| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 1g | |||
| Other Sizes |
| Targets |
Galanin (1-16) acts as an agonist at galanin receptors in the rat ventral hippocampus (IC₅₀ ≈ 3 nM). [1]
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|---|---|
| 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]
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| 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]
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| References |
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| Additional Infomation |
Galanin (1-16) is the N-terminal fragment of the neuropeptide galanin. This fragment was prepared in this study using solid-phase synthesis and enzymatic cleavage of the full-length galanin. [1]
This fragment binds with high affinity to the hippocampal galanin receptor and acts as a complete agonist to inhibit muscarinic agonist-induced phosphatidylinositol degradation. [1] The amino acid residue [Trp²] is crucial to its activity. Replacing [Trp²] with [D-Trp²] resulted in a 500-fold decrease in receptor affinity and loss of functional agonist activity in phosphatidylinositol degradation experiments. [1] |
| Molecular Formula |
C78H116N20O21
|
|---|---|
| Molecular Weight |
1669.88000
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| Exact Mass |
1668.86
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| CAS # |
125118-77-6
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| Related CAS # |
Galanin (1-16), mouse, porcine, rat TFA
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| PubChem CID |
16132180
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| Appearance |
Typically exists as solid at room temperature
|
| LogP |
1.992
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| Hydrogen Bond Donor Count |
22
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| Hydrogen Bond Acceptor Count |
23
|
| Rotatable Bond Count |
48
|
| Heavy Atom Count |
119
|
| Complexity |
3490
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| Defined Atom Stereocenter Count |
15
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| 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
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| InChi Key |
FHTSPMGFAZMZJT-GDGJPEIESA-N
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| 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
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| 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
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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 |
| 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 | 0.5988 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 |
*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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