E6005 NEW

Price	$6	$4	$2
Package	1kg	10kg	100kg

Min. Order:	1kg
Supply Ability:	100kg
Update Time:	2025-07-29

Product Details

Product Name: E6005	CAS No.: 947620-48-6
Min. Order: 1kg	Purity: 99%
Supply Ability: 100kg	Release date: 2025/07/29
Lead time: in stock	Packaging: bag/bottle/drum//IBC, as request
Delivery: By sea, by air, by express	Origin: Manufacturer, advantage products
COA, MSDS: Available, contact us for details	Contact: Tina

PRODUCT INFORMATION

Common Name	E6005
CAS Number	947620-48-6	Molecular Weight	472.49300
Density	N/A	Boiling Point	N/A
Molecular Formula	C26H24N4O5	Melting Point	N/A
MSDS	N/A	Flash Point	N/A

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Use of E6005

Lotamilast is a selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 2.8 nM.

Properties
Spectrum

Name	methyl 4-[[3-[6,7-dimethoxy-2-(methylamino)quinazolin-4-yl]phenyl]carbamoyl]benzoate
Synonym	More Synonyms

Description	Lotamilast is a selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 2.8 nM.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE) Research Areas >> Inflammation/Immunology
Target	IC50: 2.8 nM (human PDE4)[1]
In Vitro	Lotamilast potently and selectively inhibits human PDE4 activity with an IC50 of 2.8 nM and suppresses the production of various cytokines from human lymphocytes and monocytes with IC50 values ranging from 0.49 to 3.1 nM[1].
In Vivo	Lotamilast is currently in phase 2 development for patients with mild-to-moderate atopic dermatitis. In mice models, the topical application of Lotamilast produces an immediate antipruritic effect as well as an anti-inflammatory effect with reduced expression of cytokines/adhesion molecules. On the basis of these observed effects, topical RVT-501 ameliorates the appearance of atopic dermatitis-like skin lesions in two types of AD models, hapten- and mite-elicited models, exhibiting inhibitory effects comparable to that of tacrolimus[1]. A single topical application of Lotamilast significantly inhibits spontaneous scratching during 1–2 h after application in mice with chronic dermatitis; the inhibition is partial and similar between 0.01% and 0.03%. Topical application of 0.03% Lotamilast to the rostral back significantly inhibits the increased activity of the cutaneous nerve in mice with chronic dermatitis. The cutaneous concentration of cAMP is significantly decreased in mice with chronic dermatitis, and this decrease is reversed by topical Lotamilast application[2].
Kinase Assay	PDE isoenzyme activities are quantified by measuring the formation of [3H]5′-AMP or [[3H]5′-GMP from [[3H]cAMP or [[3H]cGMP using an enzyme isolated from bovine brain (for PDE1), differentiated U-937 cells (for PDE2), human platelets (for PDE3 and PDE5), and U-937 cells (for PDE4). The test compounds (RVT-501), reference compounds, or vehicle (water) is added to a reaction buffer. The reaction is initialized by addition of the enzyme, and the mixture is incubated for 60 minutes at 22°C. After incubation, the reaction is stopped by heating the plate to 60°C for 3 minutes, after which time scintillation proximity assay beads are added. After 20 minutes of shaking at 22°C, the amount of [[3H]5′-AMP or [[3H]5′-GMP is quantified with a scintillation counters[1].
Animal Admin	Mice: Lotamilast is applied to the hair-clipped rostral back. Observation of hind-paw scratching and electrophysiological recording of the cutaneous nerve branch are conducted. The effects of topical application of E6005 are evaluated 1 h after application, because topical application of the vehicle elicited hind-paw scratching for 40 min. The cutaneous concentration of cAMP is measured by enzyme immunoassay[2].
References	[1]. Ishii N, et al. Antipruritic effect of the topical phosphodiesterase 4 inhibitor E6005 ameliorates skin lesions in a mouse atopic dermatitis model. J Pharmacol Exp Ther. 2013 Jul;346(1):105-12. [2]. Andoh T, et al. Topical E6005, a novel phosphodiesterase 4 inhibitor, attenuates spontaneous itch-related responses in mice with chronic atopy-like dermatitis. Exp Dermatol. 2014 May;23(5):359-61.

Molecular Formula	C26H24N4O5
Molecular Weight	472.49300
Exact Mass	472.17500
PSA	114.90000
LogP	3.88950

unii-to043kkb9c

e6005

RVT-501

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