.045-0.45 µmol/kg per day) treatment. CHF6001 was ineffective in reversing ketamine/xylazine-induced anesthesia (a surrogate of emesis in rat) up to 5 µmol/kg administered intratracheally, a dose 50- to 150-fold higher than anti-inflammatory ED50 observed in rats. When given topically to ferrets, no emesis and nausea were evident up to 10 to 20 µmol/kg, respectively, whereas the PDE4 inhibitor GSK-256066 (6-[3-(dimethylcarbamoyl)phenyl]sulfonyl-4-(3-methoxyanilino)-8-methylquinoline-3-carboxamide) induced nausea at 1 µmol/kg intratracheally.
2.CHF6001 I: a novel highly potent and selective phosphodiesterase 4 inhibitor with robust anti-inflammatory activity and suitable for topical pulmonary administration.
Moretto N;Caruso P;Bosco R;Marchini G;Pastore F;Armani E;Amari G;Rizzi A;Ghidini E;De Fanti R;Capaldi C;Carzaniga L;Hirsch E;Buccellati C;Sala A;Carnini C;Patacchini R;Delcanale M;Civelli M;Villetti G;Facchinetti F J Pharmacol Exp Ther. 2015 Mar;352(3):559-67. doi: 10.1124/jpet.114.220541. Epub 2015 Jan 9.
This study examined the pharmacologic characterization of CHF6001 [(S)-3,5-dichloro-4-(2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)-2-(3-(cyclopropylmethoxy)-4-(methylsulfonamido)benzoyloxy)ethyl)pyridine 1-oxide], a novel phosphodiesterase (PDE)4 inhibitor designed for treating pulmonary inflammatory diseases via inhaled administration. CHF6001 was 7- and 923-fold more potent than roflumilast and cilomilast, respectively, in inhibiting PDE4 enzymatic activity (IC50 = 0.026 ± 0.006 nM). CHF6001 inhibited PDE4 isoforms A-D with equal potency, showed an elevated ratio of high-affinity rolipram binding site versus low-affinity rolipram binding site (i.e., >40) and displayed >20,000-fold selectivity versus PDE4 compared with a panel of PDEs. CHF6001 effectively inhibited (subnanomolar IC50 values) the release of tumor necrosis factor-α from human peripheral blood mononuclear cells, human acute monocytic leukemia cell line macrophages (THP-1), and rodent macrophages (RAW264.7 and NR8383). Moreover, CHF6001 potently inhibited the activation of oxidative burst in neutrophils and eosinophils, neutrophil chemotaxis, and the release of interferon-γ from CD4(+) T cells. In all these functional assays, CHF6001 was more potent than previously described PDE4 inhibitors, including roflumilast, UK-500,001 [2-(3,4-difluorophenoxy)-5-fluoro-N-((1S,4S)-4-(2-hydroxy-5-methylbenzamido)cyclohexyl)nicotinamide], and cilomilast, and it was comparable to GSK256066 [6-((3-(dimethylcarbamoyl)phenyl)sulfonyl)-4-((3-methoxyphenyl)amino)-8-methylquinoline-3-carboxamide].
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Phosphodiesterase (PDE) Products

CAS 74150-27-9 Pimobendan

(CAS: 74150-27-9)

Pimobendan is both a calcium sensitizer and a selective inhibitor of phosphodiesterase III (PDE3) with positive inotropic and vasodilator effects.

CAS 794568-92-6 BAY 73-6691

BAY 73-6691
(CAS: 794568-92-6)

BAY 73-6691 is a phosphodiesterase inhibitor selective for the PDE9A subtype under the development of Bayer. It selectively inhibits human PDE9 with IC50 value ...

CAS 3321-06-0 Denaverine hydrochloride

Denaverine hydrochloride
(CAS: 3321-06-0)

Denaverine hydrochloride is a phosphodiesterase inhibitor.Denaverine hydrochloride is applied in relaxation and delatation of birth canal in animals and spasms ...

BRL 50481
(CAS: 433695-36-4)

BRL 50481 is a potent, selective substrate-competitive inhibitor of phosphodiesterase (PDE) 7 (Ki = 180 nM).

CAS 1305116-67-9 PF 04671536 hydrochloride

PF 04671536 hydrochloride
(CAS: 1305116-67-9)

PF 04671536 is a highly potent and selective inhibitor of phosphodiesterase 8B (PDE8B) phosphodiesterase 8A (PDE8A) (IC50= 1.3 and 1.9 nM, respectively), with s...

CAS 1160521-50-5 PDE1-IN-1

(CAS: 1160521-50-5)

PDE1-IN-1 is a potent PDE1 inhibitor and neuroprotective agent.

CAS 68550-75-4 Cilostamide

(CAS: 68550-75-4)

Cilostamide is a selective and specific inhibitor of type III phosphodiesterase (PDE3). It shows moderate selectivity for PDE3A isozyme and PDE3B. It increases ...

CAS 268203-93-6 Udenafil

(CAS: 268203-93-6)

Udenafil is an oral PDE5 inhibitor. Udenafil significantly increased cAMP and cGMP levels and were more highly distributed in the prostate than plasma. The T/P ...

Quick Inquiry

Verification code

Featured Items