GALNON TFA, Inhibitor | GALNON, inhibitor
GALNON TFA (475115-35-6(free base))
Purity
98.00%
Synonyms
GALNON TFA; GALNON TFA (475115-35-6(free base)); GALNON; inhibitor
Purity/Purification
98.00%
Form/Format
Solid. Powder
Solubility
<1mg/ml refers to the product slightly soluble or insoluble
Formula
C42H47F3N4O8
SMILES
FC(F)(F)C(=O)O.O=C(OCC3c1ccccc1c2ccccc23)N[C@@H](CC4CCCCC4)C(=O)N[C@@H](CCCCN)C(=O)Nc5ccc6c(c5)OC(=O)C=C6C
Target & IC50
galanin receptor
In Vitro
Galnon stimulated insulin release potently in isolated Wistar rat islets; 100microM of the compound increased the release 8.5 times (p<0.001) at 3.3mM and 3.7 times (p<0.001) at 16.7mM glucose. Also in islet perifusions, galnon augmented several-fold both acute and late phases of insulin response to glucose. Furthermore, galnon stimulated insulin release in GK rat islets. These effects were not inhibited by the presence of galanin or the galanin receptor antagonist M35. The stimulatory effects of galnon were partly inhibited by the PKA and PKC inhibitors, H-89 and calphostin C, respectively, at 16.7 but not 3.3mM glucose. In both Wistar and GK rat islets, insulin release was stimulated by depolarization of 30mM KCl, and 100microM galnon further enhanced insulin release 1.5-2 times (p<0.05). Cytosolic calcium levels, determined by fura-2, were increased in parallel with insulin release, and the L-type Ca2+-channel blocker nimodipine suppressed insulin response to glucose and galnon[1].galnon, a GAL receptor agonist, may enhance osteoclastic bone resorption in OVX rats. Although galnon reduced bone volume, biomechanical testing revealed that bone of galnon-treated animals was mechanically superior per unit area. Taken together, galnon simultaneously improves the intrinsic quality of cortical bone whilst stimulating osteoclastic activity in the OVX rat model[2].
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
-80 degree C for 2 years in solvent
Related Product Information for GALNON, inhibitor
Galnon is a novel non-peptide galanin receptor agonist (GAL1 and GAL2 with Ki of 11.7 and 34.1uM respectively).
Product Categories/Family for GALNON, inhibitor
References
Quynh N T T, Islam S M, Anders Floren, et al. Effects of galnon, a non-peptide galanin-receptor agonist, on insulin release from rat pancreatic islets[J]. Biochem Biophys Res Commun, 2005, 328(1):213-220.
Quynh N T T, Islam S M, Anders Floren, et al. Effects of galnon, a non-peptide galanin-receptor agonist, on insulin release from rat pancreatic islets[J]. Biochem Biophys Res Commun, 2005, 328(1):213-220.
Mcgowan H W, Schuijers J A, Grills B L, et al. Galnon, a galanin receptor agonist, improves intrinsic cortical bone tissue properties but exacerbates bone loss in an ovariectomised rat model[J]. Journal of musculoskeletal & neuronal interactions, 2014, 14(2):162-172.
Mcgowan H W, Schuijers J A, Grills B L, et al. Galnon, a galanin receptor agonist, improves intrinsic cortical bone tissue properties but exacerbates bone loss in an ovariectomised rat model[J]. Journal of musculoskeletal & neuronal interactions, 2014, 14(2):162-172.
Quynh N T T, Islam S M, Anders Floren, et al. Effects of galnon, a non-peptide galanin-receptor agonist, on insulin release from rat pancreatic islets[J]. Biochem Biophys Res Commun, 2005, 328(1):213-220.
Mcgowan H W, Schuijers J A, Grills B L, et al. Galnon, a galanin receptor agonist, improves intrinsic cortical bone tissue properties but exacerbates bone loss in an ovariectomised rat model[J]. Journal of musculoskeletal & neuronal interactions, 2014, 14(2):162-172.
Mcgowan H W, Schuijers J A, Grills B L, et al. Galnon, a galanin receptor agonist, improves intrinsic cortical bone tissue properties but exacerbates bone loss in an ovariectomised rat model[J]. Journal of musculoskeletal & neuronal interactions, 2014, 14(2):162-172.
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Product Notes
The GALNON (Catalog #AAA5759345) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "GALNON TFA, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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