2. GPCR/G Protein Neuronal Signaling
  3. Neurokinin Receptor
  4. Pavinetant

Pavinetant  (Synonyms: MLE-4901; AZD2624; AZD4901)

Cat. No.: HY-14432 Purity: 99.83%
SDS COA Handling Instructions

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Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.

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

Pavinetant Chemical Structure

Pavinetant Chemical Structure

CAS No. : 941690-55-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 222 In-stock
Solution
10 mM * 1 mL in DMSO USD 222 In-stock
Solid
5 mg USD 220 In-stock
10 mg USD 330 In-stock
50 mg USD 550 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Pavinetant Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Pavinetant

View All Neurokinin Receptor Isoform Specific Products:

View All Isoforms
NK1 NK2 NK3

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.

IC50 & Target

NK3

 

Cellular Effect
Cell Line Type Value Description References
CHO IC50
1.6 nM
Compound: AZD2624; AZD4901
Displacement of [125I]His3-MePhe7)-NKB from human NK3R expressed in CHO cell membranes by topcounting method
Displacement of [125I]His3-MePhe7)-NKB from human NK3R expressed in CHO cell membranes by topcounting method
[PMID: 27298001]
In Vitro

Pavinetant (AZD2624) is a potent and selective NK3 receptor antagonist which is developed for the treatment of schizophrenia. Pavinetant exhibits an inhibitory effect on microsomal CYP3A4/5 activities with apparent IC50 values of 7.1 and 19.8 μM for midazolam and testosterone assays, respectively. No time-dependent inactivation of CYP3A4/5 activity by Pavinetant is observed. Pavinetant demonstrates weak to no inhibition of CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, and CYP2D6[1].

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

Pavinetant Related Antibodies
Clinical Trial
Molecular Weight

459.56

Formula

C26H25N3O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC[C@H](NC(C1=C(C=CC=C2)C2=NC(C3=CC=CC=C3)=C1NS(C)(=O)=O)=O)C4=CC=CC=C4
Shipping

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

DMSO : ≥ 50 mg/mL (108.80 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1760 mL 10.8800 mL 21.7599 mL
5 mM 0.4352 mL 2.1760 mL 4.3520 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.

  • Molarity Calculator

  • Dilution Calculator

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: ≥ 3 mg/mL (6.53 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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% Corn Oil

    Solubility: ≥ 3 mg/mL (6.53 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Purity: 99.83%

SDS (252 KB)

COA (258 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

The potential of Pavinetant (AZD2624) to cause time-dependent inhibition of CYP3A activities is evaluated by pre-incubating 10 μM of Pavinetant at 37°C for 0, 3, 10, 20, and 30 min in 0.1 M pH 7.4 phosphate buffer incubation mixture (0.2 mL) containing 2 mg/mL HLM and 1 mM NADPH. Verapamil, tested at 10 μM, is also incubated separately as a positive control. An aliquot of 20 μL is removed from pre-incubation tube at each time point and added to a secondary 5-min incubation (180 μL) containing 15 μM of midazolam and 1 mM of NADPH. The formation of 1′-hydroxymidazolam is used as the marker activity for CYP3A enzymes and analyzed using LC-MS. CYP3A enzyme activities after pre-incubation with Pavinetant are compared to activities following incubation with vehicle solvent (1% methanol) and without pre-incubation[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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, 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 2.1760 mL 10.8800 mL 21.7599 mL 54.3999 mL
5 mM 0.4352 mL 2.1760 mL 4.3520 mL 10.8800 mL
10 mM 0.2176 mL 1.0880 mL 2.1760 mL 5.4400 mL
15 mM 0.1451 mL 0.7253 mL 1.4507 mL 3.6267 mL
20 mM 0.1088 mL 0.5440 mL 1.0880 mL 2.7200 mL
25 mM 0.0870 mL 0.4352 mL 0.8704 mL 2.1760 mL
30 mM 0.0725 mL 0.3627 mL 0.7253 mL 1.8133 mL
40 mM 0.0544 mL 0.2720 mL 0.5440 mL 1.3600 mL
50 mM 0.0435 mL 0.2176 mL 0.4352 mL 1.0880 mL
60 mM 0.0363 mL 0.1813 mL 0.3627 mL 0.9067 mL
80 mM 0.0272 mL 0.1360 mL 0.2720 mL 0.6800 mL
100 mM 0.0218 mL 0.1088 mL 0.2176 mL 0.5440 mL
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Pavinetant 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:

Pavinetant941690-55-7MLE-4901 AZD2624 AZD4901MLE4901MLE 4901AZD2624AZD 2624AZD-2624AZD4901AZD 4901AZD-4901Neurokinin ReceptorNK receptorTachykinin receptorInhibitorinhibitorinhibit

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