Art. -Nr.: HY-107601

UBP316

(Synonyms: ACET)

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UBP316 (ACET) is a highly potent and selective kainate receptor GluK1 (GluR5) antagonist, with a K_b value of 1.4 nM. UBP316 is effective at blocking the depression of both field excitatory postsynaptic potentials (fEPSPs) and monosynaptically-evoked GABAergic transmission induced by ATPA, a GluK1 selective agonist.

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Reinheit: 99.06%
CAS. Nr.: 936095-50-0
Formel: C₂₀H₁₉N₃O₆S
Molecular Weight:429.45

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

UBP316 Chemical Structure

CAS. Nr.: 936095-50-0

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Kb: 1.4 nM (GluK1)^[1]

Alle iGluR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	>100 μM Compound: 67	Antagonist activity at human recombinant GLUA2-AMPA receptor expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay Antagonist activity at human recombinant GLUA2-AMPA receptor expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay	[PMID: 17348638]
HEK293	IC₅₀	>100 μM Compound: 67	Antagonist activity at human recombinant GLUK6 expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay Antagonist activity at human recombinant GLUK6 expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay	[PMID: 17348638]
HEK293	IC₅₀	>100 μM Compound: 67	Antagonist activity at human recombinant GLUK6/GLUK2 expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay Antagonist activity at human recombinant GLUK6/GLUK2 expressed in HEK293 cells assessed as inhibition of glutamate-stimulated calcium influx by FLIPR assay	[PMID: 17348638]

In Vitro

UBP316 is ineffective at GluK2 (GluR6) receptors at all concentrations tested (up to 100 μM) and had no effect at GluK3 (GluR7) when tested at 1 μM^[1].
UBP316 (200 nM) reduces short-term facilitation of pre-synaptic calcium transients following repetitive spikes^[1].
UBP316 effectively antagonises GluK1-mediated depression of excitatory transmission in CA1 region of the hippocampus in vitro^[1].
UBP316 blocks induction of NMDA receptor-independent long-term potentiation (LTP)^[1].

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

Chemical Information

CAS. Nr. 936095-50-0
Appearance Solid
Molecular Weight 429.45
Formel C₂₀H₁₉N₃O₆S
Color White to off-white
SMILES

OC(C(SC(C1=CC=CC=C1)=C2)=C2CN3C(N(C=C(C)C3=O)C[C@H](N)C(O)=O)=O)=O
Synonyms

ACET
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

1M NaOH : 80 mg/mL (186.28 mM; ultrasonic and adjust pH to 11 with NaOH)

DMSO : 2 mg/mL (4.66 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3286 mL

11.6428 mL

23.2856 mL

5 mM

0.4657 mL

2.3286 mL

4.6571 mL

10 mM

0.2329 mL

1.1643 mL

2.3286 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 0.2 mg/mL (0.47 mM); Clear solution

This protocol yields a clear solution of ≥ 0.2 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (2.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 0.2 mg/mL (0.47 mM); Clear solution

This protocol yields a clear solution of ≥ 0.2 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (2.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 0.2 mg/mL (0.47 mM); Clear solution

This protocol yields a clear solution of ≥ 0.2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (2.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Sheila L Dargan, et al. ACET is a highly potent and specific kainate receptor antagonist: Characterisation and effects on hippocampal mossy fibre function. Neuropharmacology. 2009 Jan;56(1):121-30. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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 / 1M NaOH	1 mM	2.3286 mL	11.6428 mL	23.2856 mL	58.2140 mL
1M NaOH	5 mM	0.4657 mL	2.3286 mL	4.6571 mL	11.6428 mL
	10 mM	0.2329 mL	1.1643 mL	2.3286 mL	5.8214 mL
	15 mM	0.1552 mL	0.7762 mL	1.5524 mL	3.8809 mL
	20 mM	0.1164 mL	0.5821 mL	1.1643 mL	2.9107 mL
	25 mM	0.0931 mL	0.4657 mL	0.9314 mL	2.3286 mL
	30 mM	0.0776 mL	0.3881 mL	0.7762 mL	1.9405 mL
	40 mM	0.0582 mL	0.2911 mL	0.5821 mL	1.4553 mL
	50 mM	0.0466 mL	0.2329 mL	0.4657 mL	1.1643 mL
	60 mM	0.0388 mL	0.1940 mL	0.3881 mL	0.9702 mL
	80 mM	0.0291 mL	0.1455 mL	0.2911 mL	0.7277 mL
	100 mM	0.0233 mL	0.1164 mL	0.2329 mL	0.5821 mL

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UBP316

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High-Throughput Bioactive Compound Library

Alle iGluR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

UBP316

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Neurotransmitter Receptor Compound Library

Anti-Alzheimer's Disease Compound Library

Neuroprotective Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Antidepressant Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle iGluR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

UBP316 Related Classifications

HY-107601 Related Classifications