, mouse, porcine, rat Chemical Structure.png)
Physicochemical Properties
| Molecular Formula | C78H116N20O21 |
| Molecular Weight | 1669.88000 |
| Exact Mass | 1668.86 |
| CAS # | 125118-77-6 |
| Related CAS # | Galanin (1-16), mouse, porcine, rat TFA |
| PubChem CID | 16132180 |
| Appearance | Typically exists as solid at room temperature |
| LogP | 1.992 |
| Hydrogen Bond Donor Count | 22 |
| Hydrogen Bond Acceptor Count | 23 |
| Rotatable Bond Count | 48 |
| Heavy Atom Count | 119 |
| Complexity | 3490 |
| Defined Atom Stereocenter Count | 15 |
| SMILES | CC[C@@H]([C@H](NC([C@@H](NC([C@@H](NC([C@@H]1CCCN1C(CNC([C@@H](NC([C@@H](NC([C@@H](NC(CNC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC(CN)=O)CC2=CNC3=CC=CC=C23)=O)[C@H](O)C)=O)CC(C)C)=O)CC(N)=O)=O)CO)=O)C)=O)=O)CC4=CC=C(O)C=C4)=O)CC(C)C)=O)CC(C)C)=O)=O)=O)CC5=CN=CN5)=O)C)=O)C(O)=O)C |
| InChi Key | FHTSPMGFAZMZJT-GDGJPEIESA-N |
| InChi Code | InChI=1S/C78H116N20O21/c1-12-41(8)64(78(118)119)96-67(107)43(10)87-69(109)56(29-47-33-81-37-85-47)93-76(116)59-18-15-23-98(59)63(105)35-84-68(108)51(24-38(2)3)90-70(110)52(25-39(4)5)91-72(112)54(27-45-19-21-48(101)22-20-45)89-62(104)34-83-66(106)42(9)86-75(115)58(36-99)95-73(113)57(30-60(80)102)92-71(111)53(26-40(6)7)94-77(117)65(44(11)100)97-74(114)55(88-61(103)31-79)28-46-32-82-50-17-14-13-16-49(46)50/h13-14,16-17,19-22,32-33,37-44,51-59,64-65,82,99-101H,12,15,18,23-31,34-36,79H2,1-11H3,(H2,80,102)(H,81,85)(H,83,106)(H,84,108)(H,86,115)(H,87,109)(H,88,103)(H,89,104)(H,90,110)(H,91,112)(H,92,111)(H,93,116)(H,94,117)(H,95,113)(H,96,107)(H,97,114)(H,118,119)/t41-,42-,43-,44+,51-,52-,53-,54-,55-,56-,57-,58-,59-,64-,65-/m0/s1 |
| Chemical Name | (2S,3S)-2-[[(2S)-2-[[(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]-3-(1H-imidazol-5-yl)propanoyl]amino]propanoyl]amino]-3-methylpentanoic acid |
| 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 |
| 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
| Targets |
Galanin (1-16) acts as an agonist at galanin receptors in the rat ventral hippocampus (IC₅₀ ≈ 3 nM). [1] |
| ln Vitro |
Galanin (1-16), mouse, pig, and rat, is an agonist of hippocampus galanin receptors with a Kd of 3 nM [1]. Galanin (1-16), mice, pigs, and rats demonstrate strong biological activity on locus coeruleus neurons [2]. Galanin (1-16) displaced 125I-labeled galanin from high-affinity binding sites in a ventral hippocampal membrane preparation with an IC₅₀ of approximately 3 nM. [1] Galanin (1-16) (1 µM) significantly inhibited the carbachol (0.1 mM)-stimulated breakdown of inositol phospholipids in slices of rat ventral hippocampus, an effect identical to that of full-length galanin-(1-29). [1] |
| ln Vivo |
Intracerebroventricular administration of Galanin (1-16) (10 µg/15 µl) caused a long-lasting inhibition of the scopolamine (0.3 mg/kg, s.c.)-induced release of acetylcholine in the rat ventral hippocampus, as measured by in vivo microdialysis. This inhibition was dose-dependent in the range of 5-20 µg/15 µl. [1] |
| Animal Protocol |
For the in vivo acetylcholine release study, a dialysis probe was implanted into the ventral hippocampus of anesthetized rats. The following day, the probe was perfused with Ringer's solution containing physostigmine. After a baseline collection period, Galanin (1-16) was administered intracerebroventricularly (at doses of 5, 10, or 20 µg in 15 µl volume) 2 minutes prior to subcutaneous injection of scopolamine (0.3 mg/kg). Perfusates were collected at 20-minute intervals and analyzed for acetylcholine content. [1] |
| References |
[1]. N-terminal galanin-(1-16) fragment is an agonist at the hippocampal galanin receptor. Proc Natl Acad Sci U S A. 1989 Dec;86(23):9588-91. [2]. A short estrogen-responsive N-terminal galanin homologue found in rat brain and gut with antiserum raised against rat galanin(1-16). Neurochem Res. 2006 Feb;31(2):177-88. |
| Additional Infomation |
Galanin (1-16) is the N-terminal fragment of the neuropeptide galanin. In this study, it was prepared by both solid-phase synthesis and enzymatic cleavage of full-length galanin. [1] The fragment exhibits high-affinity binding to hippocampal galanin receptors and functions as a full agonist in inhibiting muscarinic agonist-stimulated phosphoinositide breakdown. [1] The amino acid residue [Trp²] is crucial for activity. Substitution with [D-Trp²] resulted in a 500-fold loss in receptor affinity and abolished the functional agonist activity in the phosphoinositide breakdown assay. [1] |
Solubility Data
| 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 |
| 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 (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *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). 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)] *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. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL 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). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.5988 mL | 2.9942 mL | 5.9885 mL | |
| 5 mM | 0.1198 mL | 0.5988 mL | 1.1977 mL | |
| 10 mM | 0.0599 mL | 0.2994 mL | 0.5988 mL |