Gefapixant | MK-7264 | P2X3 Antagonist | AmBeed-信号通路专用抑制剂

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Gefapixant {[allProObj[0].p_purity_real_show]}

货号：A503454 同义名： MK-7264;AF-219

Gefapixant 是一种口服活性的 P2X3 受体（P2X3R）拮抗剂，对重组人 hP2X3 和 hP2X2/3 的 IC50 值分别约为 30 nM 和 100-250 nM。Gefapixant 可用于慢性咳嗽和膝骨关节炎的研究。

Gefapixant 化学结构
CAS号：1015787-98-0

Gefapixant 3D分子结构
CAS号：1015787-98-0

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Gefapixant 纯度/质量文件产品仅供科研

货号：A503454 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JMC, 2024. Ambeed. [ A919389 , A918471 , A995972 ]; • Anal. Chem., 2024, 96(50): 19947-19954. Ambeed. [ A261947 , A1165388 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A220462 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A165235 , A110205 ]; • Pharmaceutics, 2024, 16(12): 1546. Ambeed. [ A272538 , A187261 , A691302 , A506702 ]; 更多 >

Gefapixant 生物活性

描述

Gefapixant is an orally effective antagonist of P2X3R, with an IC50 value of approximately 30 nM against recombinant homotrimeric hP2X3, and an IC50 value ranging from 100-250 nM against the heterotrimeric hP2X2/3 receptor. Gefapixant does not inhibit receptors containing non-P2X3 subunits, including recombinant homotrimers hP2X1, hP2X2, hP2X4, rP2X5, and hP2X7. Gefapixant is useful for research into chronic cough and knee osteoarthritis^[1]^[2]^[3].

Gefapixant 动物研究

Animal study

In a rat model of knee osteoarthritis (14 days post- intra-articular administration of monoiodoacetate), Gefapixant, administered orally twice daily, alleviates weight bearing laterality and completely reverses evident hyperalgesia at two higher doses^[2].

Gefapixant 临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02612623	Refractory Chronic Cough	Phase 2	Completed	-	United States, California ... 展开 >> Afferent Investigative Site Mission Viejo, California, United States Afferent Investigative Site San Jose, California, United States United States, Colorado Afferent Investigative Site Colorado Springs, Colorado, United States United States, Florida Afferent Investigative Site Largo, Florida, United States United States, North Carolina Afferent Investigative Site Charlotte, North Carolina, United States United States, Oklahoma Afferent Investigative Site Tulsa, Oklahoma, United States United States, Texas Afferent Investigative Site Dallas, Texas, United States Afferent Investigative Site San Antonio, Texas, United States United States, Washington Afferent Investigative Site Bellevue, Washington, United States United States, Wisconsin Afferent Investigative Site Greenfield, Wisconsin, United States 收起 <<
NCT01554579	Osteoarthritis of the Knee	Phase 2	Completed	-	-
NCT01554579	-		Completed	-	-

Gefapixant 参考文献

[1]Anthony P. Ford, et al. The therapeutic promise of ATP antagonism at P2X3 receptors in respiratory and urological disorders. Front Cell Neurosci. 2013; 7: 267.

[2]Ford AP, In pursuit of P2X3 antagonists: novel therapeutics for chronic pain and afferent sensitization. Purinergic Signal. 2012 Feb;8(Suppl 1):3-26.

[3]Martin Nguyen A, et al. Validation of a visual analog scale for assessing cough severity in patients with chronic cough. Ther Adv Respir Dis. 2021 Jan-Dec;15:17534666211049743.

Gefapixant 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.83mL

0.57mL

0.28mL

14.15mL

2.83mL

1.41mL

28.30mL

5.66mL

2.83mL

Gefapixant 技术信息

CAS号	1015787-98-0
分子式	C₁₄H₁₉N₅O₄S
分子量	353.397

别名	MK-7264;AF-219
运输	蓝冰

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place,Sealed in dry,2-8°C

溶解方案

细胞实验：

DMSO: 4 mg/mL(11.32 mM)，配合低频超声，并调节pH至5-6，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

