2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. Potassium Channel Calcium Channel
  4. 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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UR 8225

UR 8225 Chemical Structure

CAS No. : 149455-36-7

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UR 8225 Related Antibodies

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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Description

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[1][2].

IC50 & Target

L-type 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.

UR 8225 Related Antibodies
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.
Molecular Weight

290.32

Formula

C18H14N2O2
CAS No.
SMILES

N#CC1=CC2=C(C(C(C)(C)C=C2N3C=CC=CC3=O)=O)C=C1
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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UR 8225 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

UR 8225149455-36-7UR8225UR-8225Potassium ChannelCalcium ChannelKcsACa2+ channelsCa channelsguinea pig tracheaSHRvoltage-gated L-type Ca2+ channelsguinea pig urinary bladder detrusor muscleWKY ratsDOCA-salt-induced hypertensive ratsrat portal vein segmentsATP-sensitive K+ channelrat aortic vascular smooth muscle cellsguinea pig papillary muscle fibresInhibitorinhibitorinhibit

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