|2-(3,5-双(三氟甲基)苯基)-N,2-二甲基-N-(6-(4-甲基哌嗪-1-基)-4-(邻甲苯基)吡啶-3-基)丙酰胺|CsnPharm

CAS No.: 290297-26-6

Netupitant/奈妥吡坦 Catalog No. CSN16120

Synonyms: CID 6451149;Ro 67-31898/000;AGE-94200

Netupitant a potent and highly selective NK1 receptor antagonist with Ki of 0.95 nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Neurokinin (NK) receptors belong to the family of G-protein coupled receptors and can be divided into three subtypes: NK1, NK2 and NK3. The endogenous ligand for NK1 receptor is the 11 amino acid neuropeptide substance P (SP)^[3]. Netupitant is a highly potent and selective, orally active neurokinin-1 receptor antagonist with Ki of 0.95 nM^[3]. In CHO NK1 cells, netupitant concentration-dependently antagonized the stimulatory effects of substance P (SP) showing insurmountable antagonism (pK(B) 8.87)^[4]. In the guinea pig ileum, netupitant concentration-dependently depressed the maximal response to SP (pK(B) 7.85) and, in functional washout experiments, displayed persistent (up to 5h) antagonist effects. In mice the intrathecal injection of SP elicited the typical scratching, biting and licking response that was dose-dependently inhibited by netupitant given intraperitoneally in the 1-10 mg/kg dose range. In gerbils, foot tapping behavior evoked by the intracerebroventricular injection of a NK1 agonist was dose-dependently counteracted by netupitant given intraperitoneally (ID(50) 1.5mg/kg) or orally (ID(50) 0.5mg/kg)^[4].
动物研究
剂量
Rat: 0.1 mg/kg - 1 mg/kg^[3] (p.o.) Mice: 10 mg/kg^[4] (i.p.)

给药途径
p.o., i.p.
临床研究

动物研究
剂量	Rat: 0.1 mg/kg - 1 mg/kg^[3] (p.o.) Mice: 10 mg/kg^[4] (i.p.)
给药途径	p.o., i.p.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03386617	Breast Cancer	Phase 2	Recruiting	December 31, 2019	Hong Kong ... more >> Department of Clinical Oncology, Prince of Wales Hospital Recruiting Hong Kong, Hong Kong Contact: Winnie Yeo, MD, FRCP 3505 2118 winnie@clo.cuhk.edu.hk Contact: Dong LAI, RN 3505 1138 dong@clo.cuhk.edu.hk Collapse <<
NCT01339260	-	-	Completed	-	-
NCT03097588	Hematopoietic Cell Transplanta... more >>tion Recipient Malignant Neoplasm Collapse <<	Phase 2	Recruiting	May 2019	United States, Oregon ... more >> OHSU Knight Cancer Institute Recruiting Portland, Oregon, United States, 97239 Contact: Joseph Bubalo 503-494-8007 bubaloj@ohsu.edu Principal Investigator: Joseph Bubalo Collapse <<

更多
参考文献

[1] Stathis M, Pietra C, et al. Inhibition of substance P-mediated responses in NG108-15 cells by netupitant and palonosetron exhibit synergistic effects. Eur J Pharmacol. 2012 Aug 15;689(1-3):25-30.
[2] Hoffmann T, Bos M, et al. Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1362-5. Epub 2005 Dec 5.
[3] Hoffmann T, Bös M, Stadler H, Schnider P, Hunkeler W, Godel T, Galley G, Ballard TM, Higgins GA, Poli SM, Sleight AJ. Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1362-5. doi: 10.1016/j.bmcl.2005.11.047. Epub 2005 Dec 5. PMID:16332435.
[4] Rizzi A, Campi B, Camarda V, Molinari S, Cantoreggi S, Regoli D, Pietra C, Calo' G. In vitro and in vivo pharmacological characterization of the novel NK₁ receptor selective antagonist Netupitant. Peptides. 2012 Sep;37(1):86-97. doi: 10.1016/j.peptides.2012.06.010. Epub 2012 Jun 23. PMID: 22732666.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7283 mL
- 8.6417 mL
- 17.2833 mL
- 5 mM
- 0.3457 mL
- 1.7283 mL
- 3.4567 mL
- 10 mM
- 0.1728 mL
- 0.8642 mL
- 1.7283 mL

