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Referencia número: HY-183206

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UR 8225

UR 8225 is an orally active ATP-sensitive K⁺ channel activator with vasodilator, smooth muscle relaxant, antihypertensive, and bronchodilator activities. UR 8225 induces membrane hyperpolarization by increasing outward K⁺ conductance and reduces Ca²⁺ influx through voltage-gated L-type Ca²⁺ channels. UR 8225 reduces total peripheral vascular resistance, shortens cardiac action potential duration, inhibits agonist-induced Ca²⁺ influx, and stimulates renin release. UR 8225 induces reflex tachycardia but lacks β-adrenergic receptor blocking activity. UR 8225 is widely applicable to research in fields related to hypertension, myocardial ischemia, ventricular fibrillation, and other conditions.

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No. CAS: 149455-36-7
Fòrmula: C₁₈H₁₄N₂O₂
Peso molecular:290.32

Almacenamiento:

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

UR 8225 Chemical Structure

No. CAS: 149455-36-7

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureza y Documentación
Referencias
Calculators
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target

L-type calcium channel

Ver todos los productos específicos de isoformas Calcium Channel :

In Vitro

UR 8225 (0.05-6.9 μM) inhibits spontaneous myogenic contractions (IC₅₀=0.05 μM) and norepinephrine-induced contractions (IC₅₀=6.9 μM) in rat portal vein segments, with effects antagonized by glyburide (HY-15206)^[1].
UR 8225 (0.32-0.76 μM) relaxes spontaneous tone (EC₅₀=0.32 μM) and inhibits histamine-induced contractions (EC₅₀=0.76 μM) in isolated guinea pig trachea, with effects reversed by glyburide (HY-15206)^[1].
UR 8225 (0.1-10 μM) concentration-dependently inhibits spontaneous contractile activity in guinea pig urinary bladder detrusor muscle, significantly reduces low KCl-induced contractions at 10 μM, and only slightly inhibits Carbamoylcholine chloride (HY-B1208)-induced contractions at 10 μM^[1].

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

In Vivo

UR 8225 (0.01-0.1 mg/kg; i.v.) acts as a potent bronchodilator in anesthetized guinea pigs, with an IC₅₀ of 0.029 mg/kg for reducing metacholine-induced bronchoconstriction^[1].
UR 8225 (0.1-1 mg/kg; p.o.) produces dose-dependent, long-lasting antihypertensive effects in conscious SHR with an ED₂₀ of 0.1 mg/kg, accompanied by reflex tachycardia and transient activation of the renin-angiotensin system^[1].
UR 8225 (0.03-0.3 mg/kg; i.v.) produces dose-dependent hypotensive effects in anesthetized normotensive rats with an ED₂₀ of 0.04 mg/kg, and these effects are completely blocked by pretreatment with 20 mg/kg i.v. glyburide (HY-15206)^[1].

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

Animal Model:

Male guinea pigs (anesthetized)^[1]
Dosage:

0.01 mg/kg; 0.1 mg/kg
Administration:

i.v.
Result:

Produced a dose-related reduction in metacholine-induced bronchoconstriction, with an IC₅₀ of 0.029 mg/kg.
Decreased metacholine-induced bronchospasm by 75.5% and reduced mean arterial blood pressure by 49.9%.

Animal Model:

Normotensive rats (anesthetized)^[1]
Dosage:

0.03 mg/kg; 0.1 mg/kg; 0.3 mg/kg
Administration:

i.v.
Result:

Produced dose-dependent reductions in MAP, with an ED₂₀ of 0.04 mg/kg.
Decreased MAP by 43% at 0.1 mg/kg i.v.; this effect was reduced to 30%, 14%, and 0.4% by pretreatment with glyburide at 3 mg/kg, 10 mg/kg, and 20 mg/kg i.v., respectively, with 20 mg/kg glyburide completely blocking the hypotensive response.

Chemical Information

No. CAS 149455-36-7
Peso molecular 290.32
Fòrmula C₁₈H₁₄N₂O₂
SMILES

N#CC1=CC2=C(C(C(C)(C)C=C2N3C=CC=CC3=O)=O)C=C1
Envío

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]. Tamargo J, et al. Pharmacology of UR‐8225, a New Potassium Channel Opener[J]. Cardiovascular drug reviews, 1996, 14(3): 256-271.

[2]. Perez-Vizcaino F, et al. Effects of the novel potassium channel opener, UR-8225, on contractile responses in rat isolated smooth muscle. Br J Pharmacol. 1993;110(3):1165-1171. [Content Brief]

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How should lyophilized recombinant proteins be reconstituted and stored?

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100 mg

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