2. Membrane Transporter/Ion Channel
  3. P2X Receptor
  4. Gefapixant

Gefapixant (MK-7264) est un antagoniste des récepteurs P2X3 (P2X3R) qui est oralement actif avec des IC50s de ~ 30 nM par rapport aux homotrimères hP2X3 recombinants et 100-250 nM à hP2X2/3 récepteurs hétérotrimériques.

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.

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Gefapixant

Gefapixant Estructura química

No. CAS : 1015787-98-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO En stock
Solid
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Revisión del cliente

Based on 2 publication(s) in Google Scholar

Other Forms of Gefapixant:

Gefapixant Related Antibodies

Top Publications Citing Use of Products

Ver todos los productos específicos de isoformas P2X Receptor:

Ver todas las isoformas
P2X1 Receptor P2X2 Receptor P2X3 Receptor P2X4 Receptor P2X7 Receptor

  • Actividad biológica

  • Protocolo

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  • Referencias

  • Revisión del cliente

Descripciòn

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[1][2][3].

IC50 & Target

P2X3 Receptor

 

In Vitro

Gefapixant displays no inhibitory impact on any non-P2X3 subunit containing receptors (IC50 values >10,000 nM at recombinant homotrimeric hP2X1, hP2X2, hP2X4, rP2X5 and hP2X7 channels)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Gefapixant Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
Peso molecular

353.40

Fòrmula

C14H19N5O4S
No. CAS
Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC(OC2=CN=C(N)N=C2N)=C(C(C)C)C=C1OC)(N)=O
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvente y solubilidad
In Vitro: 

DMSO : 29.17 mg/mL (82.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8297 mL 14.1483 mL 28.2965 mL
5 mM 0.5659 mL 2.8297 mL 5.6593 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Calculadora de molaridad

  • Calculadora de dilución

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% PBS

    Solubility: ≥ 2.5 mg/mL (7.07 mM); Clear solution

  • Protocol 2

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (5.89 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación

Purity: 99.93%

SDS (393 KB)

COA (257 KB) HNMR (258 KB) LCMS (94 KB)

Instrucciones de manejo (2659 KB)
Referencias
Administraciòn de animales
[2]

Rats[2]
A rodent model often employs for assessing potential for drug effect in osteoarthritis (OA) pain is based on intraarticular injection of monoiodoacetate (mIOA) into one knee joint of the rat. Progressive loss of chondrocytes leads to histological changes of the articular cartilage over subsequent weeks that resemble the changes which occur in human OA, leading to joint discomfort exemplified by a shift in the weight distribution (asymmetry) to favor the unaffected limb. To measure the effect of Gefapixant on the weight bearing laterality and apparent hyperalgesia, Gefapixant is given by intraplantar or oral administration to the rats, with different concentrations (6, 20, and 60 mg/kg) two times a day and continues up to a week[2].

MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Referencias

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8297 mL 14.1483 mL 28.2965 mL 70.7414 mL
5 mM 0.5659 mL 2.8297 mL 5.6593 mL 14.1483 mL
10 mM 0.2830 mL 1.4148 mL 2.8297 mL 7.0741 mL
15 mM 0.1886 mL 0.9432 mL 1.8864 mL 4.7161 mL
20 mM 0.1415 mL 0.7074 mL 1.4148 mL 3.5371 mL
25 mM 0.1132 mL 0.5659 mL 1.1319 mL 2.8297 mL
30 mM 0.0943 mL 0.4716 mL 0.9432 mL 2.3580 mL
40 mM 0.0707 mL 0.3537 mL 0.7074 mL 1.7685 mL
50 mM 0.0566 mL 0.2830 mL 0.5659 mL 1.4148 mL
60 mM 0.0472 mL 0.2358 mL 0.4716 mL 1.1790 mL
80 mM 0.0354 mL 0.1769 mL 0.3537 mL 0.8843 mL
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Gefapixant Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Gefapixant1015787-98-0MK-7264 AF-219MK7264MK 7264AF219AF 219AF-219P2X ReceptorP2XRschronic coughknee osteoarthritisP2X receptorP2X3Inhibitorinhibitorinhibit

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Nombre del producto:
Gefapixant
Cat. No.:
HY-101588
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