BMS-986165 manufacturers
- BMS-986165 API
-
- $100.00 / 1KG
-
2024-12-26
- CAS:1609392-27-9
- Min. Order: 1KG
- Purity: 99.9%
- Supply Ability: 500
- Deucravacitinib
-
- $20.00 / 10g
-
2024-12-26
- CAS:1609392-27-9
- Min. Order: 100g
- Purity: 99.9%
- Supply Ability: 1000kg
- Deucravacitinib
-
- $0.00 / 1g
-
2024-12-25
- CAS:1609392-27-9
- Min. Order: 1g
- Purity: More Than 99%
- Supply Ability: 50kg/Month
|
| | BMS-986165 Basic information | | Uses |
| Product Name: | BMS-986165 | | Synonyms: | Tyk2-IN-4;TYK2-IN-4;BMS986165;BMS-986165;BMS 986165;Deucravacitinib(BMS986165);Deucravacitinib (TYK2-IN-4;6-cyclopropaneamido-4-{[2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl]amino}-N-(2H?)methylpyridazine-3-carboxamide;DeucravacitinibQ: What is
Deucravacitinib Q: What is the CAS Number of
Deucravacitinib;6-(cyclopropanecarboxamido)-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl) phenyl)amino)-N-(methyl-d3)pyridazine-3-carboxamide;Deucravacitinib | | CAS: | 1609392-27-9 | | MF: | C20H22N8O3 | | MW: | 422.45 | | EINECS: | | | Product Categories: | API;APIS;API | | Mol File: | 1609392-27-9.mol |  |
| | BMS-986165 Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMF: 1 mg/ml; DMSO: 1 mg/ml; DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml | | form | A crystalline solid | | color | Off-white to light yellow |
| | BMS-986165 Usage And Synthesis |
| Uses | BMS-986165 is a novel oral selective TYK2 inhibitor with a unique mechanism of action that is expected to provide a promising oral option to help patients effectively manage their psoriasis. | | Uses | Deucravacitinib is a tyrosine kinase 2 inhibitor which can be useful in the treatment of systemic lupus erythematosus. | | General Description |
Deucravacitinib, a highly selective allosteric TYK2 inhibitor, received its first approval from the FDA in 2022 for the treatment of adults with moderate-to-severe plaque psoriasis who are candidates for systemic therapy or phototherapy protein and lipid kinases and pseudokinases with the exception of BMPR2 (IC50 = 193 nM) and JAK1 JH2 pseudokinase domain (IC50 = 1 nM). Despite its potent affinity for JAK1 JH2, deucravacitinib elicited low functional activity in a JAK1/JAK3-dependent IL-2 stimulated cellular assay. BMS-986202 displays >10,000-fold selectivity for TYK2 JH2 over a diverse panel of 273 kinases and pseudokinases that include JAK family members. Like deucravacitinib, its high binding affinity to JAK1 JH2 (IC50 = 7.8 nM) did not translate to functional activity in the cellular assay.
| | Pharmacokinetics |
The crystalline free base form of deucravacitinib exhibited poor aqueous solubility (5.2 μg/mL), which was still acceptable for preclinical studies. It showed moderate half-lives of 4?5 h across species (mouse, dog, and monkey). Excellent exposures and high bioavailability (F > 85%) in mice, dogs, and monkeys were obtained from oral pharmacokinetic studies at a 10 mpk dose. Following oral administration of deucravacitinib, the major metabolite in human plasma was the cyclopropyl carboxamide hydrolytic cleavage product 4 (6-amino-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)amino)-N-methylpyridazine-3-carboxamide).
|
| | BMS-986165 Preparation Products And Raw materials |
|