Art. -Nr.: HY-19958

XEN907

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XEN907 is a potent and spirooxindole blocker of Na_V1.7, with an IC₅₀ of 3 nM. XEN907 also inhibits CYP3A4 in a recombinant human enzyme assay. XEN907 can be used for the research of pain.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 98.74%
CAS. Nr.: 912656-34-9
Formel: C₂₁H₂₁NO₄
Molecular Weight:351.40

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

XEN907 Chemical Structure

CAS. Nr.: 912656-34-9

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Nav1.7

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Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.003 μM Compound: 1, XEN907	Inhibition of Homo sapiens (human) NaV1.7 expressed in HEK293 cells assessed as decrease in [14C]guanidinium influx after 2 hr by liquid scintillation counting analysis Inhibition of Homo sapiens (human) NaV1.7 expressed in HEK293 cells assessed as decrease in [14C]guanidinium influx after 2 hr by liquid scintillation counting analysis	10.1007/s00044-012-0180-1
HEK293	IC₅₀	0.003 μM Compound: 29, XEN907	Inhibition of human NaV1.7 expressed in HEK293 cells by [14C]guanidinium influx assay Inhibition of human NaV1.7 expressed in HEK293 cells by [14C]guanidinium influx assay	[PMID: 21570288]

In Vitro

XEN907 is not cytotoxic in HepG2 cells (% viable after 16 h: >99%)^[1].
XEN907 shows moderate hepatocyte stability (% remaining after 2 h: rat 21%; human 34%; dog 46%) across species^[1].

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

In Vivo

XEN907 (10 mg/kg; p.o.) exhibits moderate oral bioavailability (13 %), C_max (35 ng/mL), and AUC_last (143 h•ng/mL) in rats^[1].
XEN907 (3 mg/kg; i.v.) exhibits terminal elimination half-life (2.6 h), high plasma clearance (9.4 L/h/kg), and large volumes of distribution (35.0 L/kg) in rats^[1].

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

Chemical Information

CAS. Nr. 912656-34-9
Appearance Solid
Molecular Weight 351.40
Formel C₂₁H₂₁NO₄
Color White to off-white
SMILES

O=C(C12COC3=C1C=C(OCO4)C4=C3)N(CCCCC)C5=C2C=CC=C5
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (284.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8458 mL

14.2288 mL

28.4576 mL

5 mM

0.5692 mL

2.8458 mL

5.6915 mL

10 mM

0.2846 mL

1.4229 mL

2.8458 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 (7.11 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (7.11 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (7.11 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Chowdhury S, et al. Discovery of XEN907, a spirooxindole blocker of NaV1.7 for the treatment of pain. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3676-81. [Content Brief]

[2]. Chowdhury S, et, al. Tetracyclic spirooxindole blockers of hNaV1.7: activity in vitro and in CFA-induced inflammatory pain model. Med Chem Res (2013) 22:1825–1836.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.8458 mL	14.2288 mL	28.4576 mL	71.1440 mL
	5 mM	0.5692 mL	2.8458 mL	5.6915 mL	14.2288 mL
	10 mM	0.2846 mL	1.4229 mL	2.8458 mL	7.1144 mL
	15 mM	0.1897 mL	0.9486 mL	1.8972 mL	4.7429 mL
	20 mM	0.1423 mL	0.7114 mL	1.4229 mL	3.5572 mL
	25 mM	0.1138 mL	0.5692 mL	1.1383 mL	2.8458 mL
	30 mM	0.0949 mL	0.4743 mL	0.9486 mL	2.3715 mL
	40 mM	0.0711 mL	0.3557 mL	0.7114 mL	1.7786 mL
	50 mM	0.0569 mL	0.2846 mL	0.5692 mL	1.4229 mL
	60 mM	0.0474 mL	0.2371 mL	0.4743 mL	1.1857 mL
	80 mM	0.0356 mL	0.1779 mL	0.3557 mL	0.8893 mL
	100 mM	0.0285 mL	0.1423 mL	0.2846 mL	0.7114 mL

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XEN907

Membrane Transporter/Ion Channel Compound Library

Neuroprotective Compound Library

Sodium Channel Blocker Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Natural Product-like Compound Library

Natural Product and Natural Product-Like Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle Sodium Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

XEN907

Membrane Transporter/Ion Channel Compound Library

Neuroprotective Compound Library

Sodium Channel Blocker Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Natural Product-like Compound Library

Natural Product and Natural Product-Like Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle Sodium Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

XEN907 Related Classifications

HY-19958 Related Classifications