Cat. No.: HY-161104

Kv2.1-IN-1

1 Cited Publications

고객리뷰

Based on 1 publication(s) in Google Scholar

Kv2.1-IN-1 is an orally active and blood-brain barrier penetrant Kv2.1 inhibitor with an IC₅₀ of 0.07 μM. Kv2.1-IN-1 exhibits a selectivity >130 fold over other K⁺, Na⁺, and Ca²⁺ ion channels. Kv2.1-IN-1 decreases the apoptosis of HEK293 cells induced by H₂O₂. Kv2.1-IN-1 produces significant neuroprotection efficacy in middle cerebral artery occlusion (MCAO) rat. Kv2.1-IN-1 can be used for the study of ischemic stroke.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity: 98.64%
CAS No.: 2252448-93-2
화학식: C₂₂H₂₉N₃O₃
분자량:383.48

보관:

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

Kv2.1-IN-1 Chemical Structure

CAS No.: 2252448-93-2

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Publications (1)
용액&용해도
- In Vitro
- In Vivo
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

In Vitro

Kv2.1-IN-1 (Compound 80) (0.3-3 μM) significantly reduces the apoptosis rate of HEK293 cells induced by H₂O₂^[1].

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

Parmacokinetics

Species	Dose	Route	T_1/2	C_max	AUC_0-t	AUC_0-∞	MRT_0-t	MRT_0-∞	Bioavailability	CL	T_max	F
Rat^[1]	0.5 mg/kg	i.v.	0.51 h	693 ng/mL	174 ng·h/mL	174 ng·h/mL	0.38 h	1.39 h	2100 mL/kg	2882 mL/h/kg	/	/
Rat^[1]	5 mg/kg	p.o.	1.89 h	147 ng/mL	337 ng·h/mL	355 ng·h/mL	2.05 h	2.52 h	/	/	0.65 h	20.4 mL/h/kg

In Vivo

Kv2.1-IN-1 (Compound 80) (5 mg/kg, p.o. and 1 mg/kg, i.v., single dose) in the brain is about 54.9 ng/g at 30 min (p.o.), and the concentrations of 38.2 and 14.6 ng/g (i.v.) in the brain were observed at 15 and 30 min, respectively^[1].
Kv2.1-IN-1 (0.3-3 mg/kg, i.v. and 5 mg/kg, p.o., single dose) shows anticerebral infarct efficacy in MCAO rats model^[1].

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

Animal Model:

MCAO model established in male Sprague−Dawley (SD) rats^[1]
Dosage:

0.3, 1 and 3 mg/kg, i.v. and 5 mg/kg, p.o.
Administration:

Intravenous injection (i.v.) or oral administration (p.o.), single dose
Result:

Significantly reduced the infarct volume at the dose of 1 and 3 mg/kg (i.v.) and decrease the cerebral infarction volume ratio and the behavior score noticeably at the dose of 5 mg/kg (p.o.).

Chemical Information

CAS No. 2252448-93-2
Appearance Solid
분자량 383.48
화학식 C₂₂H₂₉N₃O₃
Color White to off-white
SMILES

O=C(C1=CC(NC(C(C)C)=O)=CC=C1OCC)NC(C2=CC=CC(NC)=C2)C
선적

Room temperature in continental US; may vary elsewhere.

보관

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

Publications (1)

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Journal Impact Factor

Acta Pharmacol Sin

Glabridin as a selective Kv2.1 inhibitor ameliorates DPN pathology by disrupting the Aβ/Kv2.1/JNK/NF-κB/NLRP3/p-Tau pathway. [Abstract]

2025 Aug;46(8):2163-2179. PMID: 40113986

용액&용해도

In Vitro:

DMSO : 100 mg/mL (260.77 mM; Need ultrasonic; 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

2.6077 mL

13.0385 mL

26.0770 mL

5 mM

0.5215 mL

2.6077 mL

5.2154 mL

10 mM

0.2608 mL

1.3038 mL

2.6077 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.

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: ≥ 5 mg/mL (13.04 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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% Corn Oil

Solubility: ≥ 5 mg/mL (13.04 mM); Clear solution

This protocol yields a clear solution of ≥ 5 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 (50.0 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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)

References

[1]. Jie Zhou, et al. Discovery of 2-Ethoxy-5-isobutyramido-N-1-substituted Benzamide Derivatives as Selective Kv2.1 Inhibitors with In Vivo Neuroprotective Effects. J Med Chem. 2023 Dec 27. [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	1 mM	2.6077 mL	13.0385 mL	26.0770 mL	65.1924 mL
	5 mM	0.5215 mL	2.6077 mL	5.2154 mL	13.0385 mL
	10 mM	0.2608 mL	1.3038 mL	2.6077 mL	6.5192 mL
	15 mM	0.1738 mL	0.8692 mL	1.7385 mL	4.3462 mL
	20 mM	0.1304 mL	0.6519 mL	1.3038 mL	3.2596 mL
	25 mM	0.1043 mL	0.5215 mL	1.0431 mL	2.6077 mL
	30 mM	0.0869 mL	0.4346 mL	0.8692 mL	2.1731 mL
	40 mM	0.0652 mL	0.3260 mL	0.6519 mL	1.6298 mL
	50 mM	0.0522 mL	0.2608 mL	0.5215 mL	1.3038 mL
	60 mM	0.0435 mL	0.2173 mL	0.4346 mL	1.0865 mL
	80 mM	0.0326 mL	0.1630 mL	0.3260 mL	0.8149 mL
	100 mM	0.0261 mL	0.1304 mL	0.2608 mL	0.6519 mL

Keywords

Kv2.1-IN-1

1 Cited Publications

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Kv2.1-IN-1

Apoptosis Compound Library

Membrane Transporter/Ion Channel Compound Library

CNS-Penetrant Compound Library

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

Anti-Alzheimer's Disease Compound Library

Neuroprotective Compound Library

Neurodegenerative Disease-related Compound Library

Potassium Channel Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cell Death Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Kv2.1-IN-1

Biological Activity

Chemical Information

Publications (1)

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

Kv2.1-IN-1

Apoptosis Compound Library

Membrane Transporter/Ion Channel Compound Library

CNS-Penetrant Compound Library

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

Anti-Alzheimer's Disease Compound Library

Neuroprotective Compound Library

Neurodegenerative Disease-related Compound Library

Potassium Channel Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cell Death Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Kv2.1-IN-1

Biological Activity

Chemical Information

Publications (1)

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

Kv2.1-IN-1 Related Classifications

HY-161104 Related Classifications