Free shipping on all orders over $ 500

Aprepitant

Cat. No. M1650
Aprepitant Structure
Synonym:

MK-0869, L-754030, Emend

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL USD 63  USD70 In stock
5mg USD 49.5  USD55 In stock
10mg USD 72  USD80 In stock
50mg USD 270  USD300 In stock
100mg USD 396  USD440 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Aprepitant (Emend) is an antiemetic chemical compound that belongs to a class of drugs called substance P antagonists (SPA). It mediates its effect by blocking the neurokinin 1 (NK1) receptor.Aprepitant has been shown to inhibit both the acute and delayed emesis induced by cytotoxic chemotherapeutic drugs by blocking substance P landing on receptors in the brains neurons.

Protocol
Cell Experiment
Cell lines human CAPAN pancreas, HEp-2 larynx, gastric 23132-87 and SW-403 colon carcinoma cells
Preparation method Proliferation assays.
Cell proliferation was evaluated using the tetrazolium compound 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)2-(4-sulfophenyl)-2H-tetrazolium, inner salt (MTS), according to the manufacturer’s instructions (CellTiter 96 Aqueous One Solution Cell Proliferation Assay). Cell numbers were quantified using a Coulter counter. Cells were cultured in 96-well plates: each well contained 104 cells in a total volume of 100 µl. Each assay included one plate The plate included blank wells (0 cells/0.1 ml), control wells (104 cells /0.1 ml), control wells with acetonitrylo, control wells treated with aprepitant and control wells treated with the most effective SP concentration and aprepitant. The plates were inoculated with aprepitant (5–70 µM for tumor cell lines) and were incubated for the first doubling time specific for each tumor cell line. The plates were also inoculated the most mitogenic exogenous SP nM concentration with the fifty-percent inhibition concentration (IC50) of aprepitant µM concentration approximately and without aprepitant for their first doubling times respectively. For the proliferation assay, 20 µl of the MTS reagent was added to each well 90 min before reading the samples on a multiscanner microplate reader (TECAN Spectra classic, Barcelona, Spain) at 492 nm. The quantity of product, as measured by optical density, is directly proportional to the number of living cells.
Concentrations 5-70 µM
Incubation time 2 days
Animal Experiment
Animal models acute cisplatin-induced emesis in ferrets
Formulation Methocel or PEG 300
Dosages 0.3, 1, 3mg/kg
Administration p.o. or i.v.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 534.43
Formula C23H21F7N4O3
CAS Number 170729-80-3
Purity >99%
Solubility DMSO 90 mg/mL
Storage at -20°C
References

Randomized, double-blind, placebo-controlled, phase III cross-over study evaluating the oral neurokinin-1 antagonist aprepitant in combination with a 5HT3 receptor antagonist and dexamethasone in patients with germ cell tumors receiving 5-day cisplatin combination chemotherapy regimens: a hoosier oncology group study.
Albany et al. J Clin Oncol. 2012 Aug 20. PMID: 22915652.

Prevention of Nausea and Vomiting Associated with Stem Cell Transplantation: Results of a Prospective, Randomized Trial of Aprepitant used with Highly Emetogenic Preparative Regimens.
Stiff et al. Biol Blood Marrow Transplant. 2012 Jul 31. PMID: 22863840.

Aprepitant versus ondansetron in preoperative triple-therapy treatment of nausea and vomiting in neurosurgery patients: study protocol for a randomized controlled trial.
Bergese et al. Trials. 2012 Aug 3;13(1):130. PMID: 22862827.

Randomized, double-blind comparison of oral aprepitant alone compared with aprepitant and transdermal scopolamine for prevention of postoperative nausea and vomiting.
Green et al. Br J Anaesth. 2012 Jul 24. PMID: 22831888.

Combination of aprepitant, palonosetron and dexamethasone as antiemetic prophylaxis in lung cancer patients receiving multiple cycles of cisplatin-based chemotherapy.
Longo et al. Int J Clin Pract. 2012 Aug;66(8):753-757. PMID: 22805267.

The NK-1 receptor antagonist aprepitant as a broad spectrum antitumor drug.
Munoz M, et al. Invest New Drugs. 2010 Apr;28(2):187-93. PMID: 19148578.

The novel NK1 receptor antagonist MK-0869 (L-754,030) and its water soluble phosphoryl prodrug, L-758,298, inhibit acute and delayed cisplatin-induced emesis in ferrets.
Tattersall FD, et al. Neuropharmacology. 2000 Feb 14;39(4):652-63. PMID: 10728886.

Related Neurokinin Receptor Products
[Leu31,Pro34]-NPY TFA (human,rat)

[Leu31,Pro34]-NPY TFA (human,rat) is a specific neuropeptide Y1 receptor agonist.

Vapreotide acetate

Vapreotide acetate (BMY-41606 acetate; RC160 acetate) is a neurokinin-1 (NK1) receptor antagonist with IC50 value of 330 nM.

Ibodutant

Ibodutant (MEN15596) is a potent and selective tachykinin NK2 receptor antagonist with a pKi of 10.1.

Serlopitant

Serlopitant is a selective Neurokinin-1 (NK-1) receptor antagonist.

Substance P

Substance P is a neuropeptide, acting as a neurotransmitter and as a neuromodulator.The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R).

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Aprepitant, MK-0869, L-754030, Emend supplier, Neurokinin Receptor, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.