WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H561846
CAS#: 937782-05-3
Description: Difamilast is a phosphodiesterase IV inhibitor.
Hodoodo Cat#: H561846
Name: Difamilast
CAS#: 937782-05-3
Chemical Formula: C23H24F2N2O5
Exact Mass: 446.17
Molecular Weight: 446.450
Elemental Analysis: C, 61.88; H, 5.42; F, 8.51; N, 6.27; O, 17.92
Synonym: Difamilast;
IUPAC/Chemical Name: N-({2-[4-(difluoromethoxy)-3-(propan-2-yloxy)phenyl]-1,3- oxazol-4-yl}methyl)-2-ethoxybenzamide
InChi Key: VFBILHPIHUPBPZ-UHFFFAOYSA-N
InChi Code: 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)
SMILES Code: O=C(NCC1=COC(C2=CC=C(OC(F)F)C(OC(C)C)=C2)=N1)C3=CC=CC=C3OCC
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 446.45 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Saeki H, Ito K, Yokota D, Tsubouchi H. Difamilast ointment in adult patients with atopic dermatitis: A phase 3 randomized, double-blind, vehicle-controlled trial. J Am Acad Dermatol. 2022 Mar;86(3):607-614. doi: 10.1016/j.jaad.2021.10.027. Epub 2021 Oct 25. PMID: 34710557.
2: Saeki H, Baba N, Ito K, Yokota D, Tsubouchi H. Difamilast, a selective phosphodiesterase 4 inhibitor, ointment in paediatric patients with atopic dermatitis: a phase III randomized double-blind, vehicle-controlled trial. Br J Dermatol. 2022 Jan;186(1):40-49. doi: 10.1111/bjd.20655. Epub 2021 Nov 1. PMID: 34289086; PMCID: PMC9298328.
3: Freitas E, Torres T. Difamilast for the treatment of atopic dermatitis. J Int Med Res. 2023 Jun;51(6):3000605231169445. doi: 10.1177/03000605231169445. PMID: 37389929; PMCID: PMC10328024.
4: Kleinman E, Laborada J, Metterle L, Eichenfield LF. What's New in Topicals for Atopic Dermatitis? Am J Clin Dermatol. 2022 Sep;23(5):595-603. doi: 10.1007/s40257-022-00712-0. Epub 2022 Sep 1. PMID: 36048410; PMCID: PMC9464760.
5: Saeki H, Imamura T, Yokota D, Tsubouchi H. Difamilast Ointment in Japanese Adult and Pediatric Patients with Atopic Dermatitis: A Phase III, Long-Term, Open-Label Study. Dermatol Ther (Heidelb). 2022 Jul;12(7):1589-1601. doi: 10.1007/s13555-022-00751-9. Epub 2022 Jun 18. PMID: 35716332; PMCID: PMC9276884.
6: Sideris N, Paschou E, Bakirtzi K, Kiritsi D, Papadimitriou I, Tsentemeidou A, Sotiriou E, Vakirlis E. New and Upcoming Topical Treatments for Atopic Dermatitis: A Review of the Literature. J Clin Med. 2022 Aug 24;11(17):4974. doi: 10.3390/jcm11174974. PMID: 36078904; PMCID: PMC9456375.
7: Freitas E, Gooderham M, Torres T. New Topical Therapies in Development for Atopic Dermatitis. Drugs. 2022 Jun;82(8):843-853. doi: 10.1007/s40265-022-01722-2. Epub 2022 May 21. PMID: 35596877.
8: Tsuji G, Hashimoto-Hachiya A, Yumine A, Takemura M, Kido-Nakahara M, Ito T, Yamamura K, Nakahara T. PDE4 inhibition by difamilast regulates filaggrin and loricrin expression via keratinocyte proline-rich protein in human keratinocytes. J Dermatol Sci. 2023 May;110(2):61-68. doi: 10.1016/j.jdermsci.2023.04.007. Epub 2023 Apr 28. PMID: 37156706.
9: Hiyama H, Arichika N, Okada M, Koyama N, Tahara T, Haruta J. Pharmacological Profile of Difamilast, a Novel Selective Phosphodiesterase 4 Inhibitor, for Topical Treatment of Atopic Dermatitis. J Pharmacol Exp Ther. 2023 Jul;386(1):45-55. doi: 10.1124/jpet.123.001609. Epub 2023 Apr 11. PMID: 37041087.
10: Lu LC, Chao CM, Chang SP, Lan SH, Lai CC. Clinical efficacy and safety of topical difamilast in the treatment of patients with atopic dermatitis: a systematic review and meta-analysis of randomized controlled trials. Expert Rev Clin Pharmacol. 2022 Dec;15(12):1471-1478. doi: 10.1080/17512433.2022.2134114. Epub 2022 Oct 11. PMID: 36210241.
11: Saeki H, Baba N, Oshiden K, Abe Y, Tsubouchi H. Phase 2, randomized, double- blind, placebo-controlled, 4-week study to evaluate the safety and efficacy of OPA- 15406 (difamilast), a new topical selective phosphodiesterase type-4 inhibitor, in Japanese pediatric patients aged 2-14 years with atopic dermatitis. J Dermatol. 2020 Jan;47(1):17-24. doi: 10.1111/1346-8138.15137. Epub 2019 Nov 11. PMID: 31713267; PMCID: PMC6972691.
12: Freitas E, Torres T. New molecules for atopic dermatitis treatment beyond biological therapy. Curr Opin Allergy Clin Immunol. 2023 Jun 1;23(3):210-215. doi: 10.1097/ACI.0000000000000910. Epub 2023 Apr 6. PMID: 37185825.
13: Chu DK, Chu AWL, Rayner DG, Guyatt GH, Yepes-Nuñez JJ, Gomez-Escobar L, Pérez-Herrera LC, Díaz Martinez JP, Brignardello-Petersen R, Sadeghirad B, Wong MM, Ceccacci R, Zhao IX, Basmaji J, MacDonald M, Chu X, Islam N, Gao Y, Izcovich A, Asiniwasis RN, Boguniewicz M, De Benedetto A, Capozza K, Chen L, Ellison K, Frazier WT, Greenhawt M, Huynh J, LeBovidge J, Lio PA, Martin SA, O'Brien M, Ong PY, Silverberg JI, Spergel JM, Smith Begolka W, Wang J, Wheeler KE, Gardner DD, Schneider L. Topical treatments for atopic dermatitis (eczema): systematic review and network meta-analysis of randomized trials. J Allergy Clin Immunol. 2023 Sep 5:S0091-6749(23)01113-2. doi: 10.1016/j.jaci.2023.08.030. Epub ahead of print. PMID: 37678572.
