Galanin Receptor Ligand M35 is a novel, potent and high-affinity galanin receptor ligand acting as a galanin receptor antagonist (Kd=0.1 nM in the rat spinal cord, rat hippocampus and isolated mouse pancreatic islets. Galanin Receptor Ligand M35 exerts a Kis of 0.11 and 2.0 nM for human GalR1 and GalR2, respectively.
Physicochemical Properties
| Molecular Formula | C107H153N27O26 |
| Molecular Weight | 2233.52502 |
| Exact Mass | 2232.15 |
| CAS # | 142846-71-7 |
| Related CAS # | Galanin Receptor Ligand M35 TFA |
| PubChem CID | 16131186 |
| Appearance | White to off-white solid powder |
| LogP | 2.163 |
| Hydrogen Bond Donor Count | 27 |
| Hydrogen Bond Acceptor Count | 28 |
| Rotatable Bond Count | 61 |
| Heavy Atom Count | 160 |
| Complexity | 5020 |
| Defined Atom Stereocenter Count | 18 |
| SMILES | C[C@H]([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](CC1=CC=C(C=C1)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N2CCC[C@H]2C(=O)N3CCC[C@H]3C(=O)N4CCC[C@H]4C(=O)NCC(=O)N[C@@H](CC5=CC=CC=C5)C(=O)N[C@@H](CO)C(=O)N6CCC[C@H]6C(=O)N[C@@H](CC7=CC=CC=C7)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N)NC(=O)[C@H](CC8=CNC9=CC=CC=C98)NC(=O)CN)O |
| InChi Key | JWMXJVFGTXYBFM-AEXVMZOXSA-N |
| InChi Code | InChI=1S/C107H153N27O26/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/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)/t60-,61+,69-,70-,71-,72-,73-,74-,75-,76-,77-,78-,79-,80-,81-,82-,83-,89-/m0/s1 |
| Chemical Name | (2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]-N-[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2S)-2-[(2S)-2-[(2S)-2-[[2-[[(2S)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-amino-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamoyl]pyrrolidin-1-yl]-3-hydroxy-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]butanediamide |
| HS Tariff Code | 2934.99.9001 |
| Storage |
Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| ln Vitro | In Rin m 5F cells, galanin inhibits the production of c-AMP stimulated by forskolin in two different ways. This is the result of galanin receptor ligand M35. Galanin Receptor Ligand M35 functions as a galanin receptor at higher concentrations (15 and 30 nM) but can be used in conjunction with galanin (10 nM) at low concentrations (1 nM) to restore galanin. a physical agonist that prevents the synthesis of cAMP stimulated by forskolin [1]. |
| ln Vivo | The shelf Sprague-Dnwley stent performs better on the swimming maze challenge when galanin Receptor Ligand M35 (6 nM/10 μL; icv) is used [1]. |
| References |
[1]. 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]. Galanin receptors and ligands. Front Endocrinol (Lausanne). 2012 Dec 7;3:146. [3]. Evidence for a role of the neuropeptide galanin in spatial learning. Neuroscience. 1992 Nov;51(1):1-5. |
Solubility Data
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~44.77 mM) H2O : ~50 mg/mL (~22.39 mM) |
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (1.12 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (1.12 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (1.12 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.4477 mL | 2.2386 mL | 4.4772 mL | |
| 5 mM | 0.0895 mL | 0.4477 mL | 0.8954 mL | |
| 10 mM | 0.0448 mL | 0.2239 mL | 0.4477 mL |