技术信息

CAS号

290297-26-6

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C30H32F6N4O

运输

蓝冰

分子量

578.59

别名

CID 6451149;Ro 67-31898/000;AGE-94200;Ro 67-3189;Ro 67-3189/000;奈妥吡坦

溶解度

DMSO	13.0 mg/mL (22.5 mM)
Water	insoluble

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT03386617	Breast Cancer	Phase 2	Recruiting	December 31, 2019	Hong Kong ... more >> Department of Clinical Oncology, Prince of Wales Hospital Recruiting Hong Kong, Hong Kong Contact: Winnie Yeo, MD, FRCP 3505 2118 winnie@clo.cuhk.edu.hk Contact: Dong LAI, RN 3505 1138 dong@clo.cuhk.edu.hk Collapse <<
NCT01339260	-	-	Completed	-	-
NCT03097588	Hematopoietic Cell Transplanta... more >>tion Recipient Malignant Neoplasm Collapse <<	Phase 2	Recruiting	May 2019	United States, Oregon ... more >> OHSU Knight Cancer Institute Recruiting Portland, Oregon, United States, 97239 Contact: Joseph Bubalo 503-494-8007 bubaloj@ohsu.edu Principal Investigator: Joseph Bubalo Collapse <<
NCT01339260	Chemotherapy-Induced Nausea an... more >>d Vomiting Collapse <<	Phase 3	Completed	-	-
NCT01376297	Chemotherapy-Induced Nausea an... more >>d Vomiting Collapse <<	Phase 3	Completed	-	-
NCT03649230	-	-	Recruiting	March 30, 2020	Canada, Alberta ... more >> Tom Baker Cancer Center Not yet recruiting Calgary, Alberta, Canada Canada, New Brunswick The Moncton Hospital Not yet recruiting Moncton, New Brunswick, Canada Canada, Nova Scotia NSHA-QEII Health Sciences Centre Not yet recruiting Halifax, Nova Scotia, Canada Cape Breton Cancer Centre Recruiting Sydney, Nova Scotia, Canada Canada, Ontario Royal Victoria Regional Health Centre Not yet recruiting Barrie, Ontario, Canada William Osler Health System Not yet recruiting Brampton, Ontario, Canada Grand River Regional Cancer Centre Recruiting Kitchener, Ontario, Canada London Health Sciences Centre Not yet recruiting London, Ontario, Canada Thunder Bay Regional Health Sciences Centre Not yet recruiting Thunder Bay, Ontario, Canada St. Michael's Hospital Not yet recruiting Toronto, Ontario, Canada Sunnybrook Health Sciences Center Not yet recruiting Toronto, Ontario, Canada Windsor Regional Cancer Centre Recruiting Windsor, Ontario, Canada Canada, Quebec Centre Integre de Sante et de Services Sociaux de la Monteregie-Centre Not yet recruiting Greenfield Park, Quebec, Canada Cisss de Chaudiere-Appalaches Not yet recruiting Lévis, Quebec, Canada Segal Cancer Centre-Jewish General Hospital Not yet recruiting Montréal, Quebec, Canada Centre de recherche du CHUS and Hopital Fleurimont Not yet recruiting Sherbrooke, Quebec, Canada Canada, Saskatchewan Saskatoon Cancer Centre Not yet recruiting Saskatoon, Saskatchewan, Canada Collapse <<
NCT03367572	Breast Carcinoma	Phase 3	Recruiting	May 1, 2023	United States, New York ... more >> University of Rochester NCORP Research Base Recruiting Rochester, New York, United States, 14642 Contact: Joseph Roscoe 585-275-5513 joseph_roscoe@urmc.rochester.edu Principal Investigator: Joseph Roscoe Collapse <<
NCT03668639	Chemotherapy-induced Nausea an... more >>d Vomiting Adverse Event Cervical Cancer Collapse <<	Phase 2 Phase 3	Recruiting	February 15, 2020	Denmark ... more >> Department of Oncology, Odense University Hospital Recruiting Odense, Denmark, 5000 Contact: Christina H. Ruhlmann, MD, PhD 22314446 ext +45 christina.ruhlmann@rsyd.dk Contact: Annemieke Sibtsen, RN 29427758 ext +45 Annemieke.Sibtsen@rsyd.dk Principal Investigator: Christina H. Ruhlmann, MD, PhD Sub-Investigator: Anja Ør Knudsen, MD Collapse <<
NCT01376297	-	-	Completed	-	-
NCT03008213	Chemotherapy Induced Nausea Vo... more >>miting Collapse <<	Phase 2	Not yet recruiting	June 2020	-
