| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
Galanin receptors (galanin receptor 1, 2, and 3) and substance P (SP) receptors (NK1 receptor).
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|---|---|
| ln Vitro |
While galanide does not directly enhance K+ conductance, it does oppose the concentration-dependent rise in K+ conductance that galanin causes (IC50=4 nM). IBa, the voltage-dependent Ba2+ current, is inhibited by galandide, which functions similarly to galanin. Gallantide produces a maximal inhibition of roughly 40% of IBa, which is also concentration-dependent (IC50=16 nM) [3].
Galantide recognizes two classes of galanin binding sites in the rat hypothalamus with KD values of less than 0.1 nM and approximately 6 nM. It also binds to a single population of substance P (SP) receptors with a KD of approximately 40 nM. Galantide displaces 125I-monoiodo-[Tyr26]galanin from membranes of insulin-producing Rin m 5F cells with an IC50 of less than 0.1 nM. It does not activate the K+ conductance but produces a concentration-dependent antagonism of the galanin-induced increase in K+ conductance with an IC50 of 4 nM. Galantide also inhibits the voltage-dependent Ba2+ current (IBa) in a concentration-dependent manner with an IC50 of 16 nM. |
| ln Vivo |
In experienced male rats, intracerebroventricular injection of galanin (5 μg/rat) inhibited sexual behavior without causing any other motor or behavioral deficits. Similarly, injection of the galanin antagonist galanide (1 or 2 micrograms/rat) can both stimulate and counteract the effects of galanin on sexual behavior, increasing sexual arousal, motivation, and performance indicators [2]. Mild acute pancreatitis is improved by galantide (AP). Galantide can considerably lower AP-induced hyperenzymeemia by 41-49% [3]. When administered at doses ranging from 6–6000 nM, galantide was found to enhance social memory in the "social recognition" test [4].
In vivo, intracerebroventricular (i.c.v.) injection of galantide (1 or 2 µg/rat) stimulates sexual behavior in experienced male rats, improving arousal, motivation, and performance indexes, and antagonizes the inhibitory effect of galanin on sexual behavior. Galantide ameliorates mild acute pancreatitis (AP) and significantly reduces AP-induced hyperenzymemia by 41-49%. It has been found to improve social memory in the 'social recognition' test when administered i.c.v. at doses ranging from 6-6000 nM. Galantide (5 µg/rat, i.c.v.) has also been shown to inhibit sexual behavior in male rats. |
| Enzyme Assay |
Galanin receptor binding affinity is assessed using in vitro radioligand binding assays with membrane preparations from rat hypothalamus or cells expressing recombinant galanin receptors. Competitive binding with [125I]monoiodo-[Tyr26]galanin is measured. KD and IC50 values are calculated from saturation and displacement curves using nonlinear regression analysis. Substance P receptor binding is assessed using similar assays with [125I]substance P.
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| Cell Assay |
Cellular activity is evaluated in cells expressing galanin receptors, such as insulin-producing Rin m 5F cells. Cells are treated with galantide at various concentrations (typically 0.001-100 µM) and galanin-induced signaling is measured, such as K+ conductance or calcium mobilization. The inhibition of galanin-induced increase in K+ conductance is measured using electrophysiological techniques (patch-clamp). The inhibition of voltage-dependent Ba2+ current (IBa) is also assessed.
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| Animal Protocol |
In vivo studies are conducted in rodents (rats, mice). Galantide is dissolved in 0.9% saline and administered via intracerebroventricular (i.c.v.) injection. For social recognition tests, the i.c.v. injection is given immediately after removal of the juvenile at the end of the first encounter. Control rats receive an equal volume (4 µL) of saline by the same route. A minimum of 10 adult rats are used for each dose level. For acute pancreatitis models, galantide is prepared in 0.01% bovine serum albumin in saline and administered to mice. Behavioral parameters, biochemical markers (e.g., serum amylase/lipase for pancreatitis), and electrophysiological recordings are measured.
