Art. -Nr.: HY-114237

GDC-0276

Kundenbewertung

Based on 1 Customer Validation

GDC-0276 is a potent, selective, reversible and orally active NaV1.7 inhibitor with an IC₅₀ value of 0.4 nM. GDC-0276 is well tolerated and exhibits a good pharmacokinetic profile. GDC-0276 has the potential for the treatment of pain and to address shortcomings of existing pain medications, such as addiction and off-target side effects.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.69%
CAS. Nr.: 1494581-70-2
Formel: C₂₄H₃₁FN₂O₄S
Molecular Weight:462.58

Speicherung:

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

GDC-0276 Chemical Structure

CAS. Nr.: 1494581-70-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Nav1.7

Alle Sodium Channel Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.011 μM Compound: 4; GDC-0276	Inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assay Inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assay	[PMID: 31012583]
HEK293	IC₅₀	0.02 μM Compound: 4; GDC-0276	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	0.049 μM Compound: 4; GDC-0276	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	0.48 μM Compound: 4; GDC-0276	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	0.0004 μM Compound: 4; GDC-0276	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	0.4 nM Compound: 4; GDC-0276	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]

In Vivo

GDC-0276 (oral adminstration; 0.5-5 mg/kg) shows enrichment of 14^C with observed specific activities of 22.6 μCi/mg. GDC-0276 is not detected in urine; however, metabolites in urine were enriched in 14^C with observed specific activities of 19.6 μCi/mg^[3].

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

Animal Model:

Six drug-naïve beagle dogs Group 1 four dogs (n=2 per sex) and Group 2 2 BDC dogs (n=2 male)^[3]
Dosage:

0.5, 1, 2, 3, 4, 5 mg/kg
Administration:

Oral adminstration
Result:

Showed mean specific activities of 12.2 µCi/mg (a 24% enrichment) (n=4 animals) and 23.5 µCi/mg (a 139% enrichment) (n=2 animals) for Groups 1 and 2, respectively.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1494581-70-2
Appearance Solid
Molecular Weight 462.58
Formel C₂₄H₃₁FN₂O₄S
Color White to off-white
SMILES

O=C(NS(=O)(N1CCC1)=O)C2=CC(C3CC3)=C(OCC4(C5)CC6CC5CC(C6)C4)C=C2F
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 : 125 mg/mL (270.22 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

2.1618 mL

10.8089 mL

21.6179 mL

5 mM

0.4324 mL

2.1618 mL

4.3236 mL

10 mM

0.2162 mL

1.0809 mL

2.1618 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 90% Corn Oil

Solubility: ≥ 6.25 mg/mL (13.51 mM); Clear solution

This protocol yields a clear solution of ≥ 6.25 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 (62.5 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 (275 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]. Rothenberg ME, et al. Safety, Tolerability, and Pharmacokinetics of GDC-0276, a Novel NaV1.7 Inhibitor, in a First-in-Human, Single- and Multiple-Dose Study i [Content Brief]

[2]. Steven J. McKerrall, et al. Nav1.7 inhibitors for the treatment of chronic pain. Bioorganic & Medicinal Chemistry Letters (2018)

[3]. Takahashi RH,et al.Unequal Absorption of Radiolabeled and Nonradiolabeled Drug from the Oral Dose Leads to Incorrect Estimates of Drug Absorption and Circulating Metabolites in a Mass Balance Study.Drug Metab Lett. 2019;13(1):37-44. [Content Brief]

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	2.1618 mL	10.8089 mL	21.6179 mL	54.0447 mL
	5 mM	0.4324 mL	2.1618 mL	4.3236 mL	10.8089 mL
	10 mM	0.2162 mL	1.0809 mL	2.1618 mL	5.4045 mL
	15 mM	0.1441 mL	0.7206 mL	1.4412 mL	3.6030 mL
	20 mM	0.1081 mL	0.5404 mL	1.0809 mL	2.7022 mL
	25 mM	0.0865 mL	0.4324 mL	0.8647 mL	2.1618 mL
	30 mM	0.0721 mL	0.3603 mL	0.7206 mL	1.8015 mL
	40 mM	0.0540 mL	0.2702 mL	0.5404 mL	1.3511 mL
	50 mM	0.0432 mL	0.2162 mL	0.4324 mL	1.0809 mL
	60 mM	0.0360 mL	0.1801 mL	0.3603 mL	0.9007 mL
	80 mM	0.0270 mL	0.1351 mL	0.2702 mL	0.6756 mL
	100 mM	0.0216 mL	0.1081 mL	0.2162 mL	0.5404 mL

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GDC-0276

Membrane Transporter/Ion Channel Compound Library

Clinical Compound Library

Neuroprotective Compound Library

Sodium Channel Blocker Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

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

GDC-0276

Membrane Transporter/Ion Channel Compound Library

Clinical Compound Library

Neuroprotective Compound Library

Sodium Channel Blocker Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

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

GDC-0276 Related Classifications

HY-114237 Related Classifications