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

Gefapixant citrate  (Synonyms: MK-7264 citrate; AF-219 citrate)

Cat. No.: HY-101588A Purity: 99.23%
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Gefapixant citrate 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 citrate can be used for the research of chronic cough and knee osteoarthritis.

For research use only. We do not sell to patients.

Gefapixant citrate Chemical Structure

Gefapixant citrate Chemical Structure

CAS No. : 2310299-91-1

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Based on 1 publication(s) in Google Scholar

Other Forms of Gefapixant citrate:

Gefapixant citrate Related Antibodies

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Description

Gefapixant citrate 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 citrate can be used for the research of chronic cough and knee osteoarthritis[1][2][3].

IC50 & Target

P2X3 Receptor

 

In Vitro

Gefapixant citrate 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 citrate Related Antibodies
In Vivo

Gefapixant citrate (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.
Clinical Trial
Molecular Weight

545.52

Formula

C20H27N5O11S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(CC(C(O)=O)(CC(O)=O)O)O.O=S(N)(C1=C(OC)C=C(C(C)C)C(OC2=CN=C(N)N=C2N)=C1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 350 mg/mL (641.59 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 1.8331 mL 9.1656 mL 18.3311 mL
5 mM 0.3666 mL 1.8331 mL 3.6662 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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 Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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(per animal)

g

Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8331 mL 9.1656 mL 18.3311 mL 45.8278 mL
5 mM 0.3666 mL 1.8331 mL 3.6662 mL 9.1656 mL
10 mM 0.1833 mL 0.9166 mL 1.8331 mL 4.5828 mL
15 mM 0.1222 mL 0.6110 mL 1.2221 mL 3.0552 mL
20 mM 0.0917 mL 0.4583 mL 0.9166 mL 2.2914 mL
25 mM 0.0733 mL 0.3666 mL 0.7332 mL 1.8331 mL
30 mM 0.0611 mL 0.3055 mL 0.6110 mL 1.5276 mL
40 mM 0.0458 mL 0.2291 mL 0.4583 mL 1.1457 mL
50 mM 0.0367 mL 0.1833 mL 0.3666 mL 0.9166 mL
60 mM 0.0306 mL 0.1528 mL 0.3055 mL 0.7638 mL
80 mM 0.0229 mL 0.1146 mL 0.2291 mL 0.5728 mL
100 mM 0.0183 mL 0.0917 mL 0.1833 mL 0.4583 mL
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Gefapixant citrate 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:

Gefapixant2310299-91-1MK-7264AF-219MK7264MK 7264AF219AF 219P2X ReceptorP2XRschronic coughknee osteoarthritisP2X receptorP2X3Inhibitorinhibitorinhibit

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