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。

AM095 free acid

CAS No. : 1228690-36-5

MCE 站：AM095 free acid

产品活性：AM095 free acid 是一种有效的 LPA1 受体拮抗剂，对重组人和小鼠 LPA1 的 IC₅₀ 值分别为 0.98 和 0.73 μM。

研究领域：GPCR/G Protein

作用靶点：LPL Receptor

In Vitro: AM095 inhibits the LPA-induced calcium flux of CHO cells stably transfected with human or mouse LPA1. The IC₅₀ for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA1-transfected CHO cells is 0.025 and 0.023 μM, respectively. AM095 reduces LPA-induced vasorelaxation by appr 90% at 10 μM as compared to vehicle control. AM095 inhibits LPA-driven chemotaxis of CHO cells overexpressing mouse LPA1 (IC₅₀=778 nM) and human A2058 melanoma cells (IC₅₀=233 nM).

In Vivo: Pharmacological antagonism of LPA1 with AM095 significantly attenuates bleomycin-induced dermal fibrosis. AM095 has high oral bioavailability and a moderate half-life and is well tolerated at the doses tested in rats and dogs after oral and intravenous dosing. AM095 dose-dependently reduces LPA-stimulated histamine release. AM095 attenuates bleomycin-induced increases in collagen, protein, and inflammatory cell infiltration in bronchalveolar lavage fluid. AM095 decreases kidney fibrosis in a mouse unilateral ureteral obstruction model.

相关产品：Bioactive Compound Library Plus  |  GPCR/G Protein Compound Library  |  Immunology/Inflammation Compound Library  |  Fingolimod hydrochloride  |  PF-543 Citrate  |  Ki16425  |  JTE-013  |  TY-52156  |  AM095  |  Sphingosine-1-phosphate  |  FTY720 (S)-Phosphate  |  SEW?2871  |  LPA2 antagonist 1  |  CYM-5541  |  ONO-7300243  |  1-Oleoyl lysophosphatidic acid  |  AS2717638  |  CYM50308  |  Radioprotectin-1  |  Ceranib-2  |  LPA2 antagonist 2  |  S1P1 Agonist III  |  CYM50260  |  4-Deoxypyridoxine 5'-phosphate  |  GRI977143  |  H2L 5765834  |  Ki16198  |  NSC12404  |  PF-543 hydrochloride  |  S1PR1-MO-1

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 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域；
•   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 等多种期刊及制药收录了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，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。