1239278-59-1|CHF-6001|(S)-3,5-dichloro-4-(2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)-2-((3-(cyclopropylmethoxy)-4-(methylsulfonamido)benzoyl)oxy)ethyl)pyridine 1-oxide|-范德生物科技公司

CHF-6001

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names：
(S)-3,5-dichloro-4-(2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)-2-((3-(cyclopropylmethoxy)-4-(methylsulfonamido)benzoyl)oxy)ethyl)pyridine 1-oxide
CAS号：
1239278-59-1
MDL Number：
MF(分子式)： C30H30Cl2F2N2O8S MW(分子量)： 687.5328
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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FMK13374-100mg	100mg	>98%	¥ 0.00	¥ 0.00		Get quote	- +	¥ 0.00

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中文别名	CHF-6001
英文别名	CHF-6001; CHF 6001; CHF6001; tanimilast; tanimilastum.
CAS号	1239278-59-1
Inchi	InChI=1S/C30H30Cl2F2N2O8S/c1-45(39,40)35-24-8-6-20(11-27(24)41-15-17-2-3-17)29(37)43-26(12-21-22(31)13-36(38)14-23(21)32)19-7-9-25(44-30(33)34)28(10-19)42-16-18-4-5-18/h6-11,13-14,17-18,26,30,35H,2-5,12,15-16H2,1H3/t26-/m0/s1
InchiKey	VCFBPAOSTLMYIV-SANMLTNESA-N
分子式 Formula	C30H30Cl2F2N2O8S
分子量 Molecular Weight	687.5328
溶解度Solubility
性状	Solid powder
储藏条件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

产品说明	CHF-6001(CAS:1239278-59-1):仅限应用于工业或者科学研究过程中非医疗目的，不应用于人类或动物的临床诊断以及治过程疗，该产品非药用，非食用。
Introduction	CHF-6001 is also known as Tanimilast. It is a novel PDE4 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). CHF6001 has the potential to be an effective topical treatment of conditions associated with pulmonary inflammation, including asthma and chronic obstructive pulmonary disease.
Application1
Application2
Application3

警示图
危险性	Warning
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安全声明
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备注

[1]Mulhall AM, Droege CA, Ernst NE, Panos RJ, Zafar MA. Phosphodiesterase 4inhibitors for the treatment of chronic obstructive pulmonary disease: a reviewof current and developing drugs. Expert Opin Investig Drugs. 2015Dec;24(12):1597-61[1]doi: 10.1517/13543784.2015.1094054. Epub 2015 Sep 30. PubMedPMID: 26419847.

[2]Moretto N, Caruso P, Bosco R, Marchini G, Pastore F, Armani E, Amari G, RizziA, 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.CHF6001 I: a novel highly potent and selective phosphodiesterase 4 inhibitor withrobust anti-inflammatory activity and suitable for topical pulmonaryadministration. J Pharmacol Exp Ther. 2015 Mar;352(3):559-67. doi:10.1124/jpet.114.220541. Epub 2015 Jan 9. PubMed PMID: 25576075.

[3] Villetti G, Carnini C, Battipaglia L, Preynat L, Bolzoni PT, Bassani F, CarusoP, Bergamaschi M, Pisano AR, Puviani V, Stellari FF, Cenacchi V, Volta R,Bertacche V, Mileo V, Bagnacani V, Moretti E, Puccini P, Catinella S, FacchinettiF, Sala A, Civelli M. CHF6001 II: a novel phosphodiesterase 4 inhibitor, suitablefor topical pulmonary administration--in vivo preclinical pharmacology profiledefines a potent anti-inflammatory compound with a wide therapeutic window. JPharmacol Exp Ther. 2015 Mar;352(3):568-78. doi: 10.1124/jpet.114.220558. Epub2015 Jan 9. PubMed PMID: 25576073.

[4] Armani E, Amari G, Rizzi A, De Fanti R, Ghidini E, Capaldi C, Carzaniga L,Caruso P, Guala M, Peretto I, La Porta E, Bolzoni PT, Facchinetti F, Carnini C,Moretto N, Patacchini R, Bassani F, Cenacchi V, Volta R, Amadei F, Capacchi S,Delcanale M, Puccini P, Catinella S, Civelli M, Villetti G. Novel class ofbenzoic acid ester derivatives as potent PDE4 inhibitors for inhaledadministration in the treatment of respiratory diseases. J Med Chem. 2014 Feb13;57(3):793-816. doi: 10.1021/jm401549m. Epub 2014 Jan 29. PubMed PMID:24400806.

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