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Aprepitant (MK-0869)

促销

neurokinin-1 receptor 拮抗剂

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产品目录号: A10083

库存状态:中国现货中国现货

产品名 目录号 价格 数量
Aprepitant 2mg A10083-2
¥ 300.00
Aprepitant 5mg A10083-5
¥ 500.00
Aprepitant 10mg A10083-10
¥ 600.00
Aprepitant 25mg A10083-25
¥ 700.00
Aprepitant (MK-0869) 10mM * 1mL in DMSO A10083-10mM-D
¥ 1,390.00

产品仅用于研究,不针对患者销售,望谅解.

产品简介

Aprepitant is classified as an NK1 antagonist. 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. It has also been shown to increase the activity of the 5-HT3 receptor antagonists ondansetron and the corticosteroid dexamethasone, which are also used to prevent nausea and vomiting caused by chemotherapy.

Aprepitant (MK-0869)

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顾客使用 Adooq 产品发表的高质量科研文献
Adooq 顾客使用 Aprepitant (MK-0869) 发表的文献 (1)
  • Kodji X, .et al. Sensory nerves mediate spontaneous behaviors in addition to inflammation in a murine model of psoriasis, FASEB J, 2018, Sep 11:fj201800395RR PMID: 30204499

Chemical Information

目录号 A10083
Mechanism of action Antagonist
分子量 534.4
化学分子式 C23H21F7N4O3
Solubility DMSO
纯度 >98%
储存方式 at -20°C 2 years
CAS No. 170729-80-3
Synonyms MK0869, MK-869, L-754030, Emend
SMILES code C[C@H](C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)O[C@@H]2[C@@H](N(CCO2)CC3=NC(=O)NN3)C4=CC=C(C=C4)F
化学名称 5-([(2R,3S)-2-((R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy)-3-(4-fluorophenyl) morpholino]methyl)-1H-1,2,4-triazol-3(2H)-one

生物活性

Description

Aprepitant is classified as an NK1 antagonist. 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. It has also been shown to increase the activity of the 5-HT3 receptor antagonists ondansetron and the corticosteroid dexamethasone, which are also used to prevent nausea and vomiting caused by chemotherapy.

Targets
Neurokinin-1 receptor (Cell-free assay)
0.1 nM

溶解性

Solubility (25°C) * In vitro DMSO 107 mg/mL (200.21 mM)
Water <1 mg/mL (<1 mM)
Ethanol 15 mg/mL (28.06 mM)
In vivo 30% PEG400/0.5% Tween80/5% propylene glycol 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

制备储备液

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 18.71 mL 93.56 mL 187.13mL
0.5 mM 3.74 mL 18.71 mL 37.43 mL
1 mM 1.87 mL 9.36 mL 18.71 mL
5 mM 0.37 mL 1.87 mL 3.74 mL

*The above data is based on the productmolecular weight 534.4 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

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