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> CLP257 [1181081-71-9]

CLP257 [1181081-71-9]

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Référence HY-110143-5mg

Conditionnement : 5mg

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CLP257 is a selective K+-Cl? cotransporter KCC2 activator with an EC50 of 616 nM. CLP257 is inactive against NKCC1, GABAA receptors, KCC1, KCC3 or KCC4. CLP257 restores impaired Cl? transport in neurons with diminished KCC2 activity. CLP257 alleviates hypersensitivity in rats with neuropathic pain. CLP257 modulates plasmalemmal KCC2 protein turnover post-translationally.

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CLP257 Chemical Structure

CLP257 Chemical Structure

CAS No. : 1181081-71-9

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Based on 1 publication(s) in Google Scholar

Description

CLP257 is a selective K+-Cl? cotransporter KCC2 activator with an EC50 of 616 nM. CLP257 is inactive against NKCC1, GABAA receptors, KCC1, KCC3 or KCC4. CLP257 restores impaired Cl? transport in neurons with diminished KCC2 activity. CLP257 alleviates hypersensitivity in rats with neuropathic pain. CLP257 modulates plasmalemmal KCC2 protein turnover post-translationally[1][2].

IC50 & Target

EC50: 616 nM (KCC2)[1]
In Vitro

There is no change in [Cl?]i in HEK293-cl cells when incubated with CLP257, indicating inactivity on NKCC1, KCC1, KCC3 or KCC4. Oocyte pre-incubation with CLP257 (200 nM) increases KCC2 transport activity by 61%, but causes no change in other CCCs. Functional, dose-dependent antagonism is also observed between CLP257 and the recently characterized KCC2 antagonist VU024055119. CLP257 (50 μM) provokes < 0.2% of the effect of 5 μM muscimol in CHO cells transduced with recombinant α1β2γ2 GABAA receptors, indicating negligible agonist activity of CLP257 on GABAA receptors[1].

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

CLP257 Related Antibodies
Masse moléculaire

307.34

Formule

C14H14FN3O2S
CAS No.

1181081-71-9
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1N=C(N2CCCCN2)S/C1=C\C3=CC=C(F)C=C3O
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years

*The compound is unstable in solutions, freshly prepared is recommended.

Solvant et solubilité
In Vitro: 

DMSO : 17.86 mg/mL (58.11 mM; Need ultrasonic; 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 3.2537 mL 16.2686 mL 32.5373 mL
5 mM 0.6507 mL 3.2537 mL 6.5075 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

  • Calculateur de molarité

  • Calculateur de dilution

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

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

    Solubility: ≥ 1.79 mg/mL (5.82 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.79 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (17.9 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.
  • Protocol 2

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

    Solubility: 1.79 mg/mL (5.82 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 1.79 mg/mL. 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 (17.9 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*The compound is unstable in solutions, freshly prepared is recommended.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Pureté et documentation

Purity: 99.76%

SDS (393 KB)

COA (253 KB) HNMR (119 KB) RP-HPLC (169 KB) LCMS (207 KB)

Instruction de manipulation (2659 KB)
Références

  • [1]. Gagnon M, et al. Chloride extrusion enhancers as novel therapeutics for neurological diseases. Nat Med. 2013 Nov;19(11):1524-8.  [Content Brief]

  • [1]. Gagnon M, et al. Chloride extrusion enhancers as novel therapeutics for neurological diseases. Nat Med. 2013 Nov;19(11):1524-8.

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2537 mL 16.2686 mL 32.5373 mL 81.3431 mL
5 mM 0.6507 mL 3.2537 mL 6.5075 mL 16.2686 mL
10 mM 0.3254 mL 1.6269 mL 3.2537 mL 8.1343 mL
15 mM 0.2169 mL 1.0846 mL 2.1692 mL 5.4229 mL
20 mM 0.1627 mL 0.8134 mL 1.6269 mL 4.0672 mL
25 mM 0.1301 mL 0.6507 mL 1.3015 mL 3.2537 mL
30 mM 0.1085 mL 0.5423 mL 1.0846 mL 2.7114 mL
40 mM 0.0813 mL 0.4067 mL 0.8134 mL 2.0336 mL
50 mM 0.0651 mL 0.3254 mL 0.6507 mL 1.6269 mL
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CLP257 Related Classifications

  • Membrane Transporter/Ion Channel
  • Potassium Channel
Help & FAQs

Keywords:

CLP2571181081-71-9CLP 257CLP-257Potassium ChannelKcsAKCC2antihyperalgesicmechanicalsensitivityneuropathicplasmamembranepost-translationallyhypersensitivityInhibitorinhibitorinhibit

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