企业QQ
官方微信
| BWX 46NPY Y5 receptor agonist,potent and highly selective |
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.
calculate
calculate
| Cas No. | 172997-92-1 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | (2S,5S,8S,11S,14R,17S,20S,Z)-N"1-((S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl)-20-((2S,3S)-2-((S)-2-amino-3-(4-hydroxyphenyl)propanamido)-3-methylpentanamido)-14-((5R,8S,11S,14S,17S)-22-amino-5-((S)-2-((S)-4-amino-2-((2S,3S)-2-((S)-2-amino-3-(4-hydro | ||
| Canonical SMILES | CCC[C@@](NC([C@](NC([C@](NC([C@](NC([C@](NC([C@](NC([C@](NC([C@](N)([H])CC1=CC=C(O)C=C1)=O)([H])[C@@](CC)([H])C)=O)([H])CC(O)=N)=O)([H])CC(C)C)=O)([H])CSSC[C@@](NC([C@](NC([C@](NC([C@](NC([C@](N)([H])CC2=CC=C(O)C=C2)=O)([H])[C@@](CC)([H])C)=O)([H])CC(N)=O | ||
| Formula | C116H186N36O28S2 | M.Wt | 2597.07 |
| Solubility | ≥260.4 mg/mL in DMSO with ultrasonic, <12.99 mg/ml="" in="" h2o,=""><12.99 mg/ml="" in="" etoh=""> | Storage | Desiccate 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. | ||
IC50: 0.5 nM for Y5
The actions of neuropeptide Y (NPY) are mediated by at least six G-protein coupled receptors denoted as Y1, Y2, Y3, Y4, Y5, and y6. Investigations using receptor selective ligands and receptor knock-out mice show that NPY effects on feeding are mediated by both Y1 and Y5 receptors. BWX 46 is a Y5 receptor selective agonist.
In vitro: BWX 46 selectively bound Y5 receptors, and inhibited cAMP synthesis by Y5 cells with potencies comparable to that of NPY. In addition, BWX 46 (10 μM) exhibited no significant effect on the cAMP synthesis by Y1, Y2, and Y4 cells. Thus, BWX 46 constitutes the lowest molecular weight Y5 selective agonist reported to date [1].
In vivo: Intrahypothalamic-injection of 30 and 40 μg of BWX 46 stimulated the food intake by rats in a gradual manner, reaching maximal level 8 h after injection. This response was similar to that exhibited by other Y5 selective agonists, but differed from that of NPY, which exhibited a rapider orexigenic stimulus within 1 h [1].
Clinical trial: Up to now, BWX 46 is still in the preclinical development stage.
Reference:[1] Ambikaipakan Balasubramaniam, Sulaiman Sheriff, Weixu Zhai, William T. Chance. Bis(31/31’){[Cys31, Nva34]NPY(27–36)-NH2}: a neuropeptide Y (NPY) Y5 receptor selective agonist with a latent stimulatory effect on food intake in rats. Peptides 23 (2002) 1485–1490
matriks/Shikari® (S-ATP) Anti-Pembrolizumab ELISA w/confirmation/PEM-QNS-KEY
intactgenomics/Methionine Auxotrophic LBA4404 | ig® | Intact Genomics/15x50μl/1076-15
goprolytix/Proteolytic Activation of Prothrombin/1 mg, 200 µg/BCT-DFP
novateinbio/Dynorphin A ( 13-17 ) Porcine Peptide/5mg/PE-54024_5mg
matriks/Shikari® (Q-ETA) Etanercept ELISA/ETA-FD-ENB
intactgenomics/Agrobacterium ElectroComponent Combo Pack | Intact Genomics/12x50µl/1290-24
Jackson/Peroxidase AffiniPure Goat Anti-Mouse IgG (H+L)/2.0 ml/115-035-003
Jackson/Peroxidase AffiniPure Goat Anti-Rabbit IgG (H+L)/2.0 ml/111-035-003
Qubit™ dsDNA BR Assay Kit Q32853现货
Invitrogen Q32855 Qubit™ RNA HS Assay Kit现货促销
LUCK-1G,D-Luciferin, Potassium Salt 钾盐现货
GoldBio/D-Luciferin, Sodium Salt (Proven and Published™)/LUCNA-1G/1 g