Galantide TFA is a reversible, non-specific galanin (GAL) receptor antagonist. Galantide TFA shows dose-dependent antagonism of galanin-induced K+ conductance with IC50 of 4 nM. Galantide TFA is useful in the study of neurological diseases and hormone metabolism.

Physicochemical Properties

Molecular Formula	C106H152F3N25O28S
Molecular Weight	2313.55
Related CAS #	Galantide;138579-66-5
Appearance	White to off-white solid powder
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)

Biological Activity

ln Vitro	Galantide TFA (0.1-10000 nM) 0.1–10,000 nM) blocks galanin-induced K+ conductance activation with an IC50 value of 4 nM[1]. Galantide TFA (0.1–10,000 nM) has an IC50 value of 16 nM and suppresses voltage-dependent Ba2+ currents in a dose-dependent manner[1]. Regarding voltage-dependent Ba2+ current, the highest inhibition rate of Galantide TFA (0.1–10,000 nM) is almost 40%[1].
ln Vivo	In rats with ovariectomies, galantide TFA (5 nm; intracerebroventricular injection, once) suppresses the release of luteinizing hormone caused by ovarian steroids [2]. In ovariectomized rats, the luteinizing hormone spike caused by estradiol benzoate is lessened by galantide TFA (1 and 5 nm; intravenously delivered in three split doses at 1300, 1400, and 1500 hours) [2].
Animal Protocol	Animal/Disease Models: Adult female Crl:CD(SD)BR ovarian steroid-primed ovariectomized (OVX) rats[2] Doses: 5 nm Route of Administration: Intracerebroventricularly (icv) injection; 5 nm, 60 min before GAL Experimental Results: Blocked GAL-induced LH release.
References	[1]. Galantide distinguishes putative subtypes of galanin receptors in mudpuppy parasympathetic neurons. Eur J Pharmacol. 1995 Dec 4;287(1):97-100. [2]. Role of galanin in stimulation of pituitary luteinizing hormone secretion as revealed by a specific receptor antagonist, galantide. Endocrinology. 1994 Feb;134(2):529-36.

Solubility Data

Solubility (In Vitro)

DMSO :~100 mg/mL (~43.22 mM) H2O :< 0.1 mg/mL

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (1.08 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (1.08 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 25.0 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	0.4322 mL	2.1612 mL	4.3224 mL
	5 mM	0.0864 mL	0.4322 mL	0.8645 mL
	10 mM	0.0432 mL	0.2161 mL	0.4322 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.