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

Fosaprepitant dimeglumine  (Synonyms: MK-0517; L785298)

Cat. No.: HY-14407A Purity: 98.02%
SDS COA Handling Instructions

Molarity Calculator

Fosaprepitant dimeglumine (MK-0517) is a proagent of Aprepitant (HY-10052). Fosaprepitant dimeglumine is a neurokinin-1 receptor antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV).

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

Fosaprepitant dimeglumine Chemical Structure

Fosaprepitant dimeglumine Chemical Structure

CAS No. : 265121-04-8

Size Price Stock Quantity
5 mg USD 55 In-stock
10 mg USD 75 In-stock
50 mg USD 270 In-stock
100 mg USD 450 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.

Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Fosaprepitant dimeglumine:

Fosaprepitant dimeglumine Related Antibodies

Top Publications Citing Use of Products

2 Publications Citing Use of MCE Fosaprepitant dimeglumine

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Fosaprepitant dimeglumine (MK-0517) is a proagent of Aprepitant (HY-10052). Fosaprepitant dimeglumine is a neurokinin-1 receptor antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV)[1].

IC50 & Target

Neurokinin-1 receptor[1]
In Vivo

Fosaprepitant dimeglumine (30 mg/kg; i.p.; daily; for 7 days) attenuates tolerance to morphine and increases the antinociceptive effect in in rats[1].

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

Animal Model: Sprague-Dawley rats[1]
Dosage: 30 mg/kg
Administration: Intraperitoneal injection, daily, for 7 days
Result: Increased the antinociceptive effect of morphine compared to control group.
Clinical Trial
Molecular Weight

1004.83

Formula

C37H56F7N6O16P
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N=C(CN2[C@@H](C3=CC=C(F)C=C3)[C@@H](O[C@H](C)C4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4)OCC2)NN1P(O)(O)=O.OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)CNC.OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)CNC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (49.76 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9952 mL 4.9760 mL 9.9519 mL
5 mM 0.1990 mL 0.9952 mL 1.9904 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 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:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 100 mg/mL (99.52 mM); Clear solution; Need ultrasonic

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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 98.02%

SDS (393 KB)

COA (259 KB) RP-HPLC (246 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 0.9952 mL 4.9760 mL 9.9519 mL 24.8798 mL
5 mM 0.1990 mL 0.9952 mL 1.9904 mL 4.9760 mL
10 mM 0.0995 mL 0.4976 mL 0.9952 mL 2.4880 mL
15 mM 0.0663 mL 0.3317 mL 0.6635 mL 1.6587 mL
20 mM 0.0498 mL 0.2488 mL 0.4976 mL 1.2440 mL
25 mM 0.0398 mL 0.1990 mL 0.3981 mL 0.9952 mL
30 mM 0.0332 mL 0.1659 mL 0.3317 mL 0.8293 mL
40 mM 0.0249 mL 0.1244 mL 0.2488 mL 0.6220 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Fosaprepitant dimeglumine 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:

Fosaprepitant dimeglumine265121-04-8MK-0517 L785298MK0517MK 0517L785298L 785298L-785298Neurokinin ReceptorNK receptorTachykinin receptorAprepitantnociceptionchemotherapy-inducednauseavomitingsubstance-PreceptorantagonistneuropeptideInhibitorinhibitorinhibit

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