HT-2157

Alias: HT-2157; HT2157; HT 2157; SNAP37889; SNAP 37889; SNAP-37889

Cat No.:V2783 Purity: ≥98%

COA Product Data Instructions for use SDS

HT-2157 (also known as SNAP 37889) is a selective, high-affinity, and competitive antagonists of galanin-3 receptor (Gal3) that has the potential for the treatment of major depressive disorder.

HT-2157 Chemical Structure CAS No.: 303149-14-6
Product category: Neuropeptide Y Receptor

This product is for research use only, not for human use. We do not sell to patients.

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Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

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J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

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Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

HT-2157 (also known as SNAP 37889) is a selective, high-affinity, and competitive antagonists of galanin-3 receptor (Gal3) that has the potential for the treatment of major depressive disorder. Administering SNAP 37889 or its more soluble analog, SNAP 398299, acutely improved the social interaction of rats. Acute SNAP 37889 has also been demonstrated to decrease guinea pig vocalizations following mother separation, lessen stress-induced hyperthermia in mice, increase punished drinking in rats, and reduce immobility and lengthen swimming times in rats during forced swim tests. Additionally, following a 14-day treatment period, SNAP 37889 prolonged social interaction times and continued to have antidepressant effects in forced swim tests with rats after a 21-day treatment period. In microdialysis studies, SNAP 37889 partially antagonized the galanin-evoked reduction in hippocampal serotonin (5-hydroxytryptamine, 5-HT), as did the 5-HT(1A) receptor antagonist WAY100635.

Biological Activity I Assay Protocols (From Reference)

Targets

Galanin-3 receptor

ln Vitro

In vitro activity: HT-2157 (SNAP 37889) is highly selective for Gal₃ over the Gal₁ and Gal₂ subtypes (Ki>10,000 nM for each subtype; n=46 of each subtype), and binds with high affinity to membranes from transiently transfected LMTK^- cells expressing the human Gal₃ receptor (Ki=17.44±0.01 nM; n>100). 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[1].

ln Vivo

In rats who prefer alcohol, the galanin-3 receptor antagonist HT-2157 (SNAP 37889) decreases operant responding for ethanol. In the iP (alcohol-preferring) rat, the novel selective GALR3 antagonist HT-2157 is used to decrease anxiety-like behavior and voluntary ethanol consumption. In either the light-dark or elevated plus maze paradigms, male intraperitoneal rats treated with HT-2157 at a dose of 30 mg/kg (i.p.) do not exhibit changes in anxiety-like behavior or altered locomotor activity. Operant responding for solutions containing ethanol, sucrose, and saccharin is decreased when HT-2157 (30 mg/kg, i.p.) is administered. The current study's overall findings demonstrate that HT-2157 (30 mg/kg, i.p.) is useful in lowering operant responding to ethanol[2].

Enzyme Assay

The ¹²⁵I-galanin displacement assay is used to determine the binding affinities for HT-2157 (SNAP 37889) and SNAP 398299 at the human Gal₁, Gal₂, and Gal₃ receptors. Furthermore, is examined for binding in a wide panel of cross-reactivity components, such as ion channels, transporters, enzymes, and G-protein-coupled receptors. The ability of HT-2157 to antagonize functional responses to galanin is examined in modified HEK-293 cells (PEAK^rapid cells) transiently cotransfected with the Gal₃ receptor and Gα_z by measuring the inhibition of adenylyl cyclase activity[1].

Animal Protocol

Rats: The effect of HT-2157 on locomotor activity is examined using adult male iP rats (n=12; 418-467 g). To make sure that any future changes in anxiety or ethanol consumption are not the result of the drug's sedative properties, locomotor activity is tested. The rats undergo three consecutive days of 60-minute sessions to acclimate to the locomotor cells (26 x 26 x 40 cm). Rats are split into two even groups and given a single injection of either HT-2157 (30 mg/kg, i.p.) or vehicle (1 ml/kg, i.p.) 30 min before they were placed in the locomotor cells for a 60-minute session in order to minimize the effect of habituation during the treatment phase. The treatments are switched around the next day, giving each rat treatment with both the vehicle and the SNAP 37889 compound. The TruScan 2.0 program automatically records movements in terms of the total distance traveled (cm), the number of moves, and the move time (s).

References

[1]. Anxiolytic- and antidepressant-like profiles of the galanin-3 receptor (Gal3) antagonists SNAP 37889 and SNAP 398299. Proc Natl Acad Sci U S A. 2005 Nov 29;102(48):17489-94.

[2]. The galanin-3 receptor antagonist, SNAP 37889, reduces operant responding for ethanol in alcohol-preferring rats. Regul Pept. 2011 Jan 17;166(1-3):59-67.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C21H13F3N2O

Molecular Weight

366.34

Exact Mass

366.1

Elemental Analysis

C, 68.85; H, 3.58; F, 15.56; N, 7.65; O, 4.37

CAS #

303149-14-6

Related CAS #

303149-14-6

Appearance

Solid powder

SMILES

C1=CC=C(C=C1)N2C3=CC=CC=C3C(=NC4=CC=CC(=C4)C(F)(F)F)C2=O

InChi Key

TXCGMRVPXUBHAL-UHFFFAOYSA-N

InChi Code

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

Chemical Name

1-phenyl-3-[3-(trifluoromethyl)phenyl]iminoindol-2-one

Synonyms

HT-2157; HT2157; HT 2157; SNAP37889; SNAP 37889; SNAP-37889

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.

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: ≥ 29 mg/mL (~79.2 mM)

Water: < 1 mg/mL

Ethanol: < 1 mg/mL

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (6.82 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 (6.82 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	2.7297 mL	13.6485 mL	27.2970 mL
	5 mM	0.5459 mL	2.7297 mL	5.4594 mL
	10 mM	0.2730 mL	1.3649 mL	2.7297 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.

Calculator

Mass

Concentration

Volume

Molecular Weight*

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
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See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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Concentration (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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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.

Note： (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.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01413932	Completed	Drug: HT-2157 Drug: Placebo	Healthy Volunteers (Part 1) Major Depressive Disorder (Part 2)	Dart NeuroScience, LLC	July 2011	Phase 1 Phase 2

Biological Data

Representative traces demonstrating that SNAP 398299 attenuates the galanin-mediated increase in outward currents in the DRNin vitro.Proc Natl Acad Sci U S A.2005 Nov 29;102(48):17489-94.
The soluble Gal3-selective antagonist, SNAP 398299, reverses thein vivoelectrophysiological effects of galanin in the DRN.Proc Natl Acad Sci U S A.2005 Nov 29;102(48):17489-94.
The Gal3-selective antagonist SNAP 37889 displays acute anxiolytic- and antidepressant-like activity in animal models.Proc Natl Acad Sci U S A.2005 Nov 29;102(48):17489-94.