| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
M1145 targets the galanin receptor type 2 (GAL2). It is a selective GAL2 agonist with a Ki of 6.55 nM. It shows significantly higher affinity for GAL2 compared to GAL1 (Ki=587 nM) and GalR3 (Ki=497 nM). By activating GAL2 receptors, it modulates galanin signaling pathways.
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| ln Vitro |
M1145 has an additive effect on galanin signal transduction; concentrations of M1145 of 0.1 μM and above all offer a maximum transduction. The capacity of M1145 to promote IP (inositol phosphates) synthesis in CHO cells expressing GalR2 was used to test signal transduction. Treatment with M1145, which has an EC50 of 38 nM and increases IP production[1].
In vitro, M1145 is a selective GAL2 agonist with a Ki of 6.55 nM and an EC50 of 38 nM. It shows more than 90-fold higher affinity for GAL2 over GAL1 (Ki=587 nM) and a 76-fold higher affinity over GalR3 (Ki=497 nM). It has an additive effect on the signal transduction of galanin. Standard in vitro assays include receptor binding studies and functional assays measuring signaling pathway activation. |
| ln Vivo |
In vivo, M1145 has an additive effect on the signal transduction of galanin. As a selective GAL2 agonist, it would be expected to modulate galanin-mediated effects on various physiological processes. However, comprehensive in vivo efficacy data from published literature are limited. The compound is primarily used as a research tool.
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| Enzyme Assay |
For non-cell-based receptor binding assays, M1145 can be evaluated using membrane preparations from cells expressing human GAL1, GAL2, or GAL3 receptors. Radioligand binding displacement experiments are performed using a suitable radiolabeled ligand such as [125I]-galanin. Membrane homogenates are incubated with increasing concentrations of the test compound and a fixed concentration of the radioligand. Bound radioligand is separated from free by rapid filtration through glass fiber filters. Non-specific binding is determined in the presence of excess unlabeled galanin. Ki values are calculated from displacement curves using nonlinear regression analysis.
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| Cell Assay |
For in vitro cellular assays, cells expressing human GAL2 receptors are cultured in appropriate media. For functional assays, the inhibition of forskolin-stimulated cAMP accumulation is measured (as GAL2 is Gi-coupled). Cells are treated with various concentrations of M1145, and cAMP levels are measured using ELISA or HTRF-based detection. EC50 values are calculated from dose-response curves. For calcium mobilization assays, cells expressing GAL2 receptors are loaded with calcium-sensitive dyes and treated with the compound.
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| Animal Protocol |
For in vivo animal studies, M1145 can be administered to rodents via intracerebroventricular (i.c.v.) injection. In models of galanin-mediated effects, its effects on feeding behavior, pain perception, and other physiological processes are assessed. Dosing regimens vary depending on the specific model and desired exposure levels.
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| ADME/Pharmacokinetics |
M1145 has a molecular weight of 2774.23 and a molecular formula of C128H205N37O32. It is a chimeric peptide. The compound should be stored according to the manufacturer's recommendations. It is for research use only and is not intended for human consumption.
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| Toxicity/Toxicokinetics |
The toxicity profile of M1145 has not been extensively reported. As a GAL2 receptor agonist, potential adverse effects may include modulation of galanin signaling. The compound is for research use only and is not intended for human consumption. Standard safety precautions should be observed when handling the compound.
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| References | |
| Additional Infomation |
M1145 (CAS 1172089-00-7) is a chimeric peptide and a selective galanin receptor type 2 (GAL2) agonist. It has a Ki of 6.55 nM for GAL2, with more than 90-fold higher affinity for GAL2 over GAL1 and a 76-fold higher affinity over GalR3. It has an additive effect on the signal transduction of galanin. It is available for research purposes only.
