1. GPCR/G Protein
    Neuronal Signaling
  2. Neurokinin Receptor

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

Cat. No.: HY-14432 Purity: 99.74%
Handling Instructions

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
10 mM * 1 mL in DMSO USD 317 In-stock
Estimated Time of Arrival: December 31
5 mg USD 288 In-stock
Estimated Time of Arrival: December 31
10 mg USD 516 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1056 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3000 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target

NK3R[1]

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].

Clinical Trial
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
Molecular Weight

459.56

Formula

C₂₆H₂₅N₃O₃S

CAS No.

941690-55-7

SMILES

CC[[email protected]](NC(C1=C(C=CC=C2)C2=NC(C3=CC=CC=C3)=C1NS(C)(=O)=O)=O)C4=CC=CC=C4

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Pavinetant
Cat. No.:
HY-14432
Quantity:

Pavinetant

Cat. No.: HY-14432