- Biapenem
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| AprepitantSubstance P (SP) inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.62%
- COA (Certificate Of Analysis)
- HPLC(Retest)
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Cell experiment [1]: | |
Cell lines | Nalm-6 cells |
Preparation method | The solubility of this compound in DMSO is >26.7mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | 20 μM |
Applications | Aprepitant decreased the metabolic activity with an estimated IC50 value of 20 μM. Aprepitant induced cell-growth inhibition and G1 cell-cycle arrest. Aprepitant significantly induced apoptosis in Nalm-6 cells. Aprepitant (20 μM) induced p53 accumulation and expression of pro-apoptotic p53 target genes. |
| Animal experiment [2]: | |
Animal models | Male C57BL/6J mice |
Dosage form | Intraperitoneal injection, 10 mg/kg |
Application | Aprepitant (10 mg/kg, i.p.) significantly attenuated AMPH-induced CPP expression and locomotor activation produced by AMPH and cocaine in mice. Aprepitant significantly enhanced the expression of CPP produced by morphine while significantly suppressing the locomotor activity of the mice conditioned with morphine. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Bayati S, Bashash D, Ahmadian S, et al. Inhibition of tachykinin NK 1 receptor using aprepitant induces apoptotic cell death and G1 arrest through Akt/p53 axis in pre-B acute lymphoblastic leukemia cells[J]. European journal of pharmacology, 2016, 791: 274-283. [2]. Mannangatti P, Sundaramurthy S, Ramamoorthy S, et al. Differential effects of aprepitant, a clinically used neurokinin-1 receptor antagonist on the expression of conditioned psychostimulant versus opioid reward[J]. Psychopharmacology, 2017, 234(4): 695-705. | |
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| Cas No. | 170729-80-3 | SDF | Download SDF |
| Synonyms | N/A | ||
| 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 | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Aprepitant (also known as MK-0869) is a novel and highly selective Neurokinin-1 (NK-1) receptor antagonist that inhibits the activity of substance P (SP), an undecapeptide belonging to the tachykinin family of peptides, on the NK-1 receptor with the dissociation constant Kd of 86 pM for human NK-1 receptor and the half maximal inhibition concentration IC50 of 0.1 nM, 4 nM and 0.7 nM for human, rat and ferret NK-1 receptors respectively [1,2].
Since SP has been demonstrated to induce cell proliferation in several human cancer cell lines with overexpressed NK-1 receptors, aprepitant has also been found to concentration-dependently induce growth inhibition in a variety of tumor cell lines, including glioma (GAMG), neuroblastoma (SKN-BE2, IMR-32 and KELLY), retinoblastoma (Y-79 and WERI-Rb-1), pancreas carcinoma (PA-TU-8902 and CAPAN-1), larynx carcinoma (HEp-2), gastric carcinoma (23132-87) and colon carcinoma (SW-403), with IC50 of 33.1 μΜ, 24.6 μΜ, 19.6 μΜ, 27.7 μΜ, 30.4 μΜ, 23 μΜ, 31.2 μΜ, 27.4 μΜ, 22.7 μΜ, 24.2 μΜ and 30.5 μΜ respectively [2].
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 M1, Rosso M. The NK-1 receptor antagonist aprepitant as a broad spectrum antitumor drug. Invest New Drugs. 2010 Apr;28(2):187-93. doi: 10.1007/s10637-009-9218-8. Epub 2009 Jan 17.
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