Aprepitant (Synonyms: Emend, L754,030, MK-869, ONO7436) |
Catalog No.GC15200
One-Click Copy Product Info
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Aprepitant은 새롭고 고선택적인 뉴로키닌-1(NK-1) 수용체 길항제이다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 170729-80-3
Sample solution is provided at 25 µL, 10mM.
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Aprepitant은 새롭고 고선택적인 뉴로키닌-1(NK-1) 수용체 길항제이다. Aprepitant은 인간 NK-1 수용체에 대한 Kd 값이 86pM이고 인간, 쥐 그리고 페럿 NK-1 수용체에 대한 IC50 값은 각각 0.1nM, 4nM, 0.7nM이다[2].
체외 실험에서 Aprepitant(5-30μM)으로 24-48시간 처리하면 Nalm-6 세포에 대해 농도 및 시간 의존적으로 세포독성과 항증식 효과를 나타냈다[3]. HEK 293 세포에 대한 Aprepitant의 IC50 값은 >90μM이었다[2]. Aprepitant은 10-60mM 농도에서 72시간 동안 모든 흑색종 세포 라인에서 농도 의존적으로 세포 성장 억제를 유발하였다[4].
체내 실험에서 3일간 Aprepitant(10mg/kg/d)을 복강 내 투여하면 정신흥분제인 암페타민(AMPH)과 코카인에 의해 유도된 조건적 장소 선호(CPP)의 발현을 약화시키면서 모르핀에 의해 유도된 CPP는 강화하였다[5].
References:
[1] Tattersall FD1, Rycroft W, Cumberbatch M, Mason G, Tye S, Williamson DJ, Hale JJ, Mills SG, Finke PE, MacCoss M, Sadowski S, Ber E, Cascieri M, Hill RG, MacIntyre DE, Hargreaves RJ. The novel NK1 receptor antagonist MK-0869 (L-754,030) and its water soluble phosphoryl prodrug, L-758,298, inhibit acute and delayed cisplatin-induced emesis in ferrets. Neuropharmacology. 2000 Feb 14;39(4):652-63.
[2] Muñoz M, Rosso M. The NK-1 receptor antagonist aprepitant as a broad spectrum antitumor drug. Invest New Drugs. 2010;28(2):187-193.
[3]Bayati S, Bashash D, Ahmadian S, et al. Inhibition of tachykinin NK1 receptor using aprepitant induces apoptotic cell death and G1 arrest through Akt/p53 axis in pre-B acute lymphoblastic leukemia cells. Eur J Pharmacol. 2016;791:274-283.
[4] Muñoz M, Rosso M, Robles-Frias MJ, et al. The NK-1 receptor is expressed in human melanoma and is involved in the antitumor action of the NK-1 receptor antagonist aprepitant on melanoma cell lines. Lab Invest. 2010;90(8):1259-1269.
[5] Mannangatti P, Sundaramurthy S, Ramamoorthy S, Jayanthi LD. Differential effects of aprepitant, a clinically used neurokinin-1 receptor antagonist on the expression of conditioned psychostimulant versus opioid reward. Psychopharmacology (Berl). 2017;234(4):695-705.
| 세포 실험 [1]: | |
세포 라인 | Nalm-6 |
제조 방법 | 10mM 농도의 Aprepitant 원액은 0.1% DMSO에 화합물을 용해해서 제조되었습니다. 세포는 5, 10, 15, 20 및 30µM의 농도에 도달하기 위해 적정량의 Aprepitant 원액으로 처리되었습니다. 4개의 음성 대조 그룹(억제제 없음) 외에 세포는 대체 음성 대조 그룹으로 해당 농도의 DMSO로 처리되었습니다. |
반응 조건 | 5, 10, 15, 20 and 30µM; 24-36 시간 동안 |
응용 분야 | Aprepitant은 농도 및 시간 의존적으로 세포 생존율과 세포 수를 감소시키고 DNA 합성 속도를 유도하고 G1기에 세포 축적을 유도하고 S기 세포 집단을 감소시켰습니다. |
| 동물 실험 [2]: | |
동물 모형 | 수컷 C57BL/6J 쥐 |
제조 방법 | Aprepitant은 DMSO에 용해하고 생리 식염수로 희석해서 최종 DMSO 농도가 0.002%가 되었습니다. |
제형 | 10mg/kg/일; 3 일 동안; i.p. |
응용 분야 | 대조 용매와 비교했을 때 Aprepitant은 CPP 발현과 운동 활성화를 현저하게 감소시켰습니다. |
References: | |
| Cas No. | 170729-80-3 | SDF | |
| Synonyms | Emend, L754,030, MK-869, ONO7436 | ||
| Chemical Name | 5-[[(2R,3S)-2-[1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl]-1,2-dihydro-1,2,4-triazol-3-one | ||
| Canonical SMILES | CC(C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)OC2C(N(CCO2)CC3=NC(=O)NN3)C4=CC=C(C=C4)F | ||
| Formula | C23H21F7N4O3 | M.Wt | 534.43 |
| Solubility | ≥ 26.7mg/mL in DMSO | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8712 mL | 9.3558 mL | 18.7115 mL |
| 5 mM | 374.2 μL | 1.8712 mL | 3.7423 mL |
| 10 mM | 187.1 μL | 935.6 μL | 1.8712 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)