VU0463271 quarterhydrate

Name: VU0463271 quarterhydrate
Brand: MedChemExpress
SKU: HY-110110A
Rating: 4.5 (1 reviews)

Cat. No.: HY-110110A Purity: ≥98.0%: FAQs
Data Sheet SDS COA Handling Instructions

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VU0463271 quarterhydrate is a potent KCC2 antagonist, with an IC₅₀ of 61 nM.

For research use only. We do not sell to patients.

VU0463271 quarterhydrate Chemical Structure

Size	Price	Stock	Quantity
1 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
5 mg		Get quote
10 mg		Get quote

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Based on 1 publication(s) in Google Scholar

Other Forms of VU0463271 quarterhydrate:

VU0463271 In-stock

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Biological Activity
Purity & Documentation
References
Customer Review

Description

VU0463271 quarterhydrate is a potent KCC2 antagonist, with an IC₅₀ of 61 nM^[1].

IC₅₀ & Target

IC50: 61 nM (KCC2)^[1].

In Vitro

VU0463271 is a potent antagonist of the neuronal-specific potassium-chloride cotransporter 2 (KCC2), with an IC₅₀ of 61 nM and >100-fold selectivity versus the closely related Na-K-2Cl cotransporter 1 (NKCC1) and no activity in a larger panel of GPCRs, ion channels and transporters. It is also found rapidly cleared in vitro^[1].
VU0463271 is applied to the transected CNS preparation and resulted in a significant increase in firing rates of the Drosophila CNS with 1 μM VU0463271 resulting in a peak firing rate that was a 2.7- and 2.5-fold increase over baseline firing rate for OR and rdl strains, respectively^[2].
VU0463271 (10-100 nM) results in approximately 20% reduction of CNS firing frequency within a small percentage of preparations^[2].

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

In Vivo

VU0463271 is found to be a moderate-to-high clearance compound in rat (CL=57 mL/min/kg) following intravenous administration (1 mg/kg); the low volume of distribution at steady state (Vss 0.4 L/kg), coupled with moderate-to-high clearance produce a relatively short t1/2 (9 min) in vivo^[1].

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

Molecular Weight

387.00

Formula

C₁₉H₁₈N₄OS₂.1/4H₂O

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N(C1CC1)C2=NC(C)=CS2)CSC3=NN=C(C4=CC=CC=C4)C=C3.[1/4].O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 19 mg/mL (49.10 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5840 mL	12.9199 mL	25.8398 mL
5 mM	0.5168 mL	2.5840 mL	5.1680 mL
10 mM	0.2584 mL	1.2920 mL	2.5840 mL

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

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: ≥98.0%

Select Batch:

Data Sheet (276 KB) SDS (251 KB)

COA (251 KB)

Handling Instructions (2659 KB)

References

[1]. Delpire E, et al. Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: development of a highly selective and more potent in vitro probe. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4532-5. [Content Brief]

[2]. Rui Chen, et al. Functional Coupling of K +-Cl - Cotransporter (KCC) to GABA-Gated Cl - Channels in the Central Nervous System of Drosophila melanogaster Leads to Altered Drug Sensitivities. ACS Chem Neurosci. 2019 Jun 19;10(6):2765-2776. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5840 mL	12.9199 mL	25.8398 mL	64.5995 mL
	5 mM	0.5168 mL	2.5840 mL	5.1680 mL	12.9199 mL
	10 mM	0.2584 mL	1.2920 mL	2.5840 mL	6.4599 mL
	15 mM	0.1723 mL	0.8613 mL	1.7227 mL	4.3066 mL
	20 mM	0.1292 mL	0.6460 mL	1.2920 mL	3.2300 mL
	25 mM	0.1034 mL	0.5168 mL	1.0336 mL	2.5840 mL
	30 mM	0.0861 mL	0.4307 mL	0.8613 mL	2.1533 mL
	40 mM	0.0646 mL	0.3230 mL	0.6460 mL	1.6150 mL