Home > mGluR & > CTEP

CTEP

RO4956371,RO 4956371,RO-4956371

CTEP是一种新型，长效的，口服生物有效的，mGlu5受体变构拮抗剂，IC50为2.2 nM，比作用于其他mGlu受体选择性高1000倍以上。

目录号
EY1807
EY1807
EY1807
EY1807
EY1807
纯度
99.42%
99.42%
99.42%
99.42%
99.42%
规格
2 mg
5 mg
10 mg
50 mg
100 mg
原价
788
915
1680
5400
7360
售价
788
915
1680
5400
7360
库存
现货
现货
现货
现货
现货
订购
订购
订购
订购
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  • 生物活性

    CTEP (RO4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, shows >1000-fold selectivity over other mGlu receptors.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

    1.0 mg/kg 口服

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Lindemann L, et al. J Pharmacol Exp Ther, 2011, 339(2), 474-486.

    分子式
    C19H13ClF3N3O    		 分子量
    391.77    		 CAS号
    871362-31-1    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    >50 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    10 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT00093457 Prostate Cancer Drug: sorafenib tosylate NCIC Clinical Trials Group|National Cancer Institute (NCI)|Canadian Cancer Trials Group Phase 2 2004-07-01 2011-09-27
    NCT01039155 Adult Solid Neoplasm|Hematopoietic and Lymphoid Cell Neoplasm Drug: Azacitidine|Other: Laboratory Biomarker Analysis|Drug: Oxaliplatin|Other: Pharmacological Study National Cancer Institute (NCI) Phase 1 2009-12-01 2015-10-05
    NCT01281852 Cervical Adenocarcinoma|Cervical Adenosquamous Carcinoma|Cervical Squamous Cell Carcinoma, Not Otherwise Specified|Recurrent Cervical Carcinoma|Stage IVB Cervical Cancer Drug: Cisplatin|Other: Laboratory Biomarker Analysis|Drug: Paclitaxel|Drug: Veliparib National Cancer Institute (NCI) Phase 1|Phase 2 2011-04-01 2017-01-31
    NCT00117169 Pulmonary Embolism Procedure: multi-detector helical computed tomography University Hospital, Geneva 2005-01-01 2012-10-12
    NCT00039091 Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(15;17)(q22;q12)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Atypical Chronic Myeloid Leukemia, BCR-ABL1 Negative|Myelodysplastic/Myeloproliferative Neoplasm, Unclassifiable|Previously Treated Myelodysplastic Syndromes|Recurrent Adult Acute Myeloid Leukemia|Recurrent Melanoma|Recurrent Non-small Cell Lung Cancer|Recurrent Ovarian Epithelial Cancer|Stage IV Melanoma|Stage IV Non-small Cell Lung Cancer Biological: ipilimumab National Cancer Institute (NCI) Phase 1 2002-03-01 2013-01-09
    NCT00054483 Adult Grade III Lymphomatoid Granulomatosis|Adult Nasal Type Extranodal NK/T-cell Lymphoma|Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Nodal Marginal Zone B-cell Lymphoma|Recurrent Adult Burkitt Lymphoma|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Adult Diffuse Mixed Cell Lymphoma|Recurrent Adult Diffuse Small Cleaved Cell Lymphoma|Recurrent Adult Grade III Lymphomatoid Granulomatosis|Recurrent Adult Immunoblastic Large Cell Lymphoma|Recurrent Adult Lymphoblastic Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Small Lymphocytic Lymphoma|Refractory Multiple Myeloma|Splenic Marginal Zone Lymphoma|Stage III Multiple Myeloma|Stage IV Adult Burkitt Lymphoma|Stage IV Adult Diffuse Large Cell Lymphoma|Stage IV Adult Diffuse Mixed Cell Lymphoma|Stage IV Adult Diffuse Small Cleaved Cell Lymphoma|Stage IV Adult Immunoblastic Large Cell Lymphoma|Stage IV Adult Lymphoblastic Lymphoma|Stage IV Grade 1 Follicular Lymphoma|Stage IV Grade 2 Follicular Lymphoma|Stage IV Grade 3 Follicular Lymphoma|Stage IV Mantle Cell Lymphoma|Stage IV Marginal Zone Lymphoma|Stage IV Small Lymphocytic Lymphoma|Unspecified Adult Solid Tumor, Protocol Specific|Waldenstr枚m Macroglobulinemia Drug: bortezomib|Other: laboratory biomarker analysis|Other: pharmacological study National Cancer Institute (NCI) Phase 1 2003-01-01 2013-05-15
