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Chemical Structure| 1015787-98-0 Chemical Structure| 1015787-98-0

Structure of Gefapixant
CAS No.: 1015787-98-0

Chemical Structure| 1015787-98-0

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Gefapixant is an orally active P2X3 receptor (P2X3R) antagonist with IC50 values of approximately 30 nM and 100-250 nM for recombinant human hP2X3 and hP2X2/3, respectively. Gefapixant can be used for research in chronic cough and knee osteoarthritis.

Synonyms: MK-7264; AF-219

4.5 *For Research Use Only !

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Product Details of Gefapixant

CAS No. :1015787-98-0
Formula : C14H19N5O4S
M.W : 353.40
SMILES Code : O=S(C1=CC(OC2=CN=C(N)N=C2N)=C(C(C)C)C=C1OC)(N)=O
Synonyms :
MK-7264; AF-219
MDL No. :MFCD24539325
InChI Key :HLWURFKMDLAKOD-UHFFFAOYSA-N
Pubchem ID :24764487

Safety of Gefapixant

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P264-P270-P271-P280-P301+P312-P302+P352-P304-P304+P340-P305+P351+P338-P312-P321-P330-P332+P313-P337+P313-P340-P362-P403-P403+P233-P405-P501

Isoform Comparison

Biological Activity

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02612623 Refractory Chronic Cough Phase 2 Completed - United States, California ... More >> 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 Less <<
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 ... More >> North West Lung Research Centre, Wythenshawe Hospital Manchester, United Kingdom, M23 9LT Less <<
NCT03449134 Chronic Cough Phase 3 Recruiting July 10, 2020 -
NCT02612610 - Completed - -
NCT01569438 Bladder Pain Syndrome Phase 2 Completed - -
NCT02502097 Idiopathic Pulmonary Fibrosis ... More >> Cough Less << Phase 2 Completed - -
NCT02349425 Refractory Chronic Cough Phase 2 Completed - -
NCT03654326 Endometriosis-related Pain Phase 2 Recruiting October 22, 2019 -
NCT03108924 Renal Insufficiency PHASE1 COMPLETED 2017-09-13 Clinical Pharmacology of Miami... More >> ( Site 0001), Hialeah, Florida, 33014, United States|Orlando Clinical Research Center ( Site 0002), Orlando, Florida, 32809, United States Less <<
NCT03449147 Chronic Cough Phase 3 Recruiting January 8, 2021 -
NCT03569033 Acute Cough Phase 2 Recruiting June 21, 2019 United Kingdom ... More >> Hvivo Service Limited. Queen Mary BioEnterprises ( Site 0003) Recruiting London, United Kingdom, E1 2AX Contact: Study Coordinator    +442077561300 Less <<
NCT02476890 Refractory Chronic Cough Phase 2 Completed - -
NCT02790840 Healthy Phase 1 Completed - United States, Arizona ... More >> Celerion Tempe, Arizona, United States, 85283 Less <<
NCT03696108 Chronic Cough Phase 3 Recruiting October 6, 2020 Japan ... More >> 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 Less <<
NCT02492776 Healthy Phase 1 Completed - United States, Arizona ... More >> Celerion Tempe, Arizona, United States, 85283 Less <<
NCT01993329 Asthma Phase 1 Completed - United Kingdom ... More >> Medicines Evaluation Unit Manchester, United Kingdom, M23 9QZ Less <<
NCT02477709 Idiopathic Pulmonary Fibrosis PHASE2 COMPLETED 2015-08-21 American Health Research, Char... More >>lotte, North Carolina, 28207, United States Less <<
NCT02476890 - Completed - -
NCT02477709 Idiopathic Pulmonary Fibrosis PHASE2 COMPLETED 2015-08-21 American Health Research, Char... More >>lotte, North Carolina, 28207, United States Less <<
NCT02229877 Healthy Volunteers Phase 1 Completed - United States, Arizona ... More >> Celerion Tempe, Arizona, United States, 85283 Less <<
NCT02397460 Refractory Chronic Cough Phase 2 Completed - United Kingdom ... More >> The Medicines Evaluation Unit Manchester, United Kingdom, M23 9QZ Less <<
NCT03482713 Chronic Cough Phase 2 Completed - Japan ... More >> 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 Less <<
NCT05813223 Chronic Cough EARLY_PHASE1 RECRUITING 2026-06-30 The University of Melbourne, P... More >>arkville, Victoria, 3010, Australia Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 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

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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