MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Etrasimod

CAS No. : 1206123-37-6

产品活性：Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P₁) receptor with an IC₅₀ value of 1.88 nM in CHO cells.

研究领域：GPCR/G Protein

作用靶点：LPL Receptor

In Vitro: APD334 is a structurally novel, selective, functional antagonist of S1P₁. In CHO cells expressing HA tagged S1P₁, APD334 is found to have an IC₅₀ value of 1.88 nM. Moderate agonism at human S1P₄ and S1P₅ is observed but is reduced relative to S1P₁, both in terms of potency and efficacy. APD334 is devoid of any agonism or antagonism at human S1P₂ and S1P₃. APD334 achieves good central exposure following oral dosing and possesses a favorable pharmacokinetic profile in multiple preclinical species. S1P₁ activity is maintained in mice (EC₅₀=0.44 nM), rats (EC₅₀=0.32 nM), dogs (EC₅₀=0.34 nM) and monkeys (EC₅₀=0.32 nM).

In Vivo: APD334 has a relatively low systemic clearance (<4% of hepatic blood flow) and high C_max across all species. In both dog and monkey a significant decrease in volume of distribution (Vss) is observed relative to rodent. Oral bioavailability is in the range of 40–100%, and the terminal phase half-life varied from 6 h in monkey, to as long as 29 h in dog. Rat and monkey t_1/2 values for siponimod (another S1P1 modulator currently in human trials) have been disclosed and are 6 and 19 h, respectively.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  GPCR/G Protein Compound Library  |  Immunology/Inflammation Compound Library  |  Clinical Compound Library  |  Drug Repurposing Compound Library  |  Orally Active Compound Library  |  Rare Diseases Drug Library  |  Anti-Pulmonary Fibrosis Compound Library  |  Non-steroidal Anti-Inflammatory Compound Library  |  Membrane Protein-targeted Compound Library  |  Membrane Receptor-targeted Compound Library  |  BMS-986020 sodium  |  ONO-0300302  |  BMS-986278  |  NAEPA  |  Sphingosine-1-phosphate-d₇  |  S1P1 agonist III  |  S1PR1 modulator 1  |  LPA2 antagonist 2  |  Radioprotectin-1  |  S1PR1 agonist 1  |  TC-SP 14  |  CYM50358  |  W146  |  Udifitimod  |  CRT0273750  |  Ki16425  |  ONO-9780307  |  CS-2100  |  Fingolimod phosphate-d₄  |  CAY10444  |  ONO-0740556  |  NIBR0213  |  CYM50260  |  ASP-4058  |  FTY720 (S)-Phosphate  |  Sonepcizumab  |  TAK-615  |  GSK2018682  |  Mocravimod hydrochloride

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物  |  寡核苷酸  |  抗体  |  点击化学

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

品牌介绍:
•   MCE (MedChemExpress) 拥有200 多种*仅有化合物库，我们致力于为*科研客户提供前沿的高品质小分子活性化合物；
•   50,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领；
•   产品种类涵盖各种重组蛋白，多肽，常用试剂盒 ，更有 PROTAC、ADC 等特色产品，广泛应用于新药研发、生命科学等科研项目；
•   提供虚拟筛选，离子通道筛选，代谢组学分析检测分析，药物筛选等专业技术服务；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种顶级期刊及制药 Patent 收录了MCE客户的科研成果；
•   专业团队跟踪新的制药及生命科学研究进展，为您提供*新的活性化合物；
•   与世界各大制药公司及*科研机构建立了长期的合作。