- Talnetant
| SB-222200Human NK-3 receptor antagonist |
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
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- Purity = 98.86%
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| Cas No. | 174635-69-9 | SDF | Download SDF |
| Synonyms | SB 222200;SB222200 | ||
| Chemical Name | 3-methyl-2-phenyl-N-[(1S)-1-phenylpropyl]quinoline-4-carboxamide | ||
| Canonical SMILES | CCC(C1=CC=CC=C1)NC(=O)C2=C(C(=NC3=CC=CC=C32)C4=CC=CC=C4)C | ||
| Formula | C26H24N2O | M.Wt | 380.48 |
| Solubility | ≥19.024 mg/mL in DMSO, ≥43.6 mg/mL in EtOH, <2.47 mg/ml="" in="" h2o=""> | 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. | ||
SB 222200 is a selective and potent antagonist of NK-3 receptor [1].Neurokinin-3 (NK-3) receptor is a member of the G-protein-coupled superfamily and functions as a receptor for tachykinin. Activation of NK-3 receptors causes phosphoinositol 4, 5 biphosphate(PIP2) breakdown into 1,4,5 inositol triphosphate (IP3) and diacylglycerol through phospholipase C activation [1].In Chinese hamster ovary (CHO) cell expressing the hNK-3 receptor, SB 222200 inhibited neurokinin B (NKB) binding to the cell membranes with a Ki value of 4.4 nM. In HEK 293 cells expressing the hNK-3 receptor, SB 222200 antagonized NKB-induced Ca2+ mobilization with an IC50 value of 18.4 nM [1]. In mice model, SB-222200 inhibited behavioral responses (rapid head shakes and tail whips) induced by senktide (the NK-3 receptor-selective agonist) with an ED50 value of 5 mg/kg in a dose-dependent way and the inhibitory effect correlated significantly with brain concentrations of SB-222200 [1]. Treatment adult male CD-1 mice with SB 222200, mice had significantly enhanced hyperactivity when challenged with cocaine, which suggested that blockade of NK-3 receptors enhanced dopamine-mediated behavioral hyperactivity.References:[1]. Sarau HM, Griswold DE, Bush B, et al. Nonpeptide tachykinin receptor antagonists. II. Pharmacological and pharmacokinetic profile of SB-222200, a central nervous system penetrant, potent and selective NK-3 receptor antagonist. J Pharmacol Exp Ther, 2000, 295(1): 373-381.[2]. Nwaneshiudu CA, Unterwald EM. Blockade of neurokinin-3 receptors modulates dopamine-mediated behavioral hyperactivity. Neuropharmacology, 2009, 57(3): 295-301.
