| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
M40 targets galanin receptor type 1 (GAL1-R) and galanin receptor type 2 (GAL2-R). It acts as a potent, non-selective antagonist at these receptors. Ki values are 1.82 nM at GAL1 and 5.1 nM at GAL2. The peptide has no effect on chow or fat intake.
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|---|---|
| ln Vitro |
Mono[125IJodo-Tyr26]galanin is displaced from binding sites in the hippocampus, hypothalamus, and spinal cord by M40 (1 μM). For all membranes, M40 has a lower affinity than galanin. In the hippocampus, 15 nM in the hypothalamus, 12 nM in the spinal cord, and 3 nM in the insulinoma cells were the IC50 values. M40 (1 μM) totally inhibits the binding site of galanin tagged with 125I [1].
In vitro, M40 (1 microM) displaces [mono[¹2⁵I]Iodo-Tyr2⁶]galanin from binding sites in the hippocampus, hypothalamus, and spinal cord. It has a lower affinity than galanin for all membranes. M40 inhibits galanin (1-29) binding in rat brain with an IC₅0 of 3-15 nM. Ki values are 1.82 nM at GAL1 and 5.1 nM at GAL2. |
| ln Vivo |
In vivo, M40 decreases food intake, ethanol consumption, and reproductive behavior. The peptide exhibits anxiolytic activity in elevated plus maze and social interaction tasks and suppresses defensive burying behavior in animal models of anxiety. It is a potent galanin receptor antagonist with anorexigenic and anxiolytic activities.
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| Enzyme Assay |
The in vitro receptor binding assay for galanin receptors uses membrane preparations from rat brain (hippocampus, hypothalamus, spinal cord) or cells expressing GAL1 and GAL2 receptors. Competitive binding is performed using [mono[¹2⁵I]Iodo-Tyr2⁶]galanin as the radioligand in the presence of varying concentrations of M40. Bound radioactivity is measured by filtration and gamma counting. Ki and IC₅0 values are calculated from competition curves.
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| Cell Assay |
For in vitro cell-based assays, cells expressing galanin receptor subtypes (GAL1 or GAL2) are cultured and treated with M40 at various concentrations. Receptor antagonism is assessed by measuring inhibition of galanin-mediated signaling (such as cAMP modulation or calcium mobilization). Experiments are typically performed in triplicate under standard culture conditions.
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| Animal Protocol |
In vivo animal studies for M40 typically involve rodent models to assess food intake, anxiety, and reproductive behavior. The peptide is administered via intracerebroventricular (ICV) or intraperitoneal injection at various doses. Food intake and ethanol consumption are measured. Anxiety-like behavior is assessed using elevated plus maze, social interaction, and defensive burying tests. Reproductive behavior may also be monitored.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of M40 are not extensively documented. As a peptide with sequence Gwtlnsagyllgpppalala-conh2, it has limited oral bioavailability and is typically administered via injection. The peptide is soluble in aqueous buffers and DMSO. Storage at -20degC is recommended. Further detailed PK parameters would require dedicated studies.
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| Toxicity/Toxicokinetics |
Toxicological data for M40 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 |
[1]. Bartfai T, et al. Galanin-receptor ligand M40 peptide distinguishes between putative galanin-receptor subtypes. Proc Natl Acad Sci U S A. 1993 Dec 1;90(23):11287-91.
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| Additional Infomation |
ST-003 is a novel galangin receptor inhibitor, and its efficacy in treating primary sclerosing cholangitis is currently being investigated.
M40 (CAS# 143896-17-7) is a potent, non-selective galanin receptor antagonist with Ki values of 1.82 nM at GAL1 and 5.1 nM at GAL2. It decreases food intake and exhibits anxiolytic activity. The peptide is used in neurobiology and behavioral research and is not approved for clinical use. |
| Molecular Formula |
C94H145N23O24
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|---|---|
| Molecular Weight |
1981.29682230949
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| Exact Mass |
1981.086
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| CAS # |
143896-17-7
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| PubChem CID |
16133821
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| Appearance |
White to off-white solid powder
|
| LogP |
2.822
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| Hydrogen Bond Donor Count |
23
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| Hydrogen Bond Acceptor Count |
25
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| Rotatable Bond Count |
54
|
| Heavy Atom Count |
141
|
| Complexity |
4360
|
| 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)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N)NC(=O)[C@H](CC5=CNC6=CC=CC=C65)NC(=O)CN)O
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| InChi Key |
OSGCBUDLRBUEGW-JZCUZNMGSA-N
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| InChi Code |
InChI=1S/C94H145N23O24/c1-46(2)33-61(82(129)100-44-76(124)115-30-19-24-71(115)93(140)117-32-20-25-72(117)94(141)116-31-18-23-70(116)91(138)104-54(14)81(128)108-63(35-48(5)6)84(131)103-53(13)80(127)107-62(34-47(3)4)83(130)101-51(11)78(97)125)109-85(132)64(36-49(7)8)110-87(134)66(38-56-26-28-58(120)29-27-56)106-75(123)43-99-79(126)52(12)102-90(137)69(45-118)113-88(135)68(40-73(96)121)111-86(133)65(37-50(9)10)112-92(139)77(55(15)119)114-89(136)67(105-74(122)41-95)39-57-42-98-60-22-17-16-21-59(57)60/h16-17,21-22,26-29,42,46-55,61-72,77,98,118-120H,18-20,23-25,30-41,43-45,95H2,1-15H3,(H2,96,121)(H2,97,125)(H,99,126)(H,100,129)(H,101,130)(H,102,137)(H,103,131)(H,104,138)(H,105,122)(H,106,123)(H,107,127)(H,108,128)(H,109,132)(H,110,134)(H,111,133)(H,112,139)(H,113,135)(H,114,136)/t51-,52-,53-,54-,55+,61-,62-,63-,64-,65-,66-,67-,68-,69-,70-,71-,72-,77-/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-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.5047 mL | 2.5236 mL | 5.0472 mL | |
| 5 mM | 0.1009 mL | 0.5047 mL | 1.0094 mL | |
| 10 mM | 0.0505 mL | 0.2524 mL | 0.5047 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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