1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. iGluR
  3. HBT1

HBT1 is an effective AMPA receptor AMPA-R potentiator. HBT1 specifically binds to the ligand-binding domain (LBD) of AMPAR and enhances receptor activity only when AMPA is present., HBT1 has almost no agonistic effect (i.e., reaching the optimal concentration, and then the efficacy decreases as the concentration continues to increase) compared with traditional AMPA-R potentiator, avoiding the bell-shaped reaction of brain-derived neurotrophic factor (BDNF) production in primary neurons. HBT1 can be applicable to a wider range of neurological and psychiatric diseases (such as depression, Alzheimer's disease, etc.).

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HBT1

HBT1 Chemical Structure

CAS No. : 489408-02-8

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Description

HBT1 is an effective AMPA receptor AMPA-R potentiator. HBT1 specifically binds to the ligand-binding domain (LBD) of AMPAR and enhances receptor activity only when AMPA is present., HBT1 has almost no agonistic effect (i.e., reaching the optimal concentration, and then the efficacy decreases as the concentration continues to increase) compared with traditional AMPA-R potentiator, avoiding the bell-shaped reaction of brain-derived neurotrophic factor (BDNF) production in primary neurons. HBT1 can be applicable to a wider range of neurological and psychiatric diseases (such as depression, Alzheimer's disease, etc.)[1].

IC50 & Target[1]

AMPA Receptor

 

In Vitro

HBT1 (0.01-100 μM) activates AMPA receptors through glutamate dependence (EC₅₀ = 2.5 μM), inducing calcium ion influx in primary neurons and CHO cells with EC₅₀ values of 1.3 and 4.6 μM, respectively[1].
HBT1 (0-10 μM) concentration-dependently increases BDNF protein levels in the presence of AMPA and shows no increase of BDNF protein levels in the absence of AMPA in primary neurons and CHO cells[1].
[3H]-HBT1 (1 nM-100 μM) binds native AMPA-R with a Kd of 416 nM and inhibits rat hippocampal membranes with an IC₅₀ of 0.28 μM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

386.39

Formula

C16H17F3N4O2S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=C(C(N)=O)C(CCCC2)=C2S1)CN3N=C(C(F)(F)F)C=C3C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Purity & Documentation
References
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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HBT1
Cat. No.:
HY-122742
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