1838123-21-9 Usage
Description
1-(4-chloro-2-hydroxy-3-(((R)-3-methyltetrahydrofuran-3-yl)sulfonyl)phenyl)-3-((R)-2-methylcyclopent-2-en-1-yl)urea, also known as TAK-499, is a synthetic compound designed for the treatment of hormone-sensitive prostate cancer. It functions by inhibiting the enzyme 17β-hydroxysteroid dehydrogenase type 3, which plays a crucial role in androgen production. By blocking this enzyme, TAK-499 effectively reduces androgen levels in the body, thereby potentially slowing the growth and spread of prostate cancer cells. TAK-499 is currently in clinical trials and demonstrates promise as a targeted therapy for prostate cancer.
Uses
Used in Pharmaceutical Industry:
TAK-499 is used as an inhibitor for the treatment of hormone-sensitive prostate cancer. It targets the enzyme 17β-hydroxysteroid dehydrogenase type 3, which is involved in the production of androgens. By inhibiting this enzyme, TAK-499 can reduce androgen levels in the body, potentially slowing the growth and spread of prostate cancer cells.
Used in Clinical Trials:
TAK-499 is utilized in clinical trials to evaluate its safety, efficacy, and potential side effects as a targeted therapy for prostate cancer. These trials are essential for determining the compound's suitability as a treatment option and for establishing the appropriate dosage and administration methods for patients.
Check Digit Verification of cas no
The CAS Registry Mumber 1838123-21-9 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,8,3,8,1,2 and 3 respectively; the second part has 2 digits, 2 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 1838123-21:
(9*1)+(8*8)+(7*3)+(6*8)+(5*1)+(4*2)+(3*3)+(2*2)+(1*1)=169
169 % 10 = 9
So 1838123-21-9 is a valid CAS Registry Number.
1838123-21-9Relevant articles and documents
Discovery of Novel 1-Cyclopentenyl-3-phenylureas as Selective, Brain Penetrant, and Orally Bioavailable CXCR2 Antagonists
Lu, Hongfu,Yang, Ting,Xu, Zhongmiao,Lin, Xichen,Ding, Qian,Zhang, Yueting,Cai, Xin,Dong, Kelly,Gong, Sophie,Zhang, Wei,Patel, Metul,Copley, Royston C. B.,Xiang, Jianing,Guan, Xiaoming,Wren, Paul,Ren, Feng
supporting information, p. 2518 - 2532 (2018/03/26)
CXCR2 has emerged as a therapeutic target for not only peripheral inflammatory diseases but also neurological abnormalities in the central nervous system (CNS). Herein, we describe the discovery of a novel 1-cyclopentenyl-3-phenylurea series as potent and CNS penetrant CXCR2 antagonists. Extensive SAR studies, wherein molecules' property forecast index (PFI) was carefully optimized for overall balanced developability profiles, led to the discovery of the advanced lead compound 68 with a desirable PFI. Compound 68 demonstrated good in vitro pharmacology with excellent selectivity over CXCR1 and other chemokine receptors. Rat and dog pharmacokinetics (PK) revealed good oral bioavailability, high oral exposure, and desirable elimination half-life of the compound in both species. In addition, the compound demonstrated dose-dependent efficacy in the in vivo pharmacology neutrophil infiltration "air pouch" model in rodents after oral administration. Further, compound 68 is a CNS penetrant molecule with high unbound fraction in brain tissue.
