Netupitant
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MedKoo CAT#: 205981

CAS#: 290297-26-6

Description: Netupitant is a selective neurokinin 1 (NK1) receptor antagonist with potential antiemetic activity. Netupitant competitively binds to and blocks the activity of the human substance P/NK1 receptors in the central nervous system (CNS), thereby inhibiting NK1-receptor binding of the endogenous tachykinin neuropeptide substance P (SP), which may result in the prevention of chemotherapy-induced nausea and vomiting (CINV).


Price and Availability

Size Price Shipping out time Quantity
25mg USD 150 Same Day
50mg USD 250 Same Day
100mg USD 450 Same Day
200mg USD 750 Same Day
500mg USD 1250 Same Day
1g USD 1950 Same Day
2g USD 2850 Same Day
5g USD 4650 Same Day
10g USD 7650 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-31. Prices are subject to change without notice.

Netupitant, purity > 98%, is in stock. The same day shipping out after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 205981
Name: Netupitant
CAS#: 290297-26-6
Chemical Formula: C30H32F6N4O
Exact Mass: 578.24803
Molecular Weight: 578.59
Elemental Analysis: C, 62.28; H, 5.57; F, 19.70; N, 9.68; O, 2.77


Synonym: AGE94200; AGE-94200; AGE 94200;Ro 67-3189; Ro-67-3189; Ro67-3189; Ro 67-3189/000; Netupitant.

IUPAC/Chemical Name: 2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethyl-N-(6-(4-methylpiperazin-1-yl)-4-(o-tolyl)pyridin-3-yl)propanamide

InChi Key: WAXQNWCZJDTGBU-UHFFFAOYSA-N

InChi Code: InChI=1S/C30H32F6N4O/c1-19-8-6-7-9-23(19)24-17-26(40-12-10-38(4)11-13-40)37-18-25(24)39(5)27(41)28(2,3)20-14-21(29(31,32)33)16-22(15-20)30(34,35)36/h6-9,14-18H,10-13H2,1-5H3

SMILES Code: CC(C)(C1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)C(N(C)C2=C(C3=CC=CC=C3C)C=C(N4CCN(C)CC4)N=C2)=O


Technical Data

Appearance:
White solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (SDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001


Additional Information

  The NK-receptor is a G-protein receptor coupled to the inositol phosphate signal-transduction pathway and is found in both the nucleus tractus solitarii and the area postrema.
 
 
 


References

1: Lorusso V, Karthaus M, Aapro M. Review of oral fixed-dose combination netupitant and palonosetron (NEPA) for the treatment of chemotherapy-induced nausea and vomiting. Future Oncol. 2014 Oct 31:1-13. [Epub ahead of print] PubMed PMID: 25360998.

2: Spinelli T, Moresino C, Baumann S, Timmer W, Schultz A. Effects of combined netupitant and palonosetron (NEPA), a cancer supportive care antiemetic, on the ECG of healthy subjects: an ICH E14 thorough QT trial. Springerplus. 2014 Jul 29;3:389. doi: 10.1186/2193-1801-3-389. eCollection 2014. PubMed PMID: 25105088; PubMed Central PMCID: PMC4124105.

3: Thomas AG, Stathis M, Rojas C, Slusher BS. Netupitant and palonosetron trigger NK1 receptor internalization in NG108-15 cells. Exp Brain Res. 2014 Aug;232(8):2637-44. doi: 10.1007/s00221-014-4017-7. Epub 2014 Jun 27. PubMed PMID: 24969614; PubMed Central PMCID: PMC4112047.

4: Andrews PL. Netupitant and palonosetron (NEPA): a winning team in the race for the optimal treatment of chemotherapy-induced nausea and vomiting? Ann Oncol. 2014 Jul;25(7):1258-9. doi: 10.1093/annonc/mdu190. Epub 2014 Jun 18. PubMed PMID: 24942276.

5: Gralla RJ, Bosnjak SM, Hontsa A, Balser C, Rizzi G, Rossi G, Borroni ME, Jordan K. A phase III study evaluating the safety and efficacy of NEPA, a fixed-dose combination of netupitant and palonosetron, for prevention of chemotherapy-induced nausea and vomiting over repeated cycles of chemotherapy. Ann Oncol. 2014 Jul;25(7):1333-9. doi: 10.1093/annonc/mdu096. Epub 2014 Mar 14. PubMed PMID: 24631949; PubMed Central PMCID: PMC4071753.

6: Hesketh PJ, Rossi G, Rizzi G, Palmas M, Alyasova A, Bondarenko I, Lisyanskaya A, Gralla RJ. Efficacy and safety of NEPA, an oral combination of netupitant and palonosetron, for prevention of chemotherapy-induced nausea and vomiting following highly emetogenic chemotherapy: a randomized dose-ranging pivotal study. Ann Oncol. 2014 Jul;25(7):1340-6. doi: 10.1093/annonc/mdu110. Epub 2014 Mar 7. PubMed PMID: 24608196; PubMed Central PMCID: PMC4071755.

7: Aapro M, Rugo H, Rossi G, Rizzi G, Borroni ME, Bondarenko I, Sarosiek T, Oprean C, Cardona-Huerta S, Lorusso V, Karthaus M, Schwartzberg L, Grunberg S. A randomized phase III study evaluating the efficacy and safety of NEPA, a fixed-dose combination of netupitant and palonosetron, for prevention of chemotherapy-induced nausea and vomiting following moderately emetogenic chemotherapy. Ann Oncol. 2014 Jul;25(7):1328-33. doi: 10.1093/annonc/mdu101. Epub 2014 Mar 5. PubMed PMID: 24603643; PubMed Central PMCID: PMC4071754.

8: Szitter I, Pintér E, Perkecz A, Kemény A, Kun J, Kereskai L, Pietra C, Quinn JP, Zimmer A, Berger A, Paige CJ, Helyes Z. Role of neurokinin 1 receptors in dextran sulfate-induced colitis: studies with gene-deleted mice and the selective receptor antagonist netupitant. Inflamm Res. 2014 May;63(5):399-409. doi: 10.1007/s00011-014-0712-x. Epub 2014 Jan 28. PubMed PMID: 24468892.

9: Spinelli T, Calcagnile S, Giuliano C, Rossi G, Lanzarotti C, Mair S, Stevens L, Nisbet I. Netupitant PET imaging and ADME studies in humans. J Clin Pharmacol. 2014 Jan;54(1):97-108. doi: 10.1002/jcph.198. Epub 2013 Nov 8. PubMed PMID: 24122871.

10: Haab F, Braticevici B, Krivoborodov G, Palmas M, Zufferli Russo M, Pietra C. Efficacy and safety of repeated dosing of netupitant, a neurokinin-1 receptor antagonist, in treating overactive bladder. Neurourol Urodyn. 2014 Mar;33(3):335-40. doi: 10.1002/nau.22406. Epub 2013 Jun 14. PubMed PMID: 23765630.