    NCT00026169 Malignant Neoplasm|Unspecified Adult Solid Tumor, Protocol Specific Drug: imatinib mesylate|Other: laboratory biomarker analysis|Other: pharmacological study National Cancer Institute (NCI) Phase 1 2001-09-01 2013-01-09
    NCT01074411 Fallopian Tube Clear Cell Adenocarcinoma|Fallopian Tube Endometrioid Adenocarcinoma|Fallopian Tube Mucinous Adenocarcinoma|Fallopian Tube Serous Adenocarcinoma|Fallopian Tube Transitional Cell Carcinoma|Ovarian Brenner Tumor|Ovarian Clear Cell Adenocarcinoma|Ovarian Clear Cell Cystadenocarcinoma|Ovarian Endometrioid Adenocarcinoma|Ovarian Mucinous Adenocarcinoma|Ovarian Mucinous Cystadenocarcinoma|Ovarian Seromucinous Carcinoma|Ovarian Serous Adenocarcinoma|Ovarian Serous Cystadenocarcinoma|Ovarian Transitional Cell Carcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Undifferentiated Fallopian Tube Carcinoma|Undifferentiated Ovarian Carcinoma Drug: Bortezomib|Drug: Carboplatin|Other: Laboratory Biomarker Analysis|Other: Pharmacological Study National Cancer Institute (NCI) Phase 1 2010-04-01 2017-01-31
    NCT02839707 Fallopian Tube Clear Cell Adenocarcinoma|Fallopian Tube Endometrioid Adenocarcinoma|High Grade Fallopian Tube Serous Adenocarcinoma|High Grade Ovarian Serous Adenocarcinoma|Ovarian Clear Cell Adenocarcinoma|Ovarian Endometrioid Adenocarcinoma|Ovarian Seromucinous Carcinoma|Primary Peritoneal High Grade Serous Adenocarcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Undifferentiated Fallopian Tube Carcinoma|Undifferentiated Ovarian Carcinoma Drug: Atezolizumab|Biological: Bevacizumab|Other: Laboratory Biomarker Analysis|Drug: Pegylated Liposomal Doxorubicin Hydrochloride|Other: Quality-of-Life Assessment National Cancer Institute (NCI) Phase 2|Phase 3 2017-05-01 2017-01-31
    NCT00989651 Fallopian Tube Carcinosarcoma|Fallopian Tube Clear Cell Adenocarcinoma|Fallopian Tube Endometrioid Adenocarcinoma|Fallopian Tube Mucinous Adenocarcinoma|Fallopian Tube Serous Neoplasm|Fallopian Tube Transitional Cell Carcinoma|Ovarian Brenner Tumor|Ovarian Carcinosarcoma|Ovarian Clear Cell Adenocarcinoma|Ovarian Endometrioid Adenocarcinoma|Ovarian Mucinous Adenocarcinoma|Ovarian Seromucinous Tumor|Ovarian Serous Adenocarcinoma|Ovarian Transitional Cell Carcinoma|Primary Peritoneal Serous Adenocarcinoma|Stage IIA Fallopian Tube Cancer|Stage IIA Ovarian Cancer|Stage IIB Fallopian Tube Cancer|Stage IIB Ovarian Cancer|Stage IIC Fallopian Tube Cancer|Stage IIC Ovarian Cancer|Stage IIIA Fallopian Tube Cancer|Stage IIIA Ovarian Cancer|Stage IIIA Primary Peritoneal Cancer|Stage IIIB Fallopian Tube Cancer|Stage IIIB Ovarian Cancer|Stage IIIB Primary Peritoneal Cancer|Stage IIIC Fallopian Tube Cancer|Stage IIIC Ovarian Cancer|Stage IIIC Primary Peritoneal Cancer|Stage IV Fallopian Tube Cancer|Stage IV Ovarian Cancer|Stage IV Primary Peritoneal Cancer|Undifferentiated Fallopian Tube Carcinoma|Undifferentiated Ovarian Carcinoma Biological: Bevacizumab|Drug: Carboplatin|Drug: Cisplatin|Other: Laboratory Biomarker Analysis|Drug: Paclitaxel|Drug: Veliparib National Cancer Institute (NCI) Phase 1 2009-10-01 2017-01-31
