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Merck
CN

SML2755

Netupitant

≥98% (HPLC)

别名:

2-(3,5-bis(Trifluoromethyl)phenyl)-N,2-dimethyl-N-(6-(4-methylpiperazin-1-yl)-4-o-tolylpyridin-3-yl)propanamide, 2-[3,5-bis(Trifluoromethyl)phenyl]-N-[6-(4-methylpiperazin-1-yl)-4-o-tolylpyridin-3-yl]-N-methylisobutyramide, AGE 94200, AGE-94200, AGE94200, CID 6451149, CID-6451149, CID6451149, N,a,a-Trimethyl-N-[4-(2-methylphenyl)-6-(4-methyl-1-piperazinyl)-3-pyridinyl]-3,5-bis(trifluoromethyl)benzeneacetamide, Ro 67-31898, Ro 67-31898/000

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关于此项目

经验公式（希尔记法）:
C30H32F6N4O
化学文摘社编号:
290297-26-6
分子量:
578.59
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD25976831

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SMILES string

FC(F)(F)c1cc(cc(c1)C(C)(C)C(=O)N(C)c2cnc(cc2c4c(cccc4)C)N3CCN(CC3)C)C(F)(F)F

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

InChI key

WAXQNWCZJDTGBU-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Quality Level

100

Biochem/physiol Actions

Brain-penetrant, orally active, potent and selective neurokinin-1 (NK1) receptor (NK1R; Tachykinin receptor 1) antagonist with antiemetic efficacy in vivo.
Netupitant is a brain-penetrant, orally active, potent and selective neurokinin-1 (NK1) receptor (NK1R; Tachykinin receptor 1) antagonist (Ca+2 mobilization IC50 = 11.2 nM/hNK1 vs. >1 μM/rNK1 & hNK2/3; hNK1/2/3 Ki = 0.95 nM/1.6 μM/1.6 μM) that effectively blocks agonist GR73632-induced foot tapping in gerbils (ID50 = 0.5 mg/kg po 2h prior to 3 pmol/5 μL GR73632/gerbil icv). In addition to antiemetic efficacy against substance P-associated vomiting reflexes, netupitant is also reported to enhance the analgesic effects of electroacupuncture (EA) among humanized mice with sickle cell disease in response to pain in vivo (10 mg/kg/day, i.p.).

pictograms

Exclamation mark
GHS07

signalword

Warning

hcodes

H315,H319

Hazard Classifications

Eye Irrit. 2 - Skin Irrit. 2

存储类别

11 - Combustible Solids

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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分析证书(COA)

Lot/Batch Number
0000391900
0000391899
0000391900
0000391899
0000253344

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Ajit G Thomas et al.
Experimental brain research, 232(8), 2637-2644 (2014-06-28)
Current therapy for chemotherapy-induced nausea and vomiting includes the use of both 5-HT3 and NK1 receptor antagonists. Acute emesis has largely been alleviated with the use of 5-HT3 receptor antagonists, while an improvement in preventing delayed emesis has been achieved
John A Rudd et al.
Frontiers in pharmacology, 7, 263-263 (2016-09-16)
Chemotherapy-induced acute and delayed emesis involves the activation of multiple pathways, with 5-hydroxytryptamine (5-HT; serotonin) playing a major role in the initial response. Substance P tachykinin NK1 receptor antagonists can reduce emesis induced by disparate emetic challenges and therefore have
Marigo Stathis et al.
European journal of pharmacology, 689(1-3), 25-30 (2012-06-12)
Netupitant is a potent and selective NK(1) receptor antagonist under development in combination with a fixed dose of palonosetron for the prevention of chemotherapy induced nausea and vomiting. Palonosetron is a 5-HT(3) receptor antagonist approved for both the prevention of
Torsten Hoffmann et al.
Bioorganic & medicinal chemistry letters, 16(5), 1362-1365 (2005-12-08)
The discovery of a novel, achiral pyridine class of potent and orally active neurokinin-1 (NK(1)) receptor antagonists is described. The evaluation of this class is briefly outlined, leading to the identification of netupitant 21 and befetupitant 29, two new proprietary
Ying Wang et al.
Journal of pain research, 12, 2419-2426 (2019-08-27)
Purpose: Chronic pain is a major comorbidity of sickle cell disease (SCD). Acupuncture, a non-opioid and non-addictive therapy to treat pain, was found to reduce pain in the majority (80%) of SCD patients in an earlier retrospective review. We observed
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