Funapide (Synonyms: TV 45070; XEN402)

Name: Funapide
Brand: MedChemExpress
SKU: HY-16723
Rating: 4.5 (0 reviews)

Cat. No.: HY-16723 Purity: 99.83%: Data Sheet
COA

SDS
Handling Instructions
FAQs
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 화학구조

CAS No. : 1259933-16-8

사이즈	재고	수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

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고객리뷰

Based on 1 Customer Validation

Other Forms of Funapide:

(R)-Funapide In-stock

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Sodium Channel Isoform Specific Products:

View All Isoforms

Na_v1.1 Na_v1.2 Na_v1.3 Na_v1.4 Na_v1.5 Na_v1.6 Na_v1.7 Na_v1.8 Na_v1.9

Biological Activity
순도&문서
References
고객리뷰

제품 설명

IC₅₀ & Target^[1]

Na_v1.7

Na_v1.8

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]

In Vitro

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.

In Vivo

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.

Clinical Trial

분자량

429.35

화학식

C₂₂H₁₄F₃NO₅

CAS No.

1259933-16-8

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

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

용액&용해도

In Vitro:

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.

몰농도 계산기
농도 희석 계산기

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 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

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.

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.

순도&문서

Purity: 99.83%

Select Batch:

Data Sheet (281 KB) SDS (393 KB)

COA (261 KB) LCMS (111 KB)

Handling Instructions (2659 KB)

References

[1]. Kitano Y, et al. Inhibition of NaV1.7: the possibility of ideal analgesics. RSC Med Chem. 2022 Aug 1;13(8):895-920. [Content Brief]

[2]. Price N , et al. Safety and Efficacy of a Topical Sodium Channel Inhibitor (TV-45070) in Patients With Postherpetic Neuralgia (PHN): A Randomized, Controlled, Proof-of-Concept, Crossover Study, With a Subgroup Analysis of the Nav1.7 R1150W Genotype. Clin J Pain. 2017 Apr;33(4):310-318. [Content Brief]

Complete Stock Solution Preparation Table

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

Funapide Related Classifications

Neurological Disease Inflammation/Immunology

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:

Funapide1259933-16-8TV 45070 XEN402TV45070TV-45070XEN402XEN 402XEN-402Sodium ChannelNa channelsNa+ channelsNav1.7 channel inhibitorAnalgesicInhibitorinhibitorinhibit

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Funapide (Synonyms: TV 45070; XEN402)

고객리뷰

Other Forms of Funapide:

Funapide Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Sodium Channel Isoform Specific Products:

Biological Activity

순도&문서

References

고객리뷰

Funapide Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

Funapide Related Classifications

Keywords:

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SAFETY DATA SHEET (SDS)

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