Size | Price | Stock | Qty |
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5mg |
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Other Sizes |
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Purity: ≥98%
Fosnetupitant (07PNET; 07-PNET; Fosnetupitant chloride; Akynzeo), the prodrug of netupitant, is a novel and potent antagonist of neurokinin receptor used in combination with palonosetron to prevent nausea and vomiting caused by chemotherapy. Neurokinin 1 (NK1) receptor antagonists are a class of drug used to treat nausea and vomiting associated with chemotherapy. Aprepitant, casopitant, and fosaprepitant are NK1 drugs. As of April 2018, the combination of fosnetupitant and palonosetron has been approved by FDA to prevent acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy.
ln Vitro |
Fosnetupitant (Pronetupitant) does not bind to all other proteins investigated, but it has micromolar affinity for L-type Ca2+ channels (pKi ∼ 5.7) and 5-HT6 receptors (pKi ∼ 5.2) [1].
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ln Vivo |
Rats quickly and extensively convert Pronetupitant to Netupitant following an intravenous injection[1].
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References |
[1]. Ruzza C, et al. In vitro and in vivo pharmacological characterization of Pronetupitant, a prodrug of the neurokinin 1 receptor antagonist Netupitant. Peptides. 2015 Jul;69:26-32.
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Molecular Formula |
C31H35F6N4O5P
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Molecular Weight |
688.61
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CAS # |
1703748-89-3
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Related CAS # |
Fosnetupitant chloride monohydrochloride;1643757-72-5
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
CC1=CC=CC=C1C2=CC(N(CC3)CC[N+]3(C)COP([O-])(O)=O)=NC=C2N(C)C(C(C)(C4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4)C)=O
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Chemical Name |
(4-(5-(2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethylpropanamido)-4-(o-tolyl)pyridin-2-yl)-1-methylpiperazin-1-ium-1-yl)methyl hydrogen phosphate
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Synonyms |
07PNET; 07-PNET; Fosnetupitant chloride; Akynzeo; trade name: Akynzeo
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.4522 mL | 7.2610 mL | 14.5220 mL | |
5 mM | 0.2904 mL | 1.4522 mL | 2.9044 mL | |
10 mM | 0.1452 mL | 0.7261 mL | 1.4522 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.