| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
Galanin receptors: GALR1, GALR2, and to a lesser extent GALR3. Galnon has higher potency at GALR2 (EC50 ~ 1‑5 microM) and GALR1 (EC50 ~ 5‑10 microM). It is a partial agonist at all three. Selectivity over other GPCRs is moderate.
|
|---|---|
| ln Vitro |
In vitro, galnon (0.1‑100 microM) inhibits forskolin‑stimulated cAMP accumulation in CHO cells expressing human GALR2 (IC50 ~ 2 microM). It also stimulates ERK1/2 phosphorylation and activates G protein‑coupled inward rectifier potassium channels in hippocampal neurons. No effect at u‑opioid or NPY receptors up to 30 microM.
|
| ln Vivo |
In vivo, galnon (5‑20 mg/kg i.p.) reduces food intake in food‑deprived mice and rats, similar to galanin. It also produces anxiolytic‑like effects in the elevated plus maze (5 mg/kg i.p.) and impairs spatial memory in the Morris water maze at higher doses (10 mg/kg). In pain models, galnon reduces inflammatory hyperalgesia (10 mg/kg i.p.).
|
| Enzyme Assay |
Use CHO cell membranes expressing human GALR2 (20 microg protein). Incubate with 0.5 nM [¹2⁵I]‑galanin and galnon (0.01‑100 microM) in 50 mM Tris‑HCl pH 7.4 with 5 mM MgCl2, 0.1% BSA for 60 min at RT. Non‑specific: 1 microM galanin. Filter through GF/B, wash, count. IC50 ~ 1‑5 microM for displacement. Note that galnon is less potent than galanin.
|
| Cell Assay |
Seed CHO‑GALR2 cells in 96‑well plates (40,000/well). For cAMP assay: pre‑incubate with 0.5 mM IBMX, then add galnon (0.1‑100 microM) plus 1 microM forskolin for 15 min. Measure cAMP by HTRF. For calcium assay: load with Fluo‑4 AM, add galnon (1‑100 microM) and measure fluorescence (some GALR2 coupling to Ca2+ may be weak). Use high concentrations to detect response.
|
| Animal Protocol |
Male NMRI mice (20‑30 g) for food intake. Fast overnight. Administer galnon (5, 10, 20 mg/kg i.p.) 15 min before presenting pre‑weighed food. Measure food intake at 1, 2, 4 h. Galnon reduces cumulative intake dose‑dependently. For anxiety: elevated plus maze (5 min). Galnon (5 mg/kg i.p.) increases time spent in open arms vs. vehicle. For memory: Morris water maze, galnon (10 mg/kg i.p.) increases escape latency.
|
| ADME/Pharmacokinetics |
Galnon is lipophilic, orally active. Oral bioavailability in rats ~40‑60%. t½ after i.p. ~1‑2 h. Brain penetration good (brain/plasma ~1.0). Metabolized by CYP3A4 to several oxidative metabolites. Excreted in urine and feces.
|
| Toxicity/Toxicokinetics |
Low acute toxicity: LD50 > 500 mg/kg i.p. in mice. At 20 mg/kg, mild sedation and reduced locomotor activity. No significant cardiovascular effects. Chronic toxicity not studied. Not clinically approved.
|
| References | |
| Additional Infomation |
Small molecule galanin receptor agonist. Used to probe galaninergic system functions. CAS 1217448‑19‑5 (TFA salt). Not a therapeutic. Research use only.
|
| Molecular Formula |
C42H47F3N4O8
|
|---|---|
| Molecular Weight |
792.84
|
| Exact Mass |
792.334
|
| CAS # |
1217448-19-5
|
| Related CAS # |
Galnon;475115-35-6
|
| PubChem CID |
16219413
|
| Appearance |
White to off-white solid powder
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
12
|
| Rotatable Bond Count |
14
|
| Heavy Atom Count |
57
|
| Complexity |
1280
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
CC1=CC(=O)OC2=C1C=CC(=C2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC3CCCCC3)NC(=O)OCC4C5=CC=CC=C5C6=CC=CC=C46.C(=O)(C(F)(F)F)O
|
| InChi Key |
NLKOPSMADZXEPE-WDAFUDAASA-N
|
| InChi Code |
InChI=1S/C40H46N4O6.C2HF3O2/c1-25-21-37(45)50-36-23-27(18-19-28(25)36)42-38(46)34(17-9-10-20-41)43-39(47)35(22-26-11-3-2-4-12-26)44-40(48)49-24-33-31-15-7-5-13-29(31)30-14-6-8-16-32(30)33;3-2(4,5)1(6)7/h5-8,13-16,18-19,21,23,26,33-35H,2-4,9-12,17,20,22,24,41H2,1H3,(H,42,46)(H,43,47)(H,44,48);(H,6,7)/t34-,35-;/m0./s1
|
| Chemical Name |
9H-fluoren-9-ylmethyl N-[(2S)-1-[[(2S)-6-amino-1-[(4-methyl-2-oxochromen-7-yl)amino]-1-oxohexan-2-yl]amino]-3-cyclohexyl-1-oxopropan-2-yl]carbamate;2,2,2-trifluoroacetic 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 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)
|
| Solubility (In Vitro) |
DMSO: 125 mg/mL (157.66 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2613 mL | 6.3064 mL | 12.6129 mL | |
| 5 mM | 0.2523 mL | 1.2613 mL | 2.5226 mL | |
| 10 mM | 0.1261 mL | 0.6306 mL | 1.2613 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
