| Identification | Back Directory | [Name]
Difamilast 937782-05-3 | [CAS]
937782-05-3 | [Synonyms]
OPA15406)
Difamilast 937782-05-3
Difamilast
(OPA-15406
Benzamide, N-[[2-[4-(difluoromethoxy)-3-(1-methylethoxy)phenyl]-4-oxazolyl]methyl]-2-ethoxy-
N-[[2-[4-(difluoromethoxy)-3-propan-2-yloxyphenyl]-1,3-oxazol-4-yl]methyl]-2-ethoxybenzamide | [Molecular Formula]
C23H24F2N2O5 | [MDL Number]
MFCD32899865 | [MOL File]
937782-05-3.mol | [Molecular Weight]
446.44 |
| Chemical Properties | Back Directory | [density ]
1.223±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 100 mg/mL (223.99 mM; Need ultrasonic) | [form ]
Solid | [pka]
13.12±0.46(Predicted) | [color ]
White to off-white | [InChI]
InChI=1S/C23H24F2N2O5/c1-4-29-18-8-6-5-7-17(18)21(28)26-12-16-13-30-22(27-16)15-9-10-19(32-23(24)25)20(11-15)31-14(2)3/h5-11,13-14,23H,4,12H2,1-3H3,(H,26,28) | [InChIKey]
VFBILHPIHUPBPZ-UHFFFAOYSA-N | [SMILES]
C(NCC1=COC(C2=CC=C(OC(F)F)C(OC(C)C)=C2)=N1)(=O)C1=CC=CC=C1OCC |
| Hazard Information | Back Directory | [Uses]
Difamilast (OPA-15406) is a topical, selective and nonsteroidal phosphodiesterase-4 (PDE4) inhibitor with particularly efficient inhibition of subtype B (IC50=11.2 nM). Difamilast can be used for the research of mild to moderate atopic dermatitis (AD)[1][2][3]. | [Biological Activity]
Difamilast is a novel atopic dermatitis drug candidate discovered by Otsuka that has phosphodiesterase 4 (PDE4) inhibitory activity. | [in vitro]
Difamilast has particularly efficient inhibition of subtype B (IC50=11.2 nM). It (OPA-15406) improves skin condition in relevant animal models of AD. | [in vivo]
OPA-1540 improves skin condition in relevant animal models of AD[1]. | [IC 50]
PDE4B: 11.2 nM (IC50) | [References]
[1] Hanifin JM, et, al. OPA-15406, a novel, topical, nonsteroidal, selective phosphodiesterase-4 (PDE4) inhibitor, in the treatment of adult and adolescent patients with mild to moderate atopic dermatitis (AD): A phase-II randomized, double-blind, placebo-con DOI:10.1016/j.jaad.2016.04.001
[2] Ahluwalia J, et, al. Phosphodiesterase 4 Inhibitor Therapies for Atopic Dermatitis: Progress and Outlook. Drugs. 2017 Sep;77(13):1389-1397. DOI:10.1007/s40265-017-0784-3
[3] Soeberdt M, et, al. Small molecule drugs for the treatment of pruritus in patients with atopic dermatitis. Eur J Pharmacol. 2020 Aug 15;881:173242. DOI:10.1016/j.ejphar.2020.173242 |
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