Description
HT-2157 (SNAP 37889) is a selective, high-affinity, competitive antagonists of galanin-3 receptor (Gal3).
Product information
CAS Number: 303149-14-6
Molecular Weight: 366.34
Formula: C21H13F3N2O
Chemical Name: (3Z)-1-phenyl-3-{[3-(trifluoromethyl)phenyl]imino}-2,3-dihydro-1H-indol-2-one
Smiles: O=C1/C(=N\C2C=C(C=CC=2)C(F)(F)F)/C2C=CC=CC=2N1C1C=CC=CC=1
InChiKey: TXCGMRVPXUBHAL-PLRJNAJWSA-N
InChi: InChI=1S/C21H13F3N2O/c22-21(23,24)14-7-6-8-15(13-14)25-19-17-11-4-5-12-18(17)26(20(19)27)16-9-2-1-3-10-16/h1-13H/b25-19-
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : ≥ 29 mg/mL (79.16 mM).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
HT-2157 (SNAP 37889) binds with high affinity to membranes from transiently transfected LMTK- cells expressing the human Gal3 receptor (Ki=17.44±0.01 nM; n>100) and is highly selective for Gal3 over the Gal1 and Gal2 subtypes (Ki>10,000 nM for each subtype; n=46 of each subtype). When tested for the antagonism of galanin-evoked inhibition of adenylyl cyclase, HT-2157 (0.1-10 μM) produces concentration-dependent rightward shifts of the concentration-effect curve to galanin.
In Vivo:
The galanin-3 receptor antagonist, HT-2157 (SNAP 37889), reduces operant responding for ethanol in alcohol-preferring rats. The novel selective GALR3 antagonist, HT-2157, to reduce anxiety-like behaviour and voluntary ethanol consumption in the iP (alcohol-preferring) rat. Male iP rats treated with HT-2157 at a dose of 30 mg/kg (i.p.) do not show altered locomotor activity or changes in anxiety-like behaviour in the elevated plus maze or light-dark paradigms. Treatment with HT-2157 (30 mg/kg, i.p.) reduces operant responding for solutions containing ethanol, sucrose and saccharin. Collectively, results from the current study shows that HT-2157 (30 mg/kg, i.p.) is effective in reducing operant responding for ethanol, independent of a sedative effect.
Products are for research use only. Not for human use.
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