    NCT00085358 Brenner Tumor|Fallopian Tube Cancer|Ovarian Carcinosarcoma|Ovarian Clear Cell Cystadenocarcinoma|Ovarian Endometrioid Adenocarcinoma|Ovarian Mixed Epithelial Carcinoma|Ovarian Mucinous Cystadenocarcinoma|Ovarian Serous Cystadenocarcinoma|Ovarian Undifferentiated Adenocarcinoma|Primary Peritoneal Cavity Cancer|Stage II Ovarian Epithelial Cancer|Stage III Ovarian Epithelial Cancer|Stage IV Ovarian Epithelial Cancer Drug: carboplatin|Drug: paclitaxel|Drug: docetaxel|Biological: bevacizumab National Cancer Institute (NCI) Phase 1 2004-05-01 2013-03-18
    NCT01239875 Cutaneous B-cell Non-Hodgkin Lymphoma|Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Nodal Marginal Zone B-cell Lymphoma|Adult Diffuse Mixed Cell Lymphoma|Adult Diffuse Small Cleaved Cell Lymphoma|Adult Grade III Lymphomatoid Granulomatosis|Adult Immunoblastic Large Cell Lymphoma|Adult Lymphoblastic Lymphoma|Grade 1 Follicular Lymphoma|Grade 2 Follicular Lymphoma|Grade 3 Follicular Lymphoma|Mantle Cell Lymphoma|Marginal Zone Lymphoma|Small Lymphocytic Lymphoma|Splenic Marginal Zone Lymphoma|Waldenstrom Macroglobulinemia With Nodal Disease Biological: dendritic cell vaccine therapy|Procedure: cryotherapy|Biological: pneumococcal polyvalent vaccine|Other: laboratory biomarker analysis|Other: immunoenzyme technique|Other: immunohistochemistry staining method|Biological: autologous dendritic cell-tumor fusion vaccine Mayo Clinic|National Cancer Institute (NCI) 2010-11-01 2017-03-21
    NCT01322802 Stage III Ovarian Epithelial Cancer|Stage III Ovarian Germ Cell Tumor|Stage IV Ovarian Epithelial Cancer|Stage IV Ovarian Germ Cell Tumor Biological: pUMVC3-hIGFBP-2 multi-epitope plasmid DNA vaccine|Other: laboratory biomarker analysis University of Washington|National Cancer Institute (NCI) Phase 1 2012-03-01 2016-04-12
    NCT01606241 Recurrent Breast Carcinoma|Recurrent Fallopian Tube Carcinoma|Recurrent Ovarian Carcinoma|Recurrent Primary Peritoneal Carcinoma|Stage IIA Breast Cancer|Stage IIA Fallopian Tube Cancer|Stage IIA Ovarian Cancer|Stage IIB Breast Cancer|Stage IIB Fallopian Tube Cancer|Stage IIB Ovarian Cancer|Stage IIC Fallopian Tube Cancer|Stage IIC Ovarian Cancer|Stage IIIA Breast Cancer|Stage IIIA Fallopian Tube Cancer|Stage IIIA Ovarian Cancer|Stage IIIA Primary Peritoneal Cancer|Stage IIIB Breast Cancer|Stage IIIB Fallopian Tube Cancer|Stage IIIB Ovarian Cancer|Stage IIIB Primary Peritoneal Cancer|Stage IIIC Breast Cancer|Stage IIIC Fallopian Tube Cancer|Stage IIIC Ovarian Cancer|Stage IIIC Primary Peritoneal Cancer|Stage IV Fallopian Tube Cancer|Stage IV Ovarian Cancer|Stage IV Primary Peritoneal Cancer Drug: Cyclophosphamide|Other: Laboratory Biomarker Analysis|Biological: Multi-epitope Folate Receptor Alpha Peptide Vaccine Mayo Clinic|National Cancer Institute (NCI) Phase 1 2012-07-01 2016-10-10
    NCT01007968 Advanced Solid Tumors Drug: LBH589 Novartis Pharmaceuticals|Novartis Phase 1 2010-03-01 2016-08-17