动物实验配方

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT02612623	Refractory Chronic Cough	Phase 2	Completed	-	United States, California ... 展开 >> Afferent Investigative Site Mission Viejo, California, United States Afferent Investigative Site San Jose, California, United States United States, Colorado Afferent Investigative Site Colorado Springs, Colorado, United States United States, Florida Afferent Investigative Site Largo, Florida, United States United States, North Carolina Afferent Investigative Site Charlotte, North Carolina, United States United States, Oklahoma Afferent Investigative Site Tulsa, Oklahoma, United States United States, Texas Afferent Investigative Site Dallas, Texas, United States Afferent Investigative Site San Antonio, Texas, United States United States, Washington Afferent Investigative Site Bellevue, Washington, United States United States, Wisconsin Afferent Investigative Site Greenfield, Wisconsin, United States 收起 <<
NCT01554579	Osteoarthritis of the Knee	Phase 2	Completed	-	-
NCT01554579	-		Completed	-	-
NCT01569438	-		Completed	-	-
NCT02612610	Refractory Chronic Cough	Phase 2	Completed	-	-
NCT01432730	Chronic Cough	Phase 2	Completed	-	United Kingdom ... 展开 >> North West Lung Research Centre, Wythenshawe Hospital Manchester, United Kingdom, M23 9LT 收起 <<
NCT03449134	Chronic Cough	Phase 3	Recruiting	July 10, 2020	-
NCT02612610	-		Completed	-	-
NCT01569438	Bladder Pain Syndrome	Phase 2	Completed	-	-
NCT02502097	Idiopathic Pulmonary Fibrosis ... 展开 >> Cough 收起 <<	Phase 2	Completed	-	-
NCT02349425	Refractory Chronic Cough	Phase 2	Completed	-	-
NCT03654326	Endometriosis-related Pain	Phase 2	Recruiting	October 22, 2019	-
NCT03108924	Renal Insufficiency	Phase 1	Completed	-	United States, Florida ... 展开 >> Clinical Pharmacology of Miami ( Site 0001) Hialeah, Florida, United States, 33014 Orlando Clinical Research Center ( Site 0002) Orlando, Florida, United States, 32809 收起 <<
NCT03449147	Chronic Cough	Phase 3	Recruiting	January 8, 2021	-
NCT03569033	Acute Cough	Phase 2	Recruiting	June 21, 2019	United Kingdom ... 展开 >> Hvivo Service Limited. Queen Mary BioEnterprises ( Site 0003) Recruiting London, United Kingdom, E1 2AX Contact: Study Coordinator +442077561300 收起 <<
NCT02476890	Refractory Chronic Cough	Phase 2	Completed	-	-
NCT02790840	Healthy	Phase 1	Completed	-	United States, Arizona ... 展开 >> Celerion Tempe, Arizona, United States, 85283 收起 <<
NCT03696108	Chronic Cough	Phase 3	Recruiting	October 6, 2020	Japan ... 展开 >> Oishi Clinic ( Site 3818) Recruiting Kasuya-gun, Fukuoka, Japan, 811-2310 Contact: Study Coordinator +81929381900 Nagata Hospital ( Site 3815) Recruiting Yanagawa, Fukuoka, Japan, 832-0059 Contact: Study Coordinator +81944723501 Japan Community Health care Organization Kanazawa Hospital ( Site 3817) Recruiting Kanazawa, Ishikawa, Japan, 920-8610 Contact: Study Coordinator +81762522200 Matsusaka City Hospital ( Site 3825) Recruiting Matsusaka, Mie, Japan, 515-8544 Contact: Study Coordinator +81598231515 Sugiura Clinic ( Site 3806) Recruiting Kawaguchi, Saitama, Japan, 332-0012 Contact: Study Coordinator +81482225015 National Hospital Organization Matsue Medical Center ( Site 3848) Recruiting Matsue, Shimane, Japan, 690-8556 Contact: Study Coordinator +81852216131 Kiheibashi Otolaryngology ( Site 3828) Recruiting Kodaira, Tokyo, Japan, 187-0044 Contact: Study Coordinator +81423323387 Tochigi Takao Clinic ( Site 3833) Recruiting Kagoshima, Japan, 