BWX 46NPY Y5 receptor agonist,potent and highly selective CAS# 172997-92-1 |
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Quality Control & MSDS
3D structure
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| Cas No. | 172997-92-1 | SDF | Download SDF |
| PubChem ID | 16142371 | Appearance | Powder |
| Formula | C116H186N36O28S2 | M.Wt | 2597.09 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | Bis(31/31'){Cys<sup>31</sup>, Nva<sup>34</sup>]NPY(27-36)-NH2} | ||
| Solubility | Soluble to 10 mg/ml in water | ||
| Sequence | YINLCTRXRY YINLCTRXRY* (Modifications: X = Nva, Tyr-10 = C-terminal amide, X* = Nva, Tyr-10* = C-terminal amide, Disulfide bridge between 5 - 5*) | ||
| SMILES | CCCC(C(=O)NC(CCCNC(=N)N)C(=O)NC(CC1=CC=C(C=C1)O)C(=O)N)NC(=O)C(CCCNC(=N)N)NC(=O)C(C(C)O)NC(=O)C(CSSCC(C(=O)NC(C(C)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCC)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC2=CC=C(C=C2)O)C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CC(=O)N)NC(=O)C(C(C)CC)NC(=O)C(CC3=CC=C(C=C3)O)N)NC(=O)C(CC(C)C)NC(=O)C(CC(=O)N)NC(=O)C(C(C)CC)NC(=O)C(CC4=CC=C(C=C4)O)N | ||
| Standard InChIKey | NCCWKDKNIQUYAI-JULUKTQUSA-N | ||
| Standard InChI | InChI=1S/C116H186N36O28S2/c1-13-21-73(97(165)137-75(23-17-43-131-113(123)124)101(169)141-79(93(121)161)51-65-31-39-69(157)40-32-65)135-99(167)77(25-19-45-133-115(127)128)139-111(179)91(61(11)153)151-107(175)85(147-103(171)81(47-57(5)6)143-105(173)83(53-87(119)159)145-109(177)89(59(9)15-3)149-95(163)71(117)49-63-27-35-67(155)36-28-63)55-181-182-56-86(148-104(172)82(48-58(7)8)144-106(174)84(54-88(120)160)146-110(178)90(60(10)16-4)150-96(164)72(118)50-64-29-37-68(156)38-30-64)108(176)152-92(62(12)154)112(180)140-78(26-20-46-134-116(129)130)100(168)136-74(22-14-2)98(166)138-76(24-18-44-132-114(125)126)102(170)142-80(94(122)162)52-66-33-41-70(158)42-34-66/h27-42,57-62,71-86,89-92,153-158H,13-26,43-56,117-118H2,1-12H3,(H2,119,159)(H2,120,160)(H2,121,161)(H2,122,162)(H,135,167)(H,136,168)(H,137,165)(H,138,166)(H,139,179)(H,140,180)(H,141,169)(H,142,170)(H,143,173)(H,144,174)(H,145,177)(H,146,178)(H,147,171)(H,148,172)(H,149,163)(H,150,164)(H,151,175)(H,152,176)(H4,123,124,131)(H4,125,126,132)(H4,127,128,133)(H4,129,130,134)/t59-,60-,61+,62+,71-,72-,73-,74-,75-,76-,77-,78-,79-,80-,81-,82-,83-,84-,85-,86-,89-,90-,91-,92-/m0/s1 | ||
| 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. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
BWX 46 Dilution Calculator
BWX 46 Molarity Calculator
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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
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Bis(31/31')[[Cys(31), Nva(34)]NPY(27-36)-NH(2)]: a neuropeptide Y (NPY) Y(5) receptor selective agonist with a latent stimulatory effect on food intake in rats.[Pubmed:12182951]
Peptides. 2002 Aug;23(8):1485-90.
The actions of neuropeptide Y (NPY) are mediated by at least six G-protein coupled receptors denoted as Y(1), Y(2), Y(3), Y(4), Y(5), and y(6). Investigations using receptor selective ligands and receptor knock-out mice suggest that NPY effects on feeding are mediated by both Y(1) and Y(5) receptors. We have previously shown that Cys-dimers of NPY C-terminal peptides exhibit Y(1) selectivity relative to Y(2) receptors. Re-investigation of their selectivity with respect to the newly cloned receptors, has identified bis(31/31') [[Cys(31), Nva(34)]NPY(27-36)-NH(2)] (BWX-46) as a Y(5) receptor selective agonist. BWX-46 selectively bound Y(5) receptors, and inhibited cAMP synthesis by Y(5) cells with potencies comparable to that of NPY. Moreover, BWX-46 (10 microM) exhibited no significant effect on the cAMP synthesis by Y(1), Y(2), and Y(4) cells. Thus, BWX-46 constitutes the lowest molecular weight Y(5) selective agonist reported to date. Intrahypothalamic (i.h.t)-injection of 30 and 40 microg 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 Y(5) selective agonists, but differed from that of NPY, which exhibited a rapid orexigenic stimulus within 1 h. It is suggested that the differences in the orexigenic stimuli of NPY and Y(5) agonists may be due to their differences in the signal transduction mechanisms.
