1. GPCR/G Protein
    Neuronal Signaling
  2. Adrenergic Receptor
  3. KUL 7211 racemate

KUL 7211 racemate 

Cat. No.: HY-19673A
Handling Instructions

KUL 7211 racemate is the racemate of KUL 7211. KUL 7211 is a selective β-adrenoceptor agonist.

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

KUL 7211 racemate Chemical Structure

KUL 7211 racemate Chemical Structure

CAS No. : 911196-40-2

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Description

KUL 7211 racemate is the racemate of KUL 7211. KUL 7211 is a selective β-adrenoceptor agonist.

IC50 & Target

β-adrenoceptor[1]

In Vitro

KUL 7211 (KUL-7211) is a new β-adrenoceptor agonist in vitro. In rat isolated organs, its selectivities, for inhibition of spontaneous uterine contraction (mediated via β2-adrenergic stimulation) and inhibition of colonic contraction (via β3-adrenergic stimulation) versus increase in atrial rate (via β1-adrenergic stimulation), are 56.3 and 242.2, respectively. KUL 7211 relaxes 80 mM KCl induced tonic contractions in both rabbit (pD2 value: 5.86±0.13, whose ureteral relaxation is mediated via β2-adrenergic stimulation) and canine (pD2 value: 6.52±0.16, via β3-adrenergic stimulation) isolated ureters in a concentration-dependent manner. These KUL 7211-induced relaxing effects are antagonized by ICI-118,551 (selective β2-adrenoceptor antagonist, pKB value: 8.91±0.24) in the rabbit ureter and by bupranolol (non-selective β-adernoceptor antagonist, pKB value: 6.85±0.12) in the canine ureter. KUL 7211 also reduces the spontaneous rhythmic contraction in a canine ureteral spiral preparation in a concentration-dependent manner, the pD2 value being 6.83±0.20. These data clearly demonstrate that KUL 7211 selectively stimulates both ureteral β2- and β3-adrenoceptors and potently relaxes ureteral smooth muscle[1].

Molecular Weight

345.39

Formula

C₁₉H₂₃NO₅

CAS No.

911196-40-2

SMILES

O=C(O)COC1=CC=C(CCNC(C)C(O)C2=CC=C(O)C=C2)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.

References
Kinase Assay
[1]

KUL 7211 (KUL-7211) is dissolved in distilled water with an equivalent molarity of HCl[1].
Experiments are carried out using rat isolated atria, uterus, and proximal colon. Rats are stunned and then killed by rapid exsanguination. Each organ is rapidly removed and suspended in a 10 or 20 mL organ bath. The bath solution is Krebs solution (118.1 mM NaCl, 4.7 mM KCl, 2.5 mM CaCl2, 1.2 mM MgSO4• 7H2O, 25.0 mM NaHCO3, 1.2 mM KH2PO4, 11.1 mM glucose) in the atria and colon experiments and Locke-Ringer solution (154 mM NaCl, 5.6 mM KCl, 2.6 mM CaCl2, 2.1 mM MgCl2, 6.0 mM NaHCO3, 2.8 mM glucose) in the uterus experiment. Each is continuously gassed with a mixture of 95% oxygen and 5% carbon dioxide at 37°C. The bath solutions contain 1 μM phentolamine, 0.5μM desipramine, and 3 0μ M hydrocortisone to block α-adrenoceptors and neuronal and extraneuronal catecholamine uptake, respectively. Spontaneous contractions are measured isometrically by means of a force-transducer and measuring system (TB-611T, AP-601G, and RPM-6004 or model 45196A, model 1829, and model 7903) connected to a thermowriting rectigraph. An initial resting tension of 5 mN is placed on each organ, and it is allowed to equilibrate for 1 h. Each preparation is exposed to only one drug[1].

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

References
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Keywords:

KUL 7211 racemateAdrenergic ReceptorBeta ReceptorInhibitorinhibitorinhibit

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