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| ADME/Pharmacokinetics |
Galantide has a molecular formula of C99H151N27O26S (or similar) and a molecular weight of approximately 2200 g/mol. The sequence is Gly-Trp-Thr-Leu-Asn-Ser-Ala-Gly-Tyr-Leu-Leu-Gly-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2. CAS Number: 138579-66-5. The compound should be stored as a powder at -80°C for 2 years or at -20°C for 1 year. In solvent, it can be stored at -80°C for 6 months or at -20°C for 1 month (sealed storage, away from moisture).
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| Toxicity/Toxicokinetics |
Specific toxicological data for galantide are not extensively published. As a research peptide, it should be handled with standard laboratory safety precautions. The compound is for research use only and not for human therapeutic applications without appropriate regulatory approval. Standard laboratory safety practices should be followed, including the use of personal protective equipment and adequate ventilation.
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| References |
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| Additional Infomation |
Galantide is a research tool compound for studying galanin receptor biology and neuropeptide signaling. It is not approved for clinical use. The compound is a chimeric peptide consisting of fragments of galanin and substance P, making it a non-specific galanin receptor antagonist. Galantide is used to investigate the role of galanin in neuroendocrine function, pain modulation, appetite regulation, and neurological disorders such as Alzheimer's disease and epilepsy. Its ability to also bind to substance P receptors adds complexity to its pharmacological profile, making it a valuable tool for studying the interactions between these two neuropeptide systems.
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| Molecular Formula |
C104H151N25O26S
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|---|---|
| Molecular Weight |
2199.561
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| Exact Mass |
2198.1
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| CAS # |
138579-66-5
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| Related CAS # |
Galantide TFA
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| PubChem CID |
16132126
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| Appearance |
White to off-white solid powder
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| LogP |
4.412
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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 |
67
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| Heavy Atom Count |
156
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| Complexity |
4770
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| Defined Atom Stereocenter Count |
17
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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)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CC3=CC=CC=C3)C(=O)N[C@@H](CC4=CC=CC=C4)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N)NC(=O)[C@H](CC5=CNC6=CC=CC=C65)NC(=O)CN)O
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| InChi Key |
TZOJVPDIYKRJSM-GKPUQKAJSA-N
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| InChi Code |
InChI=1S/C104H151N25O26S/c1-54(2)39-70(91(142)113-52-87(139)129-37-20-27-80(129)103(154)120-69(33-35-82(107)134)93(144)119-68(32-34-81(106)133)94(145)124-76(44-61-23-16-13-17-24-61)99(150)123-74(43-60-21-14-12-15-22-60)92(143)112-51-86(138)116-71(40-55(3)4)95(146)118-67(89(109)140)36-38-156-11)121-96(147)72(41-56(5)6)122-98(149)75(45-62-28-30-64(132)31-29-62)117-85(137)50-111-90(141)58(9)114-102(153)79(53-130)127-100(151)78(47-83(108)135)125-97(148)73(42-57(7)8)126-104(155)88(59(10)131)128-101(152)77(115-84(136)48-105)46-63-49-110-66-26-19-18-25-65(63)66/h12-19,21-26,28-31,49,54-59,67-80,88,110,130-132H,20,27,32-48,50-53,105H2,1-11H3,(H2,106,133)(H2,107,134)(H2,108,135)(H2,109,140)(H,111,141)(H,112,143)(H,113,142)(H,114,153)(H,115,136)(H,116,138)(H,117,137)(H,118,146)(H,119,144)(H,120,154)(H,121,147)(H,122,149)(H,123,150)(H,124,145)(H,125,148)(H,126,155)(H,127,151)(H,128,152)/t58-,59+,67-,68-,69-,70-,71-,72-,73-,74-,75-,76-,77-,78-,79-,80-,88-/m0/s1
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| Chemical Name |
(2S)-2-[[(2S)-1-[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-hydroxybutanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]propanoyl]amino]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-N-[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1,5-dioxopentan-2-yl]pentanediamide
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| Synonyms |
M15; Galantide
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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 | 0.4546 mL | 2.2732 mL | 4.5464 mL | |
| 5 mM | 0.0909 mL | 0.4546 mL | 0.9093 mL | |
| 10 mM | 0.0455 mL | 0.2273 mL | 0.4546 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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