(Rac)-AMG8379 (Synonyms: (Rac)-AMG8380)

Name: (Rac)-AMG8379
Brand: MedChemExpress
SKU: HY-108425B
Rating: 4.5 (1 reviews)

Cat. No.: HY-108425B Purity: 99.25%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

(Rac)-AMG8379 ((Rac)-AMG8380) is a racemate of AMG8379. AMG8379 is a potent, orally active and selective sulfonamide antagonist of NaV1.7, with IC₅₀s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively .

For research use only. We do not sell to patients.

(Rac)-AMG8379 Chemical Structure

CAS No. : 1641574-26-6

Size	Stock	Quantity
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	Get quote
100 mg	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of (Rac)-AMG8379:

AMG8379 Get quote
AMG8380 Get quote

Featured Recommendations

•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
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

hNa_v1.7

8.5 nM (IC₅₀)

mNa_v1.7

18.6 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	> 10 μM Compound: 16; AMG8380	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	> 14 μM Compound: 15; AMG8379	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	> 14 μM Compound: 16; AMG8380	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	> 14 μM Compound: 15; AMG8379	Inhibition of human Nav1.3 expressed in HEK293 cells by electrophysiology assay Inhibition of human Nav1.3 expressed in HEK293 cells by electrophysiology assay	[PMID: 31012583]
HEK293	IC₅₀	> 14 μM Compound: 16; AMG8380	Inhibition of human Nav1.3 expressed in HEK293 cells by electrophysiology assay Inhibition of human Nav1.3 expressed in HEK293 cells by electrophysiology assay	[PMID: 31012583]
HEK293	IC₅₀	> 14 μM Compound: 15; AMG8379	Inhibition of human Nav1.4 expressed in HEK293 cells by electrophysiology assay Inhibition of human Nav1.4 expressed in HEK293 cells by electrophysiology assay	[PMID: 31012583]
HEK293	IC₅₀	> 14 μM Compound: 16; AMG8380	Inhibition of human Nav1.4 expressed in HEK293 cells by electrophysiology assay Inhibition of human Nav1.4 expressed in HEK293 cells by electrophysiology assay	[PMID: 31012583]
HEK293	IC₅₀	> 14 μM Compound: 15; AMG8379	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	> 14 μM Compound: 16; AMG8380	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	> 30 μM Compound: 16; AMG8380	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	> 42 μM Compound: 16; AMG8380	Inhibition of rat Nav1.7 expressed in HEK293 cells by electrophysiology assay Inhibition of rat Nav1.7 expressed in HEK293 cells by electrophysiology assay	[PMID: 31012583]
HEK293	IC₅₀	0.0032 μM Compound: 15; AMG8379	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	0.017 μM Compound: 15; AMG8379	Inhibition of mouse Nav1.7 expressed in HEK293 cells by electrophysiology assay Inhibition of mouse Nav1.7 expressed in HEK293 cells by electrophysiology assay	[PMID: 31012583]
HEK293	IC₅₀	0.39 μM Compound: 16; AMG8380	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	0.68 μM Compound: 16; AMG8380	Inhibition of mouse Nav1.7 expressed in HEK293 cells by electrophysiology assay Inhibition of mouse Nav1.7 expressed in HEK293 cells by electrophysiology assay	[PMID: 31012583]
HEK293	IC₅₀	1.3 μM Compound: 15; AMG8379	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	2.2 μM Compound: 15; AMG8379	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	8.6 μM Compound: 15; AMG8379	Inhibition of rat Nav1.7 expressed in HEK293 cells by electrophysiology assay Inhibition of rat Nav1.7 expressed in HEK293 cells by electrophysiology assay	[PMID: 31012583]

Molecular Weight

543.93

Formula

C₂₅H₁₆ClF₂N₃O₅S

CAS No.

1641574-26-6

Appearance

Solid

Color

White to off-white

SMILES

O=S(NC1=NOC=C1)(C2=CC(C=CC(N3C4=CC(F)=C(C=C4OC)C5=CC(Cl)=CC(F)=C5)=O)=C3C=C2)=O.[Racemate]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (91.92 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	1.8385 mL	9.1924 mL	18.3847 mL
5 mM	0.3677 mL	1.8385 mL	3.6769 mL
10 mM	0.1838 mL	0.9192 mL	1.8385 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)

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: ≥ 2.08 mg/mL (3.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (3.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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.

Purity & Documentation

Purity: 99.25%

Select Batch:

Data Sheet (276 KB) SDS (251 KB)

COA (255 KB) HNMR (304 KB) LCMS (103 KB)

Handling Instructions (2659 KB)

References

[1]. Kornecook TJ, et al. Pharmacologic Characterization of AMG8379, a Potent and Selective Small Molecule Sulfonamide Antagonist of the Voltage-Gated Sodium Channel NaV1.7. J Pharmacol Exp Ther. 2017 Jul;362(1):146-160. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.8385 mL	9.1924 mL	18.3847 mL	45.9618 mL
	5 mM	0.3677 mL	1.8385 mL	3.6769 mL	9.1924 mL
	10 mM	0.1838 mL	0.9192 mL	1.8385 mL	4.5962 mL
	15 mM	0.1226 mL	0.6128 mL	1.2256 mL	3.0641 mL
	20 mM	0.0919 mL	0.4596 mL	0.9192 mL	2.2981 mL
	25 mM	0.0735 mL	0.3677 mL	0.7354 mL	1.8385 mL
	30 mM	0.0613 mL	0.3064 mL	0.6128 mL	1.5321 mL
	40 mM	0.0460 mL	0.2298 mL	0.4596 mL	1.1490 mL
	50 mM	0.0368 mL	0.1838 mL	0.3677 mL	0.9192 mL
	60 mM	0.0306 mL	0.1532 mL	0.3064 mL	0.7660 mL
	80 mM	0.0230 mL	0.1149 mL	0.2298 mL	0.5745 mL

(Rac)-AMG8379 Related Classifications

Neurological Disease

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:

(Rac)-AMG83791641574-26-6(Rac)-AMG8380Sodium ChannelNa channelsNa+ channelsracematedorsalrootgangliasulfonamideC-fibernociceptivepainitchInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Requested Quantity *

Applicant Name *

Salutation

Email Address *

Phone Number *

Department

Organization Name *

City

State

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

(Rac)-AMG8379 (Synonyms: (Rac)-AMG8380)

Customer Review

Other Forms of (Rac)-AMG8379:

(Rac)-AMG8379 Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Sodium Channel Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

(Rac)-AMG8379 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report