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Cat. No.: 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.

For research use only. We do not sell to patients.

CAS No.: 149455-36-7
Formula: C₁₈H₁₄N₂O₂
Molecular Weight:290.32

Storage:

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

UR 8225 Chemical Structure

CAS No.: 149455-36-7

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

L-type calcium channel

All Calcium Channel Isoforms :

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

CAS No. 149455-36-7
Molecular Weight 290.32
Formula C₁₈H₁₄N₂O₂
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[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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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.

Keywords

100 mg

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