Gefapixant
- Product Name
- Gefapixant
- CAS No.
- 1015787-98-0
- Chemical Name
- Gefapixant
- Synonyms
- Gefapixant;MK-7264;MK7264;MK 7264;CS-2846;EOS-6104;EOS-61047;RO-4926219;Gefapixant(AF-219;Gefapixant (MK-7264)
- CBNumber
- CB42596673
- Molecular Formula
- C14H19N5O4S
- Formula Weight
- 353.4
- MOL File
- 1015787-98-0.mol
Gefapixant Property
- Boiling point:
- 606.3±65.0 °C(Predicted)
- Density
- 1.391±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:38.0(Max Conc. mg/mL);107.53(Max Conc. mM)
- pka
- 9.90±0.60(Predicted)
- form
- Solid
- color
- White to off-white
- InChI
- InChI=1S/C14H19N5O4S/c1-7(2)8-4-10(22-3)12(24(17,20)21)5-9(8)23-11-6-18-14(16)19-13(11)15/h4-7H,1-3H3,(H2,17,20,21)(H4,15,16,18,19)
- InChIKey
- HLWURFKMDLAKOD-UHFFFAOYSA-N
- SMILES
- C1(S(N)(=O)=O)=CC(OC2=CN=C(N)N=C2N)=C(C(C)C)C=C1OC
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304IF INHALED:
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P312Call a POISON CENTER or doctor/physician if you feel unwell.
P321Specific treatment (see … on this label).
P330Rinse mouth.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P340Remove victim to fresh air and keep at rest in a position comfortable for breathing.
P362Take off contaminated clothing and wash before reuse.
P403Store in a well-ventilated place.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 40825
- Product name
- Gefapixant
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $28
- Updated
- 2026/04/30
- Product number
- 40825
- Product name
- Gefapixant
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $90
- Updated
- 2026/04/30
- Product number
- 40825
- Product name
- Gefapixant
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $138
- Updated
- 2026/04/30
- Product number
- 40825
- Product name
- Gefapixant
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $275
- Updated
- 2026/04/30
- Product number
- CS-0021727
- Product name
- Gefapixant
- Purity
- 99.62%
- Packaging
- 25mg
- Price
- $320
- Updated
- 2021/12/16
Gefapixant Chemical Properties,Usage,Production
Description
Gefapixant was approved in Japan in 2022 for adult patients with refractory or unexplained chronic cough, marketed under the name Lyfnua.The drug was authorised by the European Medicines Agency (EMA) in September 2023 for the same indication. However, the FDA refused to approve gefapixant for the treatment of adults with refractory or unexplained chronic cough.
Uses
Gefapixant is an orally active and potent purinergic P2X3 receptor (P2X3R) antagonist, with IC50 values of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors. Gefapixant can be used for the research of chronic cough and knee osteoarthritis.
Mechanism of action
Gefapixen is an orally available, selective P2X3 receptor antagonist used to treat cough-related conditions such as chronic cough and refractory cough. The P2X3 receptor is an ion channel expressed in sensory neurons that plays a key role in the transmission of pain and cough reflexes. Gefapixen reduces the activation of cough receptors by specifically blocking the P2X3 receptor, thereby alleviating cough symptoms.
Pharmacokinetics
Gefapixant exerts its therapeutic effects via suppressing the cough reflex initiated by sensory C fibers of the vagus nerve. In clinical studies, patients experienced a significant reduction in 24-hour cough frequency compared to placebo - this reduction was apparent by Week 4 and persisted throughout the remainder of the primary efficacy period. As renal excretion is the primary route of elimination for gefapixant, patients with severe renal impairment (eGFR < 30 mL/min/1.73m2) may require dose adjustment to maintain appropriate systemic exposures.
in vivo
Gefapixant (7d bid, orally) attenuates the weight bearing laterality with complete reversal of apparent hyperalgesia at the two higher doses in a rat model of knee osteoarthritis (14d following intra-articular administration of monoiodoacetate)[2].
IC 50
P2X3 Receptor
Gefapixant Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from Gefapixant manufacturers
- Product
- 5-(2,4-DiaMino-pyriMidin-5-yloxy)-4-isopropyl-2-Methoxy-benzenesulfonaMide 1015787-98-0
- Price
- US $9.80/KG
- Min. Order
- 1g
- Purity
- ≥99%
- Supply Ability
- 100kg
- Release date
- 2020-01-08