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Art. -Nr.: HY-115596

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BTT-369

BTT-369 is a Ca_Vα₁·Ca_Vβ₃ protein-protein complex antagonist with a K_i of 2.0 μM. BTT-369 inhibits Ca_V2.2 currents, with an apparent IC₅₀ value of 31 μM. BTT-369 disrupts the interaction between Ca_Vα₁ and Ca_Vβ₃ subunits. BTT-369 reduces the current density of Ca_V2.2, and shifts the voltage dependence of steady-state inactivation and activation of Ca_V2.2 to more positive potentials. BTT-369 alleviates mechanical hyperalgesia in a rat model of tibial nerve injury. BTT-369 can be used for the study of neuropathic pain.

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CAS. Nr.: 2413939-96-3
Formel: C₃₄H₂₈N₈O₂
Molecular Weight:580.64

Speicherung:

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

BTT-369 Chemical Structure

CAS. Nr.: 2413939-96-3

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Use of MCE Products

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

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

Ca_V2.2

31 μM (IC₅₀)

Alle Calcium Channel Isoform-spezifische Produkte anzeigen :

In Vitro

BTT-369 potently inhibits the protein-protein interaction between purified Ca_Vα₁-AID and Ca_Vβ₃, with a K_i value of 2.0 μM^[1].
BTT-369 (0.1-100 μM; 5 min-48 h) reduces Ca_V2.2 current density in HEK-CaV2.2 cells, and shifts the voltage dependence of Ca_V2.2 activation and steady-state inactivation toward more positive potentials^[1].

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

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t
Mice^[1]	1 mg/kg	i.v.	0.29 h	0.083 h	181.36 ng/mL	57.99
Mice^[1]	10 mg/kg	p.o.	1.99 h	1 h	164.7 ng/mL	635.555

In Vivo

BTT-369 (0.1 mg/kg; i.p.; single bolus injection) significantly reverses mechanical hypersensitivity in a rat tibial nerve injury model of neuropathic pain for at least 24 hours^[1].

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

Chemical Information

CAS. Nr. 2413939-96-3
Molecular Weight 580.64
Formel C₃₄H₂₈N₈O₂
SMILES

O=C(C1=CC=CC(C2=NN=NN2)=C1)N3N=C(C4=CC=C(OC)C=C4)CC3C5=CN(C6=CC=CC=C6)N=C5C7=CC=C(C)C=C7
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

Handling Instructions (2659 KB)

Verweise

[1]. Chen X, et al. Small-molecule Ca_Vα₁⋅Ca_Vβ antagonist suppresses neuronal voltage-gated calcium-channel trafficking. Proc Natl Acad Sci U S A. 2018;115(45):E10566-E10575. [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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