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。

Zamaporvint

CAS No. : 1900754-56-4

MCE 站：Zamaporvint

产品活性：Zamaporvint (RXC004) 是一种具有口服活性的选择性 Wnt 抑制剂。Zamaporvint 靶向膜结合邻酰基转移酶 Porcupine 并抑制 Wnt 配体棕榈酰化、分泌和通路激活。Zamaporvint 显示出良好的药代动力学特征，并在依赖 Wnt 配体的结直肠和胰腺细胞系中显示出强效的抗增殖作用。Zamaporvint 具有多种抗肿瘤机制，可用于癌症研究。是是

研究领域：Stem Cell/Wnt  |  Metabolic Enzyme/Protease

作用靶点：Wnt  |  Acyltransferase  |  Porcupine

In Vitro: Zamaporvint (300 nM, 48 h) treatment of L- wnt3a cells reduce the ability of conditioned medium to activate the β-catenin-responsive luciferase reporter gene in a concentration-dependent manner, with an IC₅₀ of 64 pM, ａnd the addition of recombinant Wnt3a restore the luciferase activity, suggesting no effect on downstream Wnt signaling.
The effect of Zamaporvint (100 nM, 24 hr) on proliferation reflects a concentration-dependent downregulation of c-Myc mRNA. Reduced the proportion of cells in S phase ａnd strongly suppressed the expression of the mitotic marker phospho-histone-H3 in cells with abnormal upstream components of the Wnt pathway, indicative of cell cycle arrest, ａnd was found to have reduced immunosuppression at the same dose as after administration Sexual support .
Zamaporvint (20 μM, 18 h) in plasma across species ranged from 2.5% to 7.5%, microsomal CL_int values ranged from 3.9 to 31.6 μL/min?mg, with mouse having the lowest ａnd dog the highest predicted clearances, rodents ａnd humans display low clearance.
Zamaporvint (10 μM, 2 h) has good intrinsic permeability, showing some evidence of efflux in MDR1-MDCKII cells but not in Caco-2 cells.

In Vivo: Zamaporvint (1.5 mg/kg or 5 mg/kg orally twice daily, or 5 mg/kg Zamaporvint orally once daily, for 28 days) reduces in tumor growth, ａnd inhibition of Wnt-responsive gene expression including cMyc, was observed in the Wnt liganddependent SNU-1411, AsPC1, ａnd HPAFII models, ａnd no effected tumor growth in the Wnt ligandindependent HCT116 xenograft mode.
Zamaporvint (1.5 mg/kg, 5 mg/kg, once daily) reduces Ki67-positive cells in the total tumor area, ａnd its effect is more pronounced in differentiated tumor areas, ａnd by inhibiting immune evasion in the B16F10 "cold" tumor model Antitumor effect .
Zamaporvint (1.5 or 5 mg/kg once daily) stimulates host tumor immunity, reduces resident myeloid-derived suppressor cells within B16F10 tumors ａnd synergizing with anti-programmed cell death protein-1 (PD-1, HY-P73361) to increase CD8+/regulatory T cell ratios within CT26 tumors.
Pharmacokinetic Parameters of Zamaporvint in Mice.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Metabolism/Protease Compound Library  |  Stem Cell Signaling Compound Library  |  Wnt/Hedgehog/Notch Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Differentiation Inducing Compound Library  |  Cytoskeleton Compound Library  |  Orally Active Compound Library  |  Neuroprotective Compound Library  |  Anti-Breast Cancer Compound Library  |  Lipid Metabolism Compound Library   |  Anti-Liver Cancer Compound Library   |  Anti-Colorectal Cancer Compound Library   |  Anti-Prostate Cancer Compound Library  |  Anti-Pulmonary Fibrosis Compound Library  |  Cancer Stem Cells Compound Library  |  Antihypertensive Compound Library  |  Highly Selective Inhibitors Library  |  RP-64477  |  PF-06424439 methanesulfonate  |  E-5324  |  RP 73163 Racemate  |  ACAT-IN-10  |  FzM1  |  Pamidronic acid  |  Fz7-21  |  ABT-046  |  PF-04620110  |  LGK974  |  NSC668036  |  Porcn-IN-2  |  JW67  |  Ipafricept  |  AZD3988  |  Ipivivint  |  ACAT-IN-5  |  DL-Glyceraldehyde 3-phosphate  |  WIC1  |  Pyripyropene A  |  K-604 dihydrochloride  |  Diacylglycerol acyltransferase inhibitor-1  |  ACAT-IN-4  |  JW74  |  IQ 1  |  Heparan Sulfate  |  VULM 1457  |  L-Quebrachitol

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 多种全球独家化合物库，我们致力于为全球科研客户提供前沿*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。