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Art. -Nr.: HY-190745

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(R)-(+)-A11

(R)-(+)-A11 is an orally active, selective Nav1.7 voltage-gated sodium channel blocker. (R)-(+)-A11 can be used for research on neuropathic pain.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₁₈H₂₅N₃
Molecular Weight:283.41

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (285 KB)

(R)-(+)-A11 Chemical Structure

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Use of MCE Products

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

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

Biologische Aktivität

Beschreibung

(R)-(+)-A11 is an orally active, selective Nav1.7 voltage-gated sodium channel blocker. (R)-(+)-A11 can be used for research on neuropathic pain^[1].

IC₅₀ & Target

^[1]

Na_v1.7

0.98 μM (IC₅₀)

Alle Sodium Channel Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC50	0.98 μM	Tonic-state inhibition of human Nav1.7 in HEK293 cells assessed by whole-cell patch-clamp electrophysiology. Tonic-state inhibition of human Nav1.7 in HEK293 cells assessed by whole-cell patch-clamp electrophysiology.	42911690
HEK293	IC50	0.38 μM	Inactivated-state inhibition of human Nav1.7 in HEK293 cells assessed by whole-cell patch-clamp electrophysiology. Inactivated-state inhibition of human Nav1.7 in HEK293 cells assessed by whole-cell patch-clamp electrophysiology.	42911690
HEK293	IC50	46.2 μM	Tonic-state inhibition of human Nav1.1 in HEK293 cells assessed by automated whole-cell patch clamp. Tonic-state inhibition of human Nav1.1 in HEK293 cells assessed by automated whole-cell patch clamp.	42911690
HEK293	IC50	53.5 μM	Tonic-state inhibition of human Nav1.2 in HEK293 cells assessed by automated whole-cell patch clamp. Tonic-state inhibition of human Nav1.2 in HEK293 cells assessed by automated whole-cell patch clamp.	42911690
HEK293	IC50	60.1 μM	Tonic-state inhibition of human Nav1.3 in HEK293 cells assessed by automated whole-cell patch clamp. Tonic-state inhibition of human Nav1.3 in HEK293 cells assessed by automated whole-cell patch clamp.	42911690
HEK293	IC50	82.8 μM	Tonic-state inhibition of human Nav1.4 in HEK293 cells assessed by automated whole-cell patch clamp. Tonic-state inhibition of human Nav1.4 in HEK293 cells assessed by automated whole-cell patch clamp.	42911690
HEK293	IC50	52.8 μM	Tonic-state inhibition of human Nav1.5 in HEK293 cells assessed by automated whole-cell patch clamp. Tonic-state inhibition of human Nav1.5 in HEK293 cells assessed by automated whole-cell patch clamp.	42911690
HEK293	IC50	49.5 μM	Tonic-state inhibition of human Nav1.6 in HEK293 cells assessed by automated whole-cell patch clamp. Tonic-state inhibition of human Nav1.6 in HEK293 cells assessed by automated whole-cell patch clamp.	42911690
HEK293	IC50	62.5 μM	Tonic-state inhibition of human Nav1.8 in HEK293 cells assessed by automated whole-cell patch clamp. Tonic-state inhibition of human Nav1.8 in HEK293 cells assessed by automated whole-cell patch clamp.	42911690
HEK293	IC50	80.2 μM	Tonic-state inhibition of human Nav1.9 in HEK293 cells assessed by automated whole-cell patch clamp. Tonic-state inhibition of human Nav1.9 in HEK293 cells assessed by automated whole-cell patch clamp.	42911690
HEK293	IC50	100 μM	Inactivated-state inhibition of human Nav1.1 in HEK293 cells assessed by automated whole-cell patch clamp with IC50 greater than 100 μM. Inactivated-state inhibition of human Nav1.1 in HEK293 cells assessed by automated whole-cell patch clamp with IC50 greater than 100 μM.	42911690
HEK293	IC50	38.6 μM	Inactivated-state inhibition of human Nav1.2 in HEK293 cells assessed by automated whole-cell patch clamp. Inactivated-state inhibition of human Nav1.2 in HEK293 cells assessed by automated whole-cell patch clamp.	42911690
HEK293	IC50	3.2 μM	Inactivated-state inhibition of human Nav1.3 in HEK293 cells assessed by automated whole-cell patch clamp. Inactivated-state inhibition of human Nav1.3 in HEK293 cells assessed by automated whole-cell patch clamp.	42911690
HEK293	IC50	2.7 μM	Inactivated-state inhibition of human Nav1.4 in HEK293 cells assessed by automated whole-cell patch clamp. Inactivated-state inhibition of human Nav1.4 in HEK293 cells assessed by automated whole-cell patch clamp.	42911690
HEK293	IC50	10.8 μM	Inactivated-state inhibition of human Nav1.5 in HEK293 cells assessed by automated whole-cell patch clamp. Inactivated-state inhibition of human Nav1.5 in HEK293 cells assessed by automated whole-cell patch clamp.	42911690
HEK293	IC50	5.1 μM	Inactivated-state inhibition of human Nav1.6 in HEK293 cells assessed by automated whole-cell patch clamp. Inactivated-state inhibition of human Nav1.6 in HEK293 cells assessed by automated whole-cell patch clamp.	42911690
HEK293	IC50	0.20 μM	Inactivated-state inhibition of human Nav1.7 in HEK293 cells assessed by automated whole-cell patch clamp. Inactivated-state inhibition of human Nav1.7 in HEK293 cells assessed by automated whole-cell patch clamp.	42911690
HEK293	IC50	8.2 μM	Inactivated-state inhibition of human Nav1.8 in HEK293 cells assessed by automated whole-cell patch clamp. Inactivated-state inhibition of human Nav1.8 in HEK293 cells assessed by automated whole-cell patch clamp.	42911690
DRG neuron	IC50	0.42 μM	Inhibition of capsaicin-evoked CGRP release from isolated rat DRG neurons. Inhibition of capsaicin-evoked CGRP release from isolated rat DRG neurons.	42911690

