Dabuzalgron free base

Dabuzalgron is an orally active and selective α-1A adrenergic receptor agonist.

For research use only. Not for human or veterinary use.

Target Adrenergic Receptor Apoptosis

Research area Cardiovascular Disease Endocrinology

Purity >98% Stock Inquire

Data Sheet SDS COA

Dabuzalgron structure

CAS No.: 219311-44-1

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 520.00	BP-02154-250mg	In stock	Get quote
500 mg	USD 880.00	BP-02154-500mg	In stock	Get quote
1 g	USD 1,400.00	BP-02154-1g	In stock	Get quote
2 g	USD 2,280.00	BP-02154-2g	In stock	Get quote
3 g	USD 3,200.00	BP-02154-3g	In stock	Get quote

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Description

Dabuzalgron (Ro 115-1240) is an orally active and selective α-1A adrenergic receptor agonist for the treatment of urinary incontinence. Dabuzalgron protects against Doxorubicin-induced cardiotoxicity by preserving mitochondrial function .

Biological activity

In Vitro Dabuzalgron treatment increases ERK phosphorylation in a dose-dependent fashion with an EC50 of 4.8 μM. ERK1/2 activation contributes to the cardioprotective effects of Dabuzalgron. Dabuzalgron (10 μM; 4 hours) protects NRVMs from cell death due to Doxorubicin (DOX). Activation of the α1A-AR with Dabuzalgron (10 μM; 4 hours) mitigates the detrimental effects of DOX on mitochondrial membrane potential and abrogates the activation of important elements of the apoptotic response to mitochondrial damage. In Vivo Dabuzalgron (10 μg/kg; oral gavage; twice daily; for 7 days; C57Bl6J wild-type or α1A-AR knockout mice) treatment protects against DOX cardiotoxicity by activating the α1A-AR. Dabuzalgron protects against the reduction in transcripts related to mitochondrial function, up-regulates PGC1α, preserves ATP content, and reduces oxidative stress in the hearts of mice treated with DOX.

Identifiers

SMILES: CC1=C(C=CC(=C1NS(=O)(=O)C)Cl)OCC2=NCCN2
InChIKey: FOYWMEJSRSBQGB-UHFFFAOYSA-N

Specifications

MW (average): 317.7920
Formula: C₁₂H₁₆ClN₃O₃S
CAS No.: 219311-44-1
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1].Beak J, et al. An Oral Selective Alpha-1A Adrenergic Receptor Agonist Prevents Doxorubicin Cardiotoxicity. JACC Basic Transl Sci. 2017 Feb;2(1):39-53.

Same target

Search Adrenergic Receptor

Same research area

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