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

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

Cat. No.: HY-14432 Purity: 99.83%
COA 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
Solid + Solvent
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
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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

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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].

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

Appearance

Solid

Formula

C26H25N3O3S
CAS No.
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)

*"≥" 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
10 mM 0.2176 mL 1.0880 mL 2.1760 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation
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
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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.

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  • Dilution Calculator

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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

Keywords:

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

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