In Vitro

In HEK293 cells expressing Nav subtypes, (R)-(+)-A11 exhibits the strongest inhibitory effect on Nav1.7, with a resting-state IC₅₀ of 0.98 μM and 53.9-fold selectivity for Nav1.5^[1].
(R)-(+)-A11 (10 μM) inhibits Capsaicin (HY-10448)-induced CGRP release from isolated rat DRG neurons with an IC₅₀ of 0.42 μM, and this response is significantly attenuated in Nav1.7-knockout DRG neurons^[1].

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

Parmacokinetics

Species	Dose	Route	F	T_1/2
Rat^[1]	30 mg/kg	p.o.	28.2 %	2.18 h

In Vivo

(R)-(+)-A11 (10-100 mg/kg; p.o.; single dose; 1 h before formalin injection) produces dose-dependent analgesia in the mouse formalin test, with 68% inhibition of phase II at 30 mg/kg and an ED₅₀ of 18.5 mg/kg^[1].
(R)-(+)-A11 (30 mg/kg; p.o.; once daily; starting on day 7) produces a robust and sustained reversal of CCI-induced neuropathic pain, with an MPE of 83% for mechanical allodynia at 30 mg/kg and an ED₅₀ of 17.1 mg/kg^[1].

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

Animal Model:

ICR (male, 25-30 g)^[1]
Dosage:

10 mg/kg, 30 mg/kg, 100 mg/kg
Administration:

p.o.; single administration; 1 h before formalin
Result:

Phase I and Phase II responses were dose-dependently reduced.
At 30 mg/kg p.o., Phase II inhibition was 68%.
ED50 was 18.5 mg/kg (95% CI 14.2-23.8 mg/kg).

Chemical Information

Molecular Weight 283.41
Formel C₁₈H₂₅N₃
SMILES

CC1=CC=CC2=C1N=C([C@@H](CC3CC3)N(CC)CC)N=C2
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 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]. Shim JH, et al. Discovery of a Quinazoline-Based Nav1.7 Inhibitor with MicroED-Confirmed Absolute Configuration and Oral Efficacy in Rodent Models of Neuropathic Pain. Journal of medicinal chemistry. 2026 Oct 22;69(20):24748-24766. [Content Brief]

Calculators

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)}

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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