Delgocitinib
- CAS No.
- 1263774-59-9
- Chemical Name:
- Delgocitinib
- Synonyms
- JTE052;JTE-052;LEO124249;LEO 124249;Delgocitinib;Delgocitinib(JTE-052);Corectim（Delgocitinib）;Delgocitinib (LEO124249;JTE052,Inhibitor,Janus kinase,inhibit,JAK,Delgocitinib,JTE 052;1,6-Diazaspiro[3.4]octane-1-propanenitrile, 3-methyl-β-oxo-6-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-, (3S,4R)-
- CBNumber:
- CB34667815
- Molecular Formula:
- C16H18N6O
- Molecular Weight:
- 310.35
- MOL File:
- 1263774-59-9.mol
- Modify Date:
- 2024/7/2 8:55:06
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P305+P351+P338 |
Delgocitinib Chemical Properties,Uses,Production
Characteristics
Class: non-receptor tyrosine kinase
Treatment: atopic dermatitis (topical ointment)
Protein binding = 22–29%
Definition
The lead compound to delgocitinib was tofacitinib, a potent pan-JAK inhibitor. To maintain the overall pan-JAK inhibition profile of tofacitinib, the pyrrolopyrimidine hinge binder, and the cyanoacetyl group were kept fixed. At the same time, the central aminopiperidine linker was replaced by a variety of spirocyclic scaffolds to maintain comparable binding patterns. This effort identified the three-dimensional diazaspiro[3.4]octane scaffold as the optimal linker, and further SAR studies led to delgocitinib, which demonstrates better selectivity against JAK3 compared to tofacitinib and its selectivity for the JAK family over LCK is also improved. Delgocitinib exhibits no significant inhibition of non-JAK kinases under 1 μM except ROCK2.
Definition
Delgocitinib is metabolically stable in both liver microsomes and hepatocytes across species (human, rat, dog, and monkey), and it is also not metabolized in human skin microsomes. It has favorable oral bioavailability in rats (78%) and dogs (124%). Following repeat topical application to the affected area twice daily with a maximum dose of 5 g per application, plasma levels of delgocitinib were detected in 12%, 16%, 14%, and 12% of the patients at week 4, 12, 28, and 52, respectively.
Clinical Use
Delgocitinib is a pan-JAK inhibitor that inhibits all Janus Kinase (JAK) family members. Topical delgocitinib 0.5% ointment received its first approval in Japan in 2020 for treating adults with atopic dermatitis. The FDA has granted delgocitinib cream fast-track designation for chronic hand eczema.
Delgocitinib Preparation Products And Raw materials
Raw materials
Preparation Products
Delgocitinib Suppliers
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| Zhengzhou Alfa Chemical Co.,Ltd | +8618530059196 | China | 13127 | 58 | Inquiry |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | United States | 19892 | 58 | Inquiry |
| InvivoChem | +1-708-310-1919 +1-13798911105 | United States | 6393 | 58 | Inquiry |
| Hangzhou MolCore BioPharmatech Co.,Ltd. | +86-057181025280; +8617767106207 | China | 49739 | 58 | Inquiry |
| Chengdu Peter-like Biotechnology Co., Ltd. | 028-81700200 18108052721 | China | 5182 | 58 | Inquiry |
| ShangHai Biochempartner Co.,Ltd | 17754423994 17754423994 | China | 8013 | 62 | Inquiry |
| Nanjing Tianhai Pharmaceutical Technology Co., Ltd. | 025-58351158 13851454004 | China | 144 | 58 | Inquiry |
| TargetMol Chemicals Inc. | 4008200310 | China | 24016 | 58 | Inquiry |
| Henan Anky Chemical Technology Co., Ltd. | 17836913271 | China | 2808 | 58 | Inquiry |
| Wuhan Sun-shine Bio-technology Corporation Limited | +86-027-6552-2453 | China | 727 | 58 | Inquiry |
Related articles
- Synthesis of Delgocitinib
- Delgocitinib is synthesised using bromolactone as raw material by chemical reaction.
- Dec 26，2023