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。

BPTU

CAS No. : 870544-59-5

MCE 国际站：BPTU

产品活性：BPTU (BMS-646786) 是一种非核苷酸类 P2Y₁ 受体变构拮抗剂，具有抗血栓活性。BPTU 能够阻断位于胃肠道神经肌肉接头的 P2Y₁ 受体。

研究领域：GPCR/G Protein

作用靶点：P2Y Receptor

In Vitro: BPTU blocks the supramaximal fast inhibitory junction potentials (fIJP) in a concentration-dependent manner both in the rat and mouse colon. The EC₅₀ of BPTU is approximately 0.3 μM and 0.06 μM for the rat and mouse colon, respectively. In the rat colon, addition of the P2Y agonist ADPβS at 10 μM significantly reduces spontaneous contractions to a 43.2±13.4% (N=5) (P=0.0002), and this reduction is blocked by 15 min incubation with BPTU at a concentration of 3 μM (93.3±5.1%). Similar results are obtained in the murine colon where ADPβS at 10 μM reduces the area under the curve (AUC) of contractions to a 15.8±5.1% (N=4) (P<0.0001) and its effect is reversed with BPTU at 3 μM (82.7±3.6%). Addition of MRS2365, a selective P2Y1 agonist, at a concentration of 5 μM significantly reduces spontaneous contractions to a 21.2±4.8% (N=5) (P=0.0002) in the murine colon, and this reduction is blocked by 15 min incubation with BPTU at a concentration of 3 μM (93.1±3.8%). The blockage of the MRS2365-induced response by BPTU at 3 μM also occurs in control conditions (N=5) (10.2±5.5% vs. 86.7±5.0%).

In Vivo: Uptake of BPTU from the peritoneal cavity is relatively rapid. Blood boron levels are maximal within 1 h after administration. After only 1 h, a boron tumor-to-blood ratio above 1 is found for BPTU in pigmented tumors, which is indicative of drug retention. This is not seen in the non-pigmented tumor variant, in which tumor boron levels closely follow blood levels. Up to 24 h, Borocaptate sodium (BSH) exhibits no selective retention in either tumor, but achieves higher maximum tumor boron concentrations than BPTU as a result of the administration of higher amounts of boron. During the tissue distribution phase, liver-to-kidney boron concentration ratios range from 2 to 4 for BSH and from 0.5 to 1 for BPTU.

相关产品：Covalent Screening Library Plus  |  Bioactive Compound Library Plus  |  GPCR/G Protein Compound Library  |  Anti-Cancer Compound Library  |  Covalent Screening Library  |  Neurotransmitter Receptor Compound Library  |  Targeted Diversity Library  |  Heterocyclic Compound Library  |  Membrane Protein-targeted Compound Library  |  Membrane Receptor-targeted Compound Library  |  PPTN  |  AZD1283  |  PIT  |  Ticagrelor-d₇  |  MRS2179 tetrasodium  |  Prasugrel hydrochloride  |  Vicagrel  |  MRS2279  |  Elinogrel  |  Uridine 5′-diphosphoglucose disodium salt  |  Blue FPG-A trisodium  |  2-Methylthioadenosine diphosphate trisodium  |  PSB 0474  |  Clopidogrel  |  Oral antiplatelet agent 1  |  (±)-Clopidogrel-d₇ sulfate  |  P2Y2R/GPR17 antagonist 1  |  2-Methylthio-AMP  |  AR-C118925XX  |  NF157  |  MRS2365  |  Clopidogrel-d₃ hydrogen sulfate  |  MRS 2578  |  Cangrelor

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

货号: HY-13831

品牌介绍:
•   MCE (MedChemExpress) 拥有200 多种全球独家化合物库，我们致力于为全球科研客户提供前沿最全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专利收录了MCE客户的科研成果；
•   专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。