2231329-25-0
Chemical Structure
Morcamilast
Synonym(s): ME3183; PDE4-IN-14
- CAS No.: 2231329-25-0
- Formula:C19H20F2N4O3S
- Molecular Weight:422.45
InChIKey: FJBDQIRRDKSQTK-UHFFFAOYSA-N
SMILES: FC(F)(C(C)(C)O)OC1=C(N=C(O2)N3CC4CC(C3)N4)C2=C(C=C1)C5=NC=CS5
Biological Activity: Morcamilast (ME3183) is a potent, orally active, selective phosphodiesterase 4 (PDE4) inhibitor, with IC50 values of 1.28 nM, 2.33 nM and 1.63 nM against human PDE4A1A, PDE4B1 and PDE4D2, respectively. Morcamilast inhibits the production of TNF-α, IL-12/23p40, IL-23, IL-17A, IL-4, IL-5 and IL-13 in human PBMCs and T cells, and alleviates chronic Oxazolone (HY-126360)-induced dermatitis, Substance P (HY-P0201)-induced pruritus, Imiquimod (HY-B0180)-induced psoriasis-like dermatitis and LPS (HY-D1056)-induced arthritis. Morcamilast is used for the research of psoriasis, atopic dermatitis, psoriatic arthritis and other inflammatory and immune-related diseases[1][2][3][4][5].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Morcamilast | 98.27% | Morcamilast (ME3183) is a potent, orally active, selective phosphodiesterase 4 (PDE4) inhibitor, with IC50 values of 1.28 nM, 2.33 nM and 1.63 nM against human PDE4A1A, PDE4B1 and PDE4D2, respectively. Morcamilast inhibits the production of TNF-α, IL-12/23p40, IL-23, IL-17A, IL-4, IL-5 and IL-13 in human PBMCs and T cells, and alleviates chronic Oxazolone (HY-126360)-induced dermatitis, Substance P (HY-P0201)-induced pruritus, Imiquimod (HY-B0180)-induced psoriasis-like dermatitis and LPS (HY-D1056)-induced arthritis. Morcamilast is used for the research of psoriasis, atopic dermatitis, psoriatic arthritis and other inflammatory and immune-related diseases. | ||||||||||||||||||||
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References
- [1]. Kato S, et al. Safety, Tolerability, and Pharmacokinetics of a Novel Oral Phosphodiesterase 4 Inhibitor, ME3183: First-in-Human Phase 1 Study. Clinical pharmacology in drug development. 2024 Apr;13(4):341-348. [Content Brief]
- [2]. Kaji C, et al. Inhibitory effects of ME3183, a novel phosphodiesterase-4 inhibitor, on stimulants-induced production of proinflammatory cytokines and chemokines in whole blood cell cultures of patients with plaque psoriasis. Journal of the American Academy of Dermatology. 2022;87(3 Suppl):AB72.
- [3]. Okura I, et al. ME3183, a novel phosphodiesterase-4 (PDE4) inhibitor, showed potent suppressive effects on pathogenic cytokine expression in cultures of peripheral blood mononuclear cells from psoriasis patients and on psoriatic features in mouse models. Journal of Investigative Dermatology. 2022;142(8 Suppl):S98. Abstract 573.
- [4]. Kubota-Ishida N, et al. ME3183, a novel phosphodiesterase-4 inhibitor, exhibits potent anti-inflammatory effects and is well tolerated in a non-clinical study. European journal of pharmacology. 2024 Jan 05;962:176202. [Content Brief]
- [5]. Kumura K, et al. Crystal of benzoxazole derivative. CA3104829A1. Canadian Intellectual Property Office. 2020-01-02.