    NCT02713386 Fallopian Tube Carcinosarcoma|Fallopian Tube Clear Cell Adenocarcinoma|Fallopian Tube Endometrioid Adenocarcinoma|Fallopian Tube Serous Neoplasm|High Grade Ovarian Serous Adenocarcinoma|Ovarian Carcinosarcoma|Ovarian Clear Cell Adenocarcinoma|Ovarian Endometrioid Adenocarcinoma|Primary Peritoneal Serous Adenocarcinoma|Stage III Fallopian Tube Cancer|Stage III Ovarian Cancer|Stage III Primary Peritoneal Cancer|Stage IIIA Fallopian Tube Cancer|Stage IIIA Ovarian Cancer|Stage IIIA Primary Peritoneal Cancer|Stage IIIB Fallopian Tube Cancer|Stage IIIB Ovarian Cancer|Stage IIIB Primary Peritoneal Cancer|Stage IIIC Fallopian Tube Cancer|Stage IIIC Ovarian Cancer|Stage IIIC Primary Peritoneal Cancer|Stage IV Fallopian Tube Cancer|Stage IV Ovarian Cancer|Stage IV Primary Peritoneal Cancer Drug: Carboplatin|Other: Laboratory Biomarker Analysis|Drug: Paclitaxel|Drug: Ruxolitinib Phosphate|Procedure: Therapeutic Conventional Surgery NRG Oncology|National Cancer Institute (NCI) Phase 1|Phase 2 2016-05-01 2017-01-20
    NCT01892930 Recurrent Renal Cell Cancer|Stage IV Renal Cell Cancer Radiation: stereotactic body radiation therapy|Procedure: therapeutic conventional surgery|Other: laboratory biomarker analysis Roswell Park Cancer Institute|National Cancer Institute (NCI) 2013-07-11 2017-02-09
    NCT00019929 Lung Cancer Biological: mutant p53 peptide pulsed dendritic cell vaccine|Procedure: adjuvant therapy National Cancer Institute (NCI) Phase 2 2000-08-01 2013-06-18
    NCT00005786 Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Nodal Marginal Zone B-cell Lymphoma|Prolymphocytic Leukemia|Recurrent Adult Diffuse Small Cleaved Cell Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Splenic Marginal Zone Lymphoma|Waldenstrm Macroglobulinemia Drug: arsenic trioxide|Other: laboratory biomarker analysis National Cancer Institute (NCI) 2001-01-01 2013-01-31
    NCT01076556 Chronic Lymphocytic Leukemia|Prolymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Stage I Chronic Lymphocytic Leukemia|Stage I Small Lymphocytic Lymphoma|Stage II Chronic Lymphocytic Leukemia|Stage II Small Lymphocytic Lymphoma|Stage III Chronic Lymphocytic Leukemia|Stage III Small Lymphocytic Lymphoma|Stage IV Chronic Lymphocytic Leukemia|Stage IV Small Lymphocytic Lymphoma Drug: Alvocidib Hydrochloride|Drug: Cyclophosphamide|Other: Diagnostic Laboratory Biomarker Analysis|Other: Pharmacological Study|Biological: Rituximab National Cancer Institute (NCI) Phase 1 2010-04-01 2015-11-10
    NCT02424916 Metastatic Melanoma|Brain Metastases Biological: Melanoma antigens-specific CD8+ T lymphocytes Nantes University Hospital|UMR892 Phase 1|Phase 2 2015-05-01 2015-06-09
    NCT00005840 Endometrial Clear Cell Adenocarcinoma|Endometrial Serous Adenocarcinoma|Stage III Uterine Corpus Cancer|Stage IV Uterine Corpus Cancer Drug: Paclitaxel|Drug: Cisplatin|Radiation: Radiation Therapy Gynecologic Oncology Group|National Cancer Institute (NCI) Phase 1 2000-07-01 2014-12-29
    NCT01729884 HER2-positive Breast Cancer|Male Breast Cancer|Recurrent Breast Cancer|Stage IV Breast Cancer Biological: HER-2/neu peptide vaccine|Other: laboratory biomarker analysis University of Washington|National Cancer Institute (NCI) Phase 2 2012-12-01 2014-10-30
    NCT01632332 HER2-positive Breast Cancer|Male Breast Cancer|Stage II Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer Biological: HER-2/neu peptide vaccine|Other: laboratory biomarker analysis Mayo Clinic|Tapimmune Inc. Phase 1 2012-07-01 2014-04-08
    NCT00194714 HER2/Neu Positive|HLA-A2 Positive Cells Present|Stage IV Breast Cancer|Stage IV Ovarian Cancer Biological: HER-2/neu Peptide Vaccine|Other: Laboratory Biomarker Analysis University of Washington|National Cancer Institute (NCI) Phase 1|Phase 2 2016-05-01 2017-01-04

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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