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

Camlipixant  (Synonyms: BLU-5937)

Cat. No.: HY-136026 Purity: 99.94%
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Camlipixant (BLU-5937) a potent, selective, non-competitive and orally active P2X3 homotrimeric receptor antagonist with an IC50 of 25 nM against hP2X3 homotrimeric. Camlipixant shows potent anti-tussive effect and no taste alteration. Camlipixant can be used for the research of unexplained, refractory chronic cough.

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

Camlipixant Chemical Structure

Camlipixant Chemical Structure

CAS No. : 1621164-74-6

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 293 In-stock
Solution
10 mM * 1 mL in DMSO USD 293 In-stock
Solid
1 mg USD 120 In-stock
5 mg USD 290 In-stock
10 mg USD 470 In-stock
25 mg USD 890 In-stock
50 mg USD 1420 In-stock
100 mg USD 2250 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

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Based on 1 publication(s) in Google Scholar

Camlipixant Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Camlipixant (BLU-5937) a potent, selective, non-competitive and orally active P2X3 homotrimeric receptor antagonist with an IC50 of 25 nM against hP2X3 homotrimeric. Camlipixant shows potent anti-tussive effect and no taste alteration. Camlipixant can be used for the research of unexplained, refractory chronic cough[1].

IC50 & Target

IC50: 25 nM (hP2X3), >24000 nM (hP2X2/3), 92 nM (rP2X3), 1820 nM (rP2X2/3), 126 nM (gpP2X3), 3450 nM (gpP2X2/3)[1]
In Vitro

Camlipixant (BLU-5937; 500 nM) blocks ATP-mediated dorsal root ganglion (DRG) neuron sensitization[1].

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

Camlipixant Related Antibodies
In Vivo

Camlipixant (BLU-5937; 3-30 mg/kg; oral) reduces histamine- and ATP- induced cough hypersensitivity in guinea pigs[1].
Camlipixant (BLU-5937; 10-20 mg/kg; i.p.) does not alter taste perception as compared to control animals[1].
Camlipixant (BLU-5937) exhibits excellent drug-like characteristics, including good oral bioavailability, low predicted clearance in human, no blood-brain barrier permeability and high safety margin versus human predicted efficacious exposure[1].

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

Animal Model: Male Dunkin Hartley guinea pigs[1]
Dosage: 0.3, 3, 30 mg/kg
Administration: PO, approximately 2 h prior to tussive agent exposure
Result: Significantly reduced the histamine-induced enhancement in the number of citric acid-induced coughs. Reduced significantly and dose-dependently the ATP-induced enhancement of citric acid-induced coughs.
Clinical Trial
Molecular Weight

458.46

Formula

C23H24F2N4O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1C[C@H](CC2=C(C3=C(F)C=C(C(NC)=O)C=C3F)N=C4C=C(C)C=CN42)OCC1)OC
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 : 100 mg/mL (218.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

DMSO : 100 mg/mL (218.12 mM; ultrasonic and adjust pH to 3 with 1M HCl; 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 2.1812 mL 10.9061 mL 21.8122 mL
5 mM 0.4362 mL 2.1812 mL 4.3624 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:

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
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 / DMSO 1 mM 2.1812 mL 10.9061 mL 21.8122 mL 54.5304 mL
5 mM 0.4362 mL 2.1812 mL 4.3624 mL 10.9061 mL
10 mM 0.2181 mL 1.0906 mL 2.1812 mL 5.4530 mL
15 mM 0.1454 mL 0.7271 mL 1.4541 mL 3.6354 mL
20 mM 0.1091 mL 0.5453 mL 1.0906 mL 2.7265 mL
25 mM 0.0872 mL 0.4362 mL 0.8725 mL 2.1812 mL
30 mM 0.0727 mL 0.3635 mL 0.7271 mL 1.8177 mL
40 mM 0.0545 mL 0.2727 mL 0.5453 mL 1.3633 mL
50 mM 0.0436 mL 0.2181 mL 0.4362 mL 1.0906 mL
60 mM 0.0364 mL 0.1818 mL 0.3635 mL 0.9088 mL
80 mM 0.0273 mL 0.1363 mL 0.2727 mL 0.6816 mL
100 mM 0.0218 mL 0.1091 mL 0.2181 mL 0.5453 mL
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Camlipixant 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:

Camlipixant1621164-74-6BLU-5937BLU5937BLU 5937P2X ReceptorP2XRsrefractory chronic coughcough hypersensitivityno blood-brain barrier permeabilitygood oral bioavailabilityInhibitorinhibitorinhibit

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