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Merck

SML2755

Sigma-Aldrich

Netupitant

≥98% (HPLC)

別名:

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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About This Item

実験式(ヒル表記法):
C30H32F6N4O
CAS番号:
分子量:
578.59
MDL番号:
UNSPSCコード:
12352200
NACRES:
NA.77

品質水準

アッセイ

≥98% (HPLC)

フォーム

powder

white to beige

溶解性

DMSO: 2 mg/mL, clear

保管温度

2-8°C

SMILES記法

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

生物化学的/生理学的作用

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.).

ピクトグラム

Exclamation mark

シグナルワード

Warning

危険有害性情報

危険有害性の分類

Eye Irrit. 2 - Skin Irrit. 2

保管分類コード

11 - Combustible Solids

WGK

WGK 3

引火点(°F)

Not applicable

引火点(℃)

Not applicable


適用法令

試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。

Jan Code

SML2755-VAR:
SML2755-50MG:
SML2755-BULK:
SML2755-10MG:


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試験成績書(COA)

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Anna Rizzi et al.
Peptides, 37(1), 86-97 (2012-06-27)
The novel NK(1) receptor ligand Netupitant has been characterized in vitro and in vivo. In calcium mobilization studies CHO cells expressing the human NK receptors responded to a panel of agonists with the expected order of potency. In CHO NK(1)
Weixia Zhong et al.
Neuropharmacology, 103, 195-210 (2015-12-04)
Cytoplasmic calcium (Ca(2+)) mobilization has been proposed to be an important factor in the induction of emesis. The selective sarcoplasmic/endoplasmic reticulum Ca(2+)-ATPase (SERCA) inhibitor thapsigargin, is known to deplete intracellular Ca(2+) stores, which consequently evokes extracellular Ca(2+) entry through cell
John A Rudd et al.
Frontiers in pharmacology, 9, 869-869 (2018-08-22)
Ghrelin has well-known activity to stimulate appetite and weight gain. Evidence suggests that ghrelin may also have effects in reducing chemotherapy-induced emesis via growth hormone secretagogue receptors (GHS-R1A) in the brain. However, it is not known whether the stimulation of
Beatrice Girard et al.
Experimental neurology, 285(Pt B), 110-125 (2016-10-25)
The mechanisms underlying the postnatal maturation of micturition from a somatovesical to a vesicovesical reflex are not known but may involve neuropeptides in the lower urinary tract. A transgenic mouse model with chronic urothelial overexpression (OE) of NGF exhibited increased
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

ライフサイエンス、有機合成、材料科学、クロマトグラフィー、分析など、あらゆる分野の研究に経験のあるメンバーがおります。.

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