| Identification | Back Directory | [Name]
CHF6001 | [CAS]
1239278-59-1 | [Synonyms]
CHF6001
Tanimilast
CHF-6001 1239278-59-1
Benzoic acid, 3-(cyclopropylmethoxy)-4-[(methylsulfonyl)amino]-, (1S)-1-[3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl]-2-(3,5-dichloro-1-oxido-4-pyridinyl)ethyl ester | [Molecular Formula]
C30H30Cl2F2N2O8S | [MDL Number]
MFCD28502112 | [MOL File]
1239278-59-1.mol | [Molecular Weight]
687.54 |
| Chemical Properties | Back Directory | [Boiling point ]
811.5±75.0 °C(Predicted) | [density ]
1.52±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
7.25±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Tanimilast (CHF-6001) is an orally active and selective phosphodiesterase 4 inhibitor(IC50=0.026 ± 0.006 nM) with robust anti-inflammatory activity and suitable for topical pulmonary administration. Tanimilast increases cellular cAMP levels, and inhibits NF-κB signaling pathway. Tanimilast is used for the research of obstructive lung diseases[1][2]. | [in vivo]
Tanimilast (100-600 μg/kg, dry powder inhalation, single dose) ameliorates LPS (HY-D1056)-induced acute pulmonary inflammation in mouse models[3]. | Animal Model: | LPS (HY-D1056)-induced acute pulmonary inflammation in mouse models[3] | | Dosage: | 100-600 μg/kg | | Administration: | dry powder inhalation, single dose | | Result: | Reduced the number of white blood cells (WBC) and neutrophils in bronchoalveolar lavage fluid (BALF).
Reduced the concentrations of proinflammatory cytokines, such as TNF-α, G-CSF, IL-1β, and RANTES in BALF.
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| [IC 50]
PDE4: 0.026 nM (IC50) | [References]
[1] Moretto N, et al., CHF6001 I: a novel highly potent and selective phosphodiesterase 4 inhibitor with robust anti-inflammatory activity and suitable for topical pulmonary administration. J Pharmacol Exp Ther. 2015 Mar;352(3):559-67. DOI:10.1124/jpet.114.220541
[2] Gianello V, et al., The PDE4 inhibitor CHF6001 modulates pro-inflammatory cytokines, chemokines and Th1- and Th17-polarizing cytokines in human dendritic cells. Biochem Pharmacol. 2019 May;163:371-380. DOI:10.1016/j.bcp.2019.03.006
[3] Stellari FF, et al., CHF6001 Inhibits NF-κB Activation and Neutrophilic Recruitment in LPS-Induced Lung Inflammation in Mice. Front Pharmacol. 2019 Nov 12;10:1337. DOI:10.3389/fphar.2019.01337 |
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| Company Name: |
BOC Sciences
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| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
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