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

CAS No. : 1345614-59-6

MCE 站：AM095

产品活性：AM095 是一种选择性的 LPA₁ 受体拮抗剂。作用于人和鼠 转染 LPA₁ 的 CHO 细胞，AM095 拮抗 LPA 诱导的钙流动，IC₅₀ 分别为 0.025 和 0.023 μM。

研究领域：GPCR/G Protein

作用靶点：LPL Receptor

In Vitro: AM095 is a potent LPA₁ receptor antagonist because it inhibits GTPγS binding to Chinese hamster ovary (CHO) cell membranes overexpressing recombinant human or mouse LPA₁ with IC₅₀ values of 0.98 and 0.73 μM, respectively. AM095 inhibits LPA-driven chemotaxis of CHO cells overexpressing mouse LPA₁ (IC₅₀=778 nM) and human A2058 melanoma cells (IC₅₀=233 nM). The IC₅₀ of AM095 in the human LPA₁ GTPγS binding assay is comparable with that of our previously published compound AM966 (IC₅₀=0.98±0.17 μM) and the Debio-0719 compound (IC₅₀=0.60±0.04 μM). 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.

In Vivo: 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. After oral (10 mg/kg) dosing in rats, AM095 plasma concentrations peaked at 2 h with a C_max of 41 μM, thereafter decreasing to 10 nM by 24 h. After intravenous (2 mg/kg) dosing, a C_max of 12 μM is observed within 15 min, which also decreased to approximately 10 nM by 24 h, yielding a t_1/2 of 1.79 h. In dogs, a single oral dose of 5 mg/kg yielded a peak plasma concentration of 21 μM within 15 min of dosing, which then decreased to 10 nM by 24 h. In contrast, an intravenous dose of 2 mg/kg resulted in a C_max of 11 μM within 15 min and decreased to 15 nM by 8 h, yielding a t_1/2 of 1.5 h.

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  |  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。