1. Membrane Transporter/Ion Channel
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  3. Funapide

Funapide  (Synonyms: TV 45070; XEN402)

製品番号: HY-16723 純度: 99.83%
COA 取扱説明書 Technical Support

Funapide (TV 45070; XEN402) is an orally active inhibitor of voltage-gated sodium channels (VGSC) in the peripheral nervous system with IC50 values ??of 84 nM and 54 nM for Nav1.5 and Nav1.7, respectively. Funapide has analgesic effects.

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Funapide

Funapide 構造式

CAS 番号 : 1259933-16-8

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 429 在庫あり
Solution
10 mM * 1 mL in DMSO USD 429 在庫あり
Solid
5 mg $390 在庫あり
10 mg $590 在庫あり
25 mg $950 在庫あり
50 mg $1280 在庫あり
100 mg $1730 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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Sodium Channel アイソフォーム固有の製品をすべて表示:

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製品説明

Funapide (TV 45070; XEN402) is an orally active inhibitor of voltage-gated sodium channels (VGSC) in the peripheral nervous system with IC50 values ??of 84 nM and 54 nM for Nav1.5 and Nav1.7, respectively. Funapide has analgesic effects[1][2].

IC50 & Target[1]

Nav1.7

 

Nav1.8

 

Nav1.2

601 nM (IC50)

Nav1.5

84 nM (IC50)

Nav1.6

173 nM (IC50)

Nav1.7

54 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
0.054 μM
Compound: 1;TV-45070/XEN-402
Inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay
[PMID: 31012583]
HEK293 IC50
0.084 μM
Compound: 1;TV-45070/XEN-402
Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay
[PMID: 31012583]
HEK293 IC50
0.17 μM
Compound: 1;TV-45070/XEN-402
Inhibition of human Nav1.6 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.6 expressed in HEK293 cells by electrophysiology assay
[PMID: 31012583]
HEK293 IC50
0.6 μM
Compound: 1;TV-45070/XEN-402
Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay
[PMID: 31012583]
HEK293 IC50
4.8 μM
Compound: 1;TV-45070/XEN-402
Inhibition of human Nav1.8 expressed in HEK293 cells by electrophysiology assay
Inhibition of human Nav1.8 expressed in HEK293 cells by electrophysiology assay
[PMID: 31012583]
体外実験

Funapide is a potent state-dependent voltage-gated sodium channel (VGSC) inhibitor with IC50s of 601, 84, 173 and 54 nM for NaV1.2, NaV1.5, NaV1.6 and NaV1.7, respectively[1].

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

体内実験

Funapide produces analgesia in models of hereditary erythromelalgia (IEM) and postherpetic neuropathic pain (PHN) (NaV1.7 gain-of-function mutations). In doing so, Funapide blocks Nav1.7-mediated pain associated with IEM[1][2].

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

臨床実験
分子量

429.35

分子式

C22H14F3NO5

CAS 番号
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C([C@]12COC3=C1C=C(OCO4)C4=C3)N(CC5=CC=C(C(F)(F)F)O5)C6=C2C=CC=C6

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 : 200 mg/mL (465.82 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 2.3291 mL 11.6455 mL 23.2910 mL
5 mM 0.4658 mL 2.3291 mL 4.6582 mL
10 mM 0.2329 mL 1.1646 mL 2.3291 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.

  • Molarity Calculator

  • Dilution Calculator

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

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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

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体積 (開始)

V1

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体積 (終了)

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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: ≥ 5.25 mg/mL (12.23 mM); Clear solution

    This protocol yields a clear solution of ≥ 5.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (52.5 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: ≥ 5.25 mg/mL (12.23 mM); Clear solution

    This protocol yields a clear solution of ≥ 5.25 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 (52.5 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

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(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: 99.83%

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, 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 2.3291 mL 11.6455 mL 23.2910 mL 58.2276 mL
5 mM 0.4658 mL 2.3291 mL 4.6582 mL 11.6455 mL
10 mM 0.2329 mL 1.1646 mL 2.3291 mL 5.8228 mL
15 mM 0.1553 mL 0.7764 mL 1.5527 mL 3.8818 mL
20 mM 0.1165 mL 0.5823 mL 1.1646 mL 2.9114 mL
25 mM 0.0932 mL 0.4658 mL 0.9316 mL 2.3291 mL
30 mM 0.0776 mL 0.3882 mL 0.7764 mL 1.9409 mL
40 mM 0.0582 mL 0.2911 mL 0.5823 mL 1.4557 mL
50 mM 0.0466 mL 0.2329 mL 0.4658 mL 1.1646 mL
60 mM 0.0388 mL 0.1941 mL 0.3882 mL 0.9705 mL
80 mM 0.0291 mL 0.1456 mL 0.2911 mL 0.7278 mL
100 mM 0.0233 mL 0.1165 mL 0.2329 mL 0.5823 mL
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  • 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
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製品名:
Funapide
製品番号:
HY-16723
数量:
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