Galanin Receptor Ligand M35 TFA

Galanin Receptor Ligand M35 TFA is a high-affinity ligand and antagonist of galanin receptor (Kd=0.1 nM). Galanin Receptor Ligand M35 TFA exerts a Ki values of 0.11 and 2.0 nM for human galanin receptor type 1 and 2, respectively.

Product information

Molecular Weight: 2347.55

Formula: C109H154F3N27O28

Chemical Name: (S)-N1-((5S, 8S, 11S, 17S, 20S)-1-((S)-2-((S)-2-((S)-2-(2-((S)-1-((S)-1-((S)-2-((S)-1-((S)-1-amino-5-guanidino-1-oxopentan-2-ylamino)-1-oxo-3-phenylpropan-2-ylcarbamoyl)pyrrolidin-1-yl)-3-hydroxy-1-oxopropan-2-ylamino)-1-oxo-3-phenylpropan-2-ylamino)-2-oxoethylcarbamoyl)pyrrolidine-1-carbonyl)pyrrolidine-1-carbonyl)pyrrolidin-1-yl)-21-hydroxy-11-(4-hydroxybenzyl)-5, 8-diisobutyl-17-methyl-1, 4, 7, 10, 13, 16, 19-heptaoxo-3, 6, 9, 12, 15, 18-hexaazahenicosan-20-yl)-2-((S)-2-((2S, 3R)-2-((S)-2-(2-aminoacetamido)-3-(1H-indol-3-yl)propanamido)-3-hydroxybutanamido)-4-methylpentanamido)succinamide 2, 2, 2-trifluoroacetate

Smiles: C[C@@H](O)[C@H](NC(=O)[C@H](CC1=CNC2=CC=CC=C12)NC(=O)CN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](CC1C=CC(O)=CC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CC1C=CC=CC=1)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(N)=O.OC(=O)C(F)(F)F

InChiKey: AUGHCBHCBNYFSH-ZRGIVSPOSA-N

InChi: InChI=1S/C107H153N27O26.C2HF3O2/c1-57(2)42-70(123-93(147)71(43-58(3)4)124-95(149)74(47-64-33-35-66(138)36-34-64)121-86(141)52-115-91(145)60(7)118-100(154)78(55-135)128-98(152)77(49-84(109)139)125-94(148)72(44-59(5)6)127-103(157)89(61(8)137)130-99(153)76(119-85(140)50-108)48-65-51-114-68-27-16-15-26-67(65)68)92(146)117-54-88(143)131-38-20-31-82(131)105(159)134-41-21-32-83(134)106(160)133-40-18-29-80(133)101(155)116-53-87(142)120-73(45-62-22-11-9-12-23-62)96(150)129-79(56-136)104(158)132-39-19-30-81(132)102(156)126-75(46-63-24-13-10-14-25-63)97(151)122-69(90(110)144)28-17-37-113-107(111)112;3-2(4,5)1(6)7/h9-16,22-27,33-36,51,57-61,69-83,89,114,135-138H,17-21,28-32,37-50,52-56,108H2,1-8H3,(H2,109,139)(H2,110,144)(H,115,145)(H,116,155)(H,117,146)(H,118,154)(H,119,140)(H,120,142)(H,121,141)(H,122,151)(H,123,147)(H,124,149)(H,125,148)(H,126,156)(H,127,157)(H,128,152)(H,129,150)(H,130,153)(H4,111,112,113);(H,6,7)/t60-,61+,69-,70-,71-,72-,73-,74-,75-,76-,77-,78-,79-,80-,81-,82-,83-,89-;/m0./s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: To be determined

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Galanin Receptor Ligand M35 TFA has a dual effect on the galanin mediated inhibition of Forskolin stimulated cyclic AMP production in Rin m 5F cells. Co-applied with galanin (10 nM), Galanin Receptor Ligand M35 TFA at low concentrations (1 nM) is able to reverse the inhibitory effect of galanin. But when present at higher concentrations (15 and 30 nM), Galanin Receptor Ligand M35 TFA acts as a galanin receptor agonist, inhibiting the forskolin stimulated production of cAMP.

In Vivo:

Galanin Receptor Ligand M35 TFA (6 nM/10 μL; i.c.v.) improves the ability of the male Sprague-Dnwley rats to acquire the swim maze task.

References:

1. Kask K, et al. Binding and agonist/antagonist actions of M35, galanin(1-13)-bradykinin(2-9)amide chimeric peptide, in Rin m 5F insulinoma cells. Regul Pept. 1995 Nov 10;59(3):341-8.
2. Ogren SO, et al. Evidence for a role of the neuropeptide galanin in spatial learning. Neuroscience. 1992 Nov;51(1):1-5.
3. Webling KE, et al. Galanin receptors and ligands. Front Endocrinol (Lausanne). 2012 Dec 7;3:146.

Products are for research use only. Not for human use.