2. GPCR/G Protein Neuronal Signaling Metabolic Enzyme/Protease
  3. Neurokinin Receptor Cytochrome P450
  4. Casopitant mesylate

Casopitant mesylate  (Synonyms: GW679769B)

Cat. No.: HY-14405A Purity: 99.84%
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Casopitant mesylate (GW679769B) is a potent, selective, brain permeable and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant mesylate is a second in the class of antiemetics that acts to antagonise the emetogenic effect of substance P. Casopitant mesylate is also a substrate and a weak-to-moderate inhibitor of CYP3A4. Casopitant mesylate can be used for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV).

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

Casopitant mesylate Chemical Structure

Casopitant mesylate Chemical Structure

CAS No. : 414910-30-8

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5 mg USD 400 In-stock
10 mg USD 640 In-stock
25 mg USD 1300 In-stock
50 mg USD 2100 In-stock
100 mg USD 3360 In-stock
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Based on 1 publication(s) in Google Scholar

Casopitant mesylate Related Antibodies

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View All Cytochrome P450 Isoform Specific Products:

View All Isoforms
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP2D6 CYP3A4 CYP17A1

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Description

Casopitant mesylate (GW679769B) is a potent, selective, brain permeable and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant mesylate is a second in the class of antiemetics that acts to antagonise the emetogenic effect of substance P. Casopitant mesylate is also a substrate and a weak-to-moderate inhibitor of CYP3A4. Casopitant mesylate can be used for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV)[1][2].

IC50 & Target[1]

NK1

 

CYP3A4

 

In Vivo

In a ferret-model of Cisplatin- induced emesis, Casopitant (GW679769) inhibits retching and vomiting and reduced nausea-like behaviours in a dose-dependent manner. The pharmacokinetics and brain penetration of casopitant are studied in the ferret-model of cisplatin-induced emesis. Following a single intraperitoneal dose, radioactive labeled Casopitant ([14C]Casopitant) is rapidly absorbed, with plasma and brain concentrations being approximately equal at two hours post-dosing. [14C]Casopitant is found in the brain as the parent compound and two major oxidative metabolites (M1 and M2), accounting for approximately 76%, 19%, and 3% of the radioactivity, respectively; suggesting that the pharmacologic activity of Casopitant in the ferret is largely attributable to the parent compound. Casopitant possesses a high affinity for brain NK1 receptors in the ferret[2].

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

712.72

Formula

C31H39F7N4O5S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1[C@@H](C2=CC=C(F)C=C2C)C[C@@H](N3CCN(C(C)=O)CC3)CC1)N([C@@H](C4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4)C)C.CS(=O)(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (46.76 mM; ultrasonic and warming and heat to 60°C; 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 1.4031 mL 7.0154 mL 14.0308 mL
5 mM 0.2806 mL 1.4031 mL 2.8062 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 (sealed storage, away from moisture). 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: ≥ 0.71 mg/mL (1.00 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.71 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.1 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: ≥ 0.71 mg/mL (1.00 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.71 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.1 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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 (sealed storage, away from moisture). 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 1.4031 mL 7.0154 mL 14.0308 mL 35.0769 mL
5 mM 0.2806 mL 1.4031 mL 2.8062 mL 7.0154 mL
10 mM 0.1403 mL 0.7015 mL 1.4031 mL 3.5077 mL
15 mM 0.0935 mL 0.4677 mL 0.9354 mL 2.3385 mL
20 mM 0.0702 mL 0.3508 mL 0.7015 mL 1.7538 mL
25 mM 0.0561 mL 0.2806 mL 0.5612 mL 1.4031 mL
30 mM 0.0468 mL 0.2338 mL 0.4677 mL 1.1692 mL
40 mM 0.0351 mL 0.1754 mL 0.3508 mL 0.8769 mL
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Casopitant mesylate 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:

Casopitant414910-30-8GW679769BNeurokinin ReceptorCytochrome P450NK receptorTachykinin receptorCYPsChemotherapyNK1antiemeticssafetyCYP3A4substance-PPONVCINVbrainpermeableInhibitorinhibitorinhibit

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