HT-2157
Based on 5 publication(s) in Google Scholar
HT-2157 (SNAP 37889) is a selective, high-affinity, competitive antagonists of galanin-3 receptor (Gal3).
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- Pureté: 98.0%
- CAS No.: 303149-14-6
- Formule: C21H13F3N2O
- Masse moléculaire:366.34
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Stockage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) HT-2157
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Activité biologique
Galanin-3 receptor[1]
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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 303149-14-6
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Appearance Solid
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Masse moléculaire 366.34
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Formule C21H13F3N2O
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Color Yellow to orange
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SMILES
O=C1N(C2=CC=CC=C2)C3=C(C=CC=C3)/C1=N/C4=CC=CC(C(F)(F)F)=C4
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Synonyms
SNAP 37889
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (5)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
Cuproptosis and Mitophagy Mediated by the THUMPD1/IGF2R-Dependent Suppression of AKT and Activation of AMPK Signaling Suppress Lung Adenocarcinoma Progression. [Abstract]2026 May 4:e21238. PMID: 42080375 -
Exp Neurol
Cortical spreading depolarization is a potential target for rat brain excitability modulation by Galanin. [Abstract]2023 Dec:370:114569. PMID: 37827229 -
Am J Pathol
Spexin/NPQ Induces FBJ Osteosarcoma Oncogene (Fos) and Produces Antinociceptive Effect against Inflammatory Pain in the Mouse Model. [Abstract]2019 Apr;189(4):886-899. PMID: 30664863 -
Int J Endocrinol
2020 Aug 5;2020:4913785. PMID: 32831833 -
Solvant et solubilité
DMSO : ≥ 29 mg/mL (79.16 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.82 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
Binding affinities for HT-2157 (SNAP 37889) and SNAP 398299 at the human Gal1, Gal2, and Gal3 receptors are determined by using the 125I-galanin displacement assay. Additionally, is tested for binding in a broad cross-reactivity panel that included G-protein-coupled receptors, ion channels, enzymes, and transporters. The ability of HT-2157 to antagonize functional responses to galanin is examined in modified HEK-293 cells (PEAKrapid cells) transiently cotransfected with the Gal3 receptor and Gαz by measuring the inhibition of adenylyl cyclase activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats[2]
The effect of HT-2157 on locomotor activity is examined using adult male iP rats (n=12; 418-467 g). Locomotor activity is tested to ensure that any potential change in anxiety or ethanol consumption in subsequent tests is not due to any sedative property of the drug. Rats are habituated to the locomotor cells (26×26×40 cm) for 60 minute sessions which are conducted daily for three consecutive days. To minimise the effect of habituation during the treatment phase, rats are divided into two even groups which received a single injection of either HT-2157 (30 mg/kg, i.p.) or vehicle (1 ml/kg i.p.) 30 min prior to being placed in the locomotor cells for a 60 minute session. The following day the treatments are reversed so that all rats received treatment with both the vehicle and SNAP 37889 compound. Movements in terms of number of moves, move time (s) and total distance travelled (cm), are recorded automatically using TruScan 2.0 software.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (282 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Swanson CJ, et al. 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. [Content Brief]
[2]. Ash BL, et al. 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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7297 mL | 13.6485 mL | 27.2970 mL | 68.2426 mL |
| 5 mM | 0.5459 mL | 2.7297 mL | 5.4594 mL | 13.6485 mL | |
| 10 mM | 0.2730 mL | 1.3649 mL | 2.7297 mL | 6.8243 mL | |
| 15 mM | 0.1820 mL | 0.9099 mL | 1.8198 mL | 4.5495 mL | |
| 20 mM | 0.1365 mL | 0.6824 mL | 1.3649 mL | 3.4121 mL | |
| 25 mM | 0.1092 mL | 0.5459 mL | 1.0919 mL | 2.7297 mL | |
| 30 mM | 0.0910 mL | 0.4550 mL | 0.9099 mL | 2.2748 mL | |
| 40 mM | 0.0682 mL | 0.3412 mL | 0.6824 mL | 1.7061 mL | |
| 50 mM | 0.0546 mL | 0.2730 mL | 0.5459 mL | 1.3649 mL | |
| 60 mM | 0.0455 mL | 0.2275 mL | 0.4550 mL | 1.1374 mL |
HT-2157 Related Classifications
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