| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Galanin Receptor Ligand M35 targets galanin receptors (GAL receptors), specifically human galanin receptor type 1 (GAL1) and type 2 (GAL2). It binds with high affinity (Kd = 0.1 nM) and exhibits Ki values of 0.11 nM for human galanin receptor type 1 and 2.0 nM for type 2. The peptide acts as a galanin receptor antagonist in various tissues including rat spinal cord and hippocampus.
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| 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].
In vitro, Galanin Receptor Ligand M35 binds to galanin receptors with high affinity (Kd = 0.1 nM). It has Ki values of 0.11 nM for human galanin receptor type 1 and 2.0 nM for type 2. The peptide acts as an antagonist of galanin-mediated inhibition of forskolin-stimulated cyclic AMP production in Rin m 5F cells. It has a dual effect on galanin-mediated signaling, acting as an antagonist in some contexts. |
| 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].
In vivo, Galanin Receptor Ligand M35 (6 nM/10 microL; i.c.v.) improves the ability of male Sprague-Dawley rats to acquire the swim maze task. This suggests cognitive-enhancing effects through galanin receptor modulation. The peptide acts as a galanin receptor antagonist in the rat spinal cord and hippocampus. Further in vivo studies would be needed to fully characterize its behavioral and physiological effects. |
| Enzyme Assay |
The in vitro receptor binding assay for galanin receptors uses radiolabeled M35 (typically [¹2⁵I]-M35) for equilibrium binding studies. Membrane preparations from cells or tissues expressing galanin receptors are incubated with [¹2⁵I]-M35 and varying concentrations of unlabeled M35. Bound radioactivity is measured by filtration and gamma counting. Kd and Ki values are calculated from saturation and competition binding curves. For functional assays, forskolin-stimulated cAMP production is measured in Rin m 5F cells.
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| Cell Assay |
For in vitro cell-based assays, Rin m 5F pancreatic beta-cells are cultured and treated with galanin (10 nM) and Galanin Receptor Ligand M35 at various concentrations. Forskolin-stimulated cAMP production is measured by ELISA or radioimmunoassay to assess the peptide's effect on galanin-mediated inhibition of cAMP accumulation. Cells are maintained under standard culture conditions and experiments are typically performed in triplicate. Receptor binding studies are also performed using cells expressing human galanin receptor types 1 and 2.
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| Animal Protocol |
In vivo animal studies for Galanin Receptor Ligand M35 typically involve male Sprague-Dawley rats. The peptide is administered intracerebroventricularly (i.c.v.) at doses such as 6 nM/10 microL. Behavioral testing, such as swim maze acquisition, is performed to assess cognitive effects. Brain tissue may be collected for receptor occupancy studies or neurochemical analysis. The peptide's effects on spinal cord and hippocampal galanin signaling are also studied.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Galanin Receptor Ligand M35 are not extensively documented. As a peptide with molecular weight 2233.58 and molecular formula C10₇H1₅3N2₇O2₆, it has limited oral bioavailability and is typically administered via injection (intracerebroventricular or intravenous). The peptide sequence is GWTLNSAGYLLGPPPGFSPFR-NH2. Storage: keep away from moisture; powder at -20degC for 3 years; in solvent at -80degC for 1 year.
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| Toxicity/Toxicokinetics |
Toxicological data for Galanin Receptor Ligand M35 are not well characterized. As a research peptide, standard safety precautions should be observed. The compound is for laboratory use only and not intended for human therapeutic applications. Peptide-based research compounds generally have favorable safety profiles but may have immunogenicity risks. Comprehensive toxicity profiling would be required for therapeutic development.
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| References | |
| Additional Infomation |
Galanin Receptor Ligand M35 (CAS# 142846-71-7) is a chimeric peptide [galanin (1-13)-bradykinin (2-9) amide] with sequence GWTLNSAGYLLGPPPGFSPFR-NH2. It is used as a high-affinity galanin receptor ligand for studying galanin-mediated signaling. The peptide is not approved for clinical use and is strictly for laboratory research purposes. Radiolabeled M35 is used in equilibrium binding studies.
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| Molecular Formula |
C107H153N27O26
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|---|---|
| Molecular Weight |
2233.52502
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| Exact Mass |
2232.15
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| CAS # |
142846-71-7
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| Related CAS # |
Galanin Receptor Ligand M35 TFA
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| PubChem CID |
16131186
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| Appearance |
White to off-white solid powder
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| LogP |
2.163
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| Hydrogen Bond Donor Count |
27
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| Hydrogen Bond Acceptor Count |
28
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| Rotatable Bond Count |
61
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| Heavy Atom Count |
160
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| Complexity |
5020
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| Defined Atom Stereocenter Count |
18
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| 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
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| InChi Key |
JWMXJVFGTXYBFM-AEXVMZOXSA-N
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| 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
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| 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
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~44.77 mM)
H2O : ~50 mg/mL (~22.39 mM) |
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| 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. View More
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. |
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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