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Referencia número: 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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No. CAS: 2413939-96-3
Fòrmula: C₃₄H₂₈N₈O₂
Peso molecular:580.64

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

BTT-369 Chemical Structure

No. CAS: 2413939-96-3

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
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Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

Ca_V2.2

31 μM (IC₅₀)

Ver todos los productos específicos de isoformas 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

No. CAS 2413939-96-3
Peso molecular 580.64
Fòrmula 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
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Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[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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Actividad biológica
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- IC₅₀ & Target
- In Vitro
- In Vivo
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BTT-369

Ver todos los productos específicos de isoformas Calcium Channel

Actividad biológica

Chemical Information

Pureza y Documentación

Referencias

Calculators

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BTT-369 Related Classifications

HY-115596 Related Classifications