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Cat. No.: 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 No.: 2413939-96-3
Formule: C₃₄H₂₈N₈O₂
Masse moléculaire:580.64

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

BTT-369 Chemical Structure

CAS No.: 2413939-96-3

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Fluorescent Dye

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

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
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Activité biologique

Description

IC₅₀ & Target^[1]

Ca_V2.2

31 μM (IC₅₀)

Voir tous les produits spécifiques à Isoform Calcium Channel :

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 No. 2413939-96-3
Masse moléculaire 580.64
Formule 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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[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]

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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.

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100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références

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BTT-369

Voir tous les produits spécifiques à Isoform Calcium Channel

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

BTT-369 Related Classifications

HY-115596 Related Classifications