890-0073 Contact: Study Coordinator +81998138111 Nagano Red Cross Hospital ( Site 3859) Recruiting Nagano, Japan, 380-8582 Contact: Study Coordinator +81262264131 Saiseikai Niigata Daini Hospital ( Site 3831) Recruiting Niigata, Japan, 950-1104 Contact: Study Coordinator +81252336161 Oita Red Cross Hospital ( Site 3837) Recruiting Oita, Japan, 870-0033 Contact: Study Coordinator +81975326181 Yamagata Clinic ( Site 3813) Recruiting Oita, Japan, 870-0921 Contact: Study Coordinator +81975562456 Chibana Clinic ( Site 3809) Recruiting Okinawa, Japan, 904-2143 Contact: Study Coordinator +81989391301 Ito ENT Clinic ( Site 3816) Recruiting Shizuoka, Japan, 420-0803 Contact: Study Coordinator +81542651000 收起 <<
NCT02492776	Healthy	Phase 1	Completed	-	United States, Arizona ... 展开 >> Celerion Tempe, Arizona, United States, 85283 收起 <<
NCT01993329	Asthma	Phase 1	Completed	-	United Kingdom ... 展开 >> Medicines Evaluation Unit Manchester, United Kingdom, M23 9QZ 收起 <<
NCT02477709	Idiopathic Pulmonary Fibrosis	Phase 2	Completed	-	United States, North Carolina ... 展开 >> American Health Research Charlotte, North Carolina, United States, 28207 收起 <<
NCT02476890	-		Completed	-	-
NCT02477709	-		Completed	-	-
NCT02229877	Healthy Volunteers	Phase 1	Completed	-	United States, Arizona ... 展开 >> Celerion Tempe, Arizona, United States, 85283 收起 <<
NCT02397460	Refractory Chronic Cough	Phase 2	Completed	-	United Kingdom ... 展开 >> The Medicines Evaluation Unit Manchester, United Kingdom, M23 9QZ 收起 <<
NCT03482713	Chronic Cough	Phase 2	Completed	-	Japan ... 展开 >> Nagoya City University Hospital ( Site 3328) Nagoya, Aichi, Japan, 467-8602 Idaimae Minamiyojo Int Clinic ( Site 3321) Sapporo, Hokkaido, Japan, 064-0804 Tsumura Cardiovascular-internal-medicine Clinic ( Site 3314) Kakogawa, Hyogo, Japan, 675-0101 Hitachi, Ltd. Hitachinaka General Hospital ( Site 3301) Hitachinaka, Ibaraki, Japan, 312-0057 Saiseikai Kanazawa Hospital ( Site 3337) Kanazawa, Ishikawa, Japan, 920-0353 Komatsu Municipal Hospital ( Site 3308) Komatsu, Ishikawa, Japan, 923-8560 Kamei Internal Medicine and Respiratory Clinic ( Site 3309) Takamatsu, Kagawa, Japan, 761-8073 Yokohama City Minato Red Cross Hospital ( Site 3306) Yokohama, Kanagawa, Japan, 231-8682 Matsusaka City Hospital ( Site 3325) Matsusaka, Mie, Japan, 515-8544 Nagaoka Red Cross Hospital ( Site 3307) Nagaoka, Niigata, Japan, 940-2085 Kawaguchi Respiratory Clinic ( Site 3304) Higashiosaka, Osaka, Japan, 577-0843 Fukushima Medical University Hospital ( Site 3338) Fukushima, Japan, 960-1295 Doujin Memorial Medical Foundation, Meiwa Hospital ( Site 3310) Tokyo, Japan, 101-0041 Nihonbashi Medical & Allergy Clinic ( Site 3334) Tokyo, Japan, 103-0022 Fukuwa Clinic ( Site 3311) Tokyo, Japan, 103-0027 Showa University Hospital ( Site 3331) Tokyo, Japan, 142-8666 收起 <<

Gefapixant {[allProObj[0].p_purity_real_show]}

Gefapixant 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Gefapixant 质控信息

Gefapixant 生物活性

Gefapixant 动物研究

Gefapixant 临床研究

Gefapixant 参考文献

Gefapixant 实验方案

Gefapixant 技术信息

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Gefapixant {[allProObj[0].p_purity_real_show]}

Gefapixant 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Gefapixant 质控信息

Gefapixant 生物活性

Gefapixant 动物研究

Gefapixant 临床研究

Gefapixant 参考文献

Gefapixant 实验方案

Gefapixant 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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Gefapixant 纯度/质量文件产品仅供科研