2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. Padsevonil

Padsevonil  (Synonyms: UCB-0942)

製品番号: HY-109009 純度: 99.65%
COA 取扱説明書 Technical Support

Padsevonil (UCB0942) is a potent antiepileptic agent that selectively acts on presynaptic and postsynaptic targets. Padsevonil binds to synaptic vesicular protein 2 (SV2) with high affinity. Padsevonil is also a positive allosteric modulator and partial agonist of GABAAR, with high potency against α1 and α5 receptors. Padsevonil has antiepileptic effects in a variety of rodent models.

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Padsevonil

Padsevonil 構造式

CAS 番号 : 1294000-61-5

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 566 在庫あり
Solution
10 mM * 1 mL in DMSO USD 566 在庫あり
Solid
1 mg $206 在庫あり
5 mg $515 在庫あり
10 mg $755 在庫あり
25 mg $1460 在庫あり
50 mg $2260 在庫あり
100 mg $3150 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 2 publication(s) in Google Scholar

Other Forms of Padsevonil:

Padsevonil 関連抗体

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製品説明

Padsevonil (UCB0942) is a potent antiepileptic agent that selectively acts on presynaptic and postsynaptic targets. Padsevonil binds to synaptic vesicular protein 2 (SV2) with high affinity. Padsevonil is also a positive allosteric modulator and partial agonist of GABAAR, with high potency against α1 and α5 receptors. Padsevonil has antiepileptic effects in a variety of rodent models[1][2].

体外実験

Padsevonil (0.01-30 µM) regulates GABAAR activity through allosteric sites on the receptor in CHO cells that stably express human α1β2γ2 GABAAR with an EC50 of 138 nM[1].
Padsevonil (0-30 µM) enhances natural GABAAR activity in a concentration-dependent manner in primary rat neurons with an EC50 of 208 nM[1].

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

Padsevonil 関連抗体
体内実験

Padsevonil (0.014-181.4 mg/kg; intraperitoneal injection; single dose) has protective effects on the mouse model of acute epilepsy induced by 6Hz stimulation, acoustic stimulation and pilarine (HY-B0726A), with the ED50 values of 0.16, 0.17 and 0.19 mg/kg, respectively[2].
Padsevonil (0.14-30 mg/kg; intraperitoneal injection; single dose) has a protective effect in a rodent model of chronic epilepsy [2].

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

Animal Model: Kainate treated male C57BL/6 mice[2]
Dosage: 1, 3, 10 and 30 mg/kg
Administration: Intraperitoneal injection (i.p.); single dose
Result: Significantly decreased the number of hippocampal paroxysmal discharges in dose-dependent manner.
Animal Model: Platinum electrodes treated male Wistar rats[2]
Dosage: 0.14, 0.43, 1.38 and 4.33 mg/kg
Administration: Intraperitoneal injection (i.p.); single dose
Result: Produced dose-related suppression in the cumulative duration of spontaneous spike and wave discharges, and the suppression was almost complete at a dose of 4.33 mg/kg.
臨床実験
分子量

432.80

分子式

C14H14ClF5N4O2S
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C1N(C[C@@H](CC(F)(F)Cl)C1)CC(N(N=C(COC)S2)C2=N3)=C3C(F)(F)F
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (231.05 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 2.3105 mL 11.5527 mL 23.1054 mL
5 mM 0.4621 mL 2.3105 mL 4.6211 mL
10 mM 0.2311 mL 1.1553 mL 2.3105 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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: ≥ 2.5 mg/mL (5.78 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

    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: ≥ 2.5 mg/mL (5.78 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 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 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.
純度とドキュメンテーション

純度: 99.65%

COA (246 KB) LCMS (98 KB)

取扱説明書 (2659 KB)
参考文献

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3105 mL 11.5527 mL 23.1054 mL 57.7634 mL
5 mM 0.4621 mL 2.3105 mL 4.6211 mL 11.5527 mL
10 mM 0.2311 mL 1.1553 mL 2.3105 mL 5.7763 mL
15 mM 0.1540 mL 0.7702 mL 1.5404 mL 3.8509 mL
20 mM 0.1155 mL 0.5776 mL 1.1553 mL 2.8882 mL
25 mM 0.0924 mL 0.4621 mL 0.9242 mL 2.3105 mL
30 mM 0.0770 mL 0.3851 mL 0.7702 mL 1.9254 mL
40 mM 0.0578 mL 0.2888 mL 0.5776 mL 1.4441 mL
50 mM 0.0462 mL 0.2311 mL 0.4621 mL 1.1553 mL
60 mM 0.0385 mL 0.1925 mL 0.3851 mL 0.9627 mL
80 mM 0.0289 mL 0.1444 mL 0.2888 mL 0.7220 mL
100 mM 0.0231 mL 0.1155 mL 0.2311 mL 0.5776 mL
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Padsevonil Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

Padsevonil1294000-61-5UCB-0942UCB0942UCB 0942GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorCHONeuronsEpilepsy modelInhibitorinhibitorinhibit

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