NCT03040726	In Situ Neoplasm ... more >> Malignant Neoplasms Nausea and Vomiting, Chronic Collapse <<	Phase 2 Phase 3	Recruiting	May 2019	United States, Texas ... more >> University of Texas MD Anderson Cancer Center Recruiting Houston, Texas, United States, 77030 Contact: Clinical Research Operations CR_Study_Registration@mdanderson.org Collapse <<
NCT03403712	Chemotherapy-induced Nausea an... more >>d Vomiting Collapse <<	Phase 3	Recruiting	October 2018	-
NCT02517021	-	-	Completed	-	-
NCT02517021	Chemotherapy-Induced Nausea an... more >>d Vomiting Collapse <<	Phase 3	Completed	-	-
NCT03204279	Chemotherapy-induced Nausea an... more >>d Vomiting (CINV) Collapse <<	Phase 2	Recruiting	January 2019	United States, Delaware ... more >> Nemours/A.I. duPont Hospital for Children Recruiting Wilmington, Delaware, United States, 19803 Contact: Emi Caywood, MD 302-651-5500 ecaywood@nemours.org United States, Florida Nemours Children's Clinic Recruiting Jacksonville, Florida, United States, 32207 Contact: Manisha Bansal, MD 904-697-3896 mbansal@nemours.org Nemours Children's Hospital - Orlando Recruiting Orlando, Florida, United States, 32827 Contact: Ramamoorthy Nagasubramanian, MD 407-650-7652 rnagasub@nemours.org United States, Maine Maine Medical Center - Cancer Medicine and Blood Disorders - Scarborough Recruiting Scarborough, Maine, United States, 04074 Contact: Stanley Chaleff, MD 207-885-7565 Chales1@mmc.org United States, South Carolina Medical University of South Carolina Recruiting Charleston, South Carolina, United States, 29425 Contact: Jacqueline Kraveka, MD 843-792-2957 kravekjm@musc.edu Russian Federation Chelyabinsk Regional Children's Clinical Hospital Recruiting Chelyabinsk, Russian Federation Contact: Elena Basharova, Dr +7 (351) 261 1371 lbasharova@mail.ru Children's Territorial Clinical Hospital Recruiting Krasnodar, Russian Federation Contact: Mikhail Melnikov, Dr. +7 (861) 268 5214 kkdkb@mail.ru Dmitry Rogachev National Scientific and Practical Center for Pediatric Hematology, Oncology and Immunology Recruiting Moscow, Russian Federation Contact: Alexey Maschan, Prof. +7 (495) 936 9169 amaschan@mail.ru City Clinical Hospital #31 Recruiting St. Petersburg, Russian Federation Contact: Margarita Belogurova, Prof. +7 (812) 235 0721 deton.hospital31@inbox.ru First I.P. Pavlov State Medical University of St. Petersburg Recruiting St. Petersburg, Russian Federation Contact: Lyudmila Zubarovskaya, Dr. +7 (812) 233 4473 zubarovskaya_ls@mail.ru Voronezh Regional Children's Cinical Hospital #1 Recruiting Voronezh, Russian Federation, 394024 Contact: Natalia B Yudina, MD 7 (910) 732 14 21 n.yudina@list.ru Regional Children's Clinical Hospital #1 Recruiting Yekaterinburg, Russian Federation Contact: Oleg Arakaev, Dr +8 (343) 216 68 97 olegarakaev@gmail.com Serbia University Children's Hospital, Center for Pediatrics, Department of Hematology and Oncology Recruiting Belgrade, Serbia Contact: Dragana Janic, Dr. +381 (11) 206 0691 drjanic@eunet.rs Clinical Center Nis, Clinic of Pediatric Internal Diseases Recruiting Nis, Serbia Contact: Vesna Bogicevic, Dr. +381 (64) 181 0880 vajav@mts.rs Ukraine Dnipropetrovsk Regional Children's Clinical Hospital Recruiting Dnipro, Ukraine, 49100 Contact: Natalia A. Dementieva, MD +380 (56) 713 7100 dementievana@ukr.net; k7-dodkb@yandex.ru National Institute of Cancer, Research Department of Pediatric Oncology Recruiting Kyiv, Ukraine Contact: Hryhorii Klymniuk, MD +380 (44) 259 0185 gklymnyuk@gmail.com West Ukrainian Specialized Children's Medical Center, Department of Pediatric Surgery Recruiting Lviv, Ukraine Contact: Zoriana Kizyma, MD +380 (322) 702 079 zoryanakizyma@gmail.com Collapse <<

Netupitant/奈妥吡坦 Catalog No. CSN16120

靶点选择性

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