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| Molecular Formula |
C128H205N37O32
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|---|---|
| Molecular Weight |
2774.22602820396
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| Exact Mass |
2773.558
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| CAS # |
1172089-00-7
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| Related CAS # |
M1145 TFA
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| PubChem CID |
71744999
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| Appearance |
White to off-white solid powder
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| LogP |
-2.9
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| Hydrogen Bond Donor Count |
36
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| Hydrogen Bond Acceptor Count |
35
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| Rotatable Bond Count |
82
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| Heavy Atom Count |
197
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| Complexity |
6480
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| Defined Atom Stereocenter Count |
24
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| SMILES |
O=C([C@@H]1CCCN1C([C@H](CC(C)C)NC([C@H](C(C)C)NC([C@@H]1CCCN1C(CNC([C@H](CC(C)C)NC([C@H](CC(C)C)NC([C@H](CC1C=CC(=CC=1)O)NC(CNC([C@H](C)NC([C@H](CO)NC([C@H](CC(N)=O)NC([C@H](CC(C)C)NC([C@H]([C@@H](C)O)NC([C@H](CC1=CNC2C=CC=CC1=2)NC([C@H](CC(N)=O)NC(CNC([C@H](CCCNC(=N)N)NC(CNC([C@H](CCCNC(=N)N)N)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)N1CCC[C@H]1C(N1CCC[C@H]1C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N)=O)C)=O)CC(C)C)=O)C)=O)CC(C)C)=O)C)=O)=O
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| InChi Key |
XIHYPTIVAPJZFP-HEPWHOECSA-N
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| InChi Code |
InChI=1S/C128H205N37O32/c1-62(2)46-81(110(181)143-60-101(174)162-42-24-32-92(162)121(192)160-102(68(13)14)122(193)158-90(51-67(11)12)124(195)164-44-26-34-94(164)126(197)165-45-27-35-95(165)125(196)163-43-25-33-93(163)120(191)147-72(18)107(178)152-83(48-64(5)6)112(183)146-71(17)106(177)151-82(47-63(3)4)111(182)144-69(15)104(132)175)153-113(184)84(49-65(7)8)154-115(186)86(52-74-36-38-76(168)39-37-74)149-99(172)57-140-105(176)70(16)145-119(190)91(61-166)159-117(188)89(55-97(131)170)156-114(185)85(50-66(9)10)157-123(194)103(73(19)167)161-118(189)87(53-75-56-139-79-30-21-20-28-77(75)79)155-116(187)88(54-96(130)169)150-100(173)59-142-109(180)80(31-23-41-138-128(135)136)148-98(171)58-141-108(179)78(129)29-22-40-137-127(133)134/h20-21,28,30,36-39,56,62-73,78,80-95,102-103,139,166-168H,22-27,29,31-35,40-55,57-61,129H2,1-19H3,(H2,130,169)(H2,131,170)(H2,132,175)(H,140,176)(H,141,179)(H,142,180)(H,143,181)(H,144,182)(H,145,190)(H,146,183)(H,147,191)(H,148,171)(H,149,172)(H,150,173)(H,151,177)(H,152,178)(H,153,184)(H,154,186)(H,155,187)(H,156,185)(H,157,194)(H,158,193)(H,159,188)(H,160,192)(H,161,189)(H4,133,134,137)(H4,135,136,138)/t69-,70-,71-,72-,73+,78-,80-,81-,82-,83-,84-,85-,86-,87-,88-,89-,90-,91-,92-,93-,94-,95-,102-,103-/m0/s1
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| Chemical Name |
(2S)-N-[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[(2S)-2-[[(2S)-1-[[(2S)-1-[(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]-4-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]carbamoyl]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]amino]-1,4-dioxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-5-carbamimidamidopentanoyl]amino]acetyl]amino]-5-carbamimidamidopentanoyl]amino]acetyl]amino]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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 | 0.3605 mL | 1.8023 mL | 3.6046 mL | |
| 5 mM | 0.0721 mL | 0.3605 mL | 0.7209 mL | |
| 10 mM | 0.0360 mL | 0.1802 mL | 0.3605 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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