1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. UCL 2077

UCL 2077 is a potassium channel and slow afterhyperpolarization (sAHP) inhibitor. UCL 2077 selectively blocks sAHP channels without affecting L-type Ca2+ currents. UCL 2077 blocks KCNQ1- and KCNQ2-containing K+ channels, decreases erg current amplitude, increases erg deactivation rate. UCL 2077 can be used for the research of hippocampus-dependent memory retrieval deficit and cardiac arrhythmias.

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UCL 2077

UCL 2077 Chemical Structure

CAS No. : 918311-87-2

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10 mM * 1 mL in DMSO
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Description

UCL 2077 is a potassium channel and slow afterhyperpolarization (sAHP) inhibitor. UCL 2077 selectively blocks sAHP channels without affecting L-type Ca2+ currents. UCL 2077 blocks KCNQ1- and KCNQ2-containing K+ channels, decreases erg current amplitude, increases erg deactivation rate. UCL 2077 can be used for the research of hippocampus-dependent memory retrieval deficit and cardiac arrhythmias[1][2][3].

In Vitro

UCL 2077 potently and selectively blocks the sAHP in cultured rat hippocampal pyramidal neurons with an IC50 of 0.5 μM[1].
UCL 2077 (0.1-100 µM) potently inhibits erg-mediated potassium current in pituitary GH3 cells with an IC50 of 4.7 µM and Kd of 5.1 µM[2].
UCL 2077 (30 µM) significantly reduces both activation (za) and deactivation (z(deact)) gating charges of IK(erg) in pituitary GH3 cells[2].
UCL 2077 (3-30 µM) concentration-dependently reduces the voltage hysteresis of IK(erg) in pituitary GH3 cells, with 10 µM decreasing the hysteresis area by approximately 50%[2].
UCL 2077 (1-100 µM) inhibits delayed-rectifier potassium current (Ik(DR)) in pituitary GH3 cells with an IC50 of 13.4 µM[2].
UCL 2077 (3-30 µM) concentration-dependently reduces the open probability of IKca channels in pituitary GH3 cells without altering single-channel amplitude, and this suppression is reversed by 9-Phenanthrol (HY-108457)[2].
UCL 2077 (3-10 µM) concentration-dependently increases spontaneous action current frequency in pituitary GH3 cells, and this effect is abolished by KCNH2 siRNA knockdown, indicating dependence on erg potassium channels[2].

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

In Vivo

UCL 2077 (0.5-2 μg/dorsal hippocampus; central infusion into dorsal hippocampus; single dose) rescues contextual fear memory retrieval in norepinephrine/epinephrine-deficient Dbh-/- mice[1].
UCL 2077 (2 μg/dorsal hippocampus; central infusion into dorsal hippocampus; single dose) fully rescues contextual fear memory retrieval in β1-adrenergic receptor-deficient β1 KO mice without altering non-specific freezing behavior[1].

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

Animal Model: hybrid 129/Sv × C57BL/6 (Dbh-/-, norepinephrine/epinephrine-deficient, 3-5 months old, both sexes)[1]
Dosage: 0.5 μg/dorsal hippocampus; 1 μg/dorsal hippocampus; 2 μg/dorsal hippocampus
Administration: central infusion into dorsal hippocampus; single dose
Result: Significantly increased freezing percentage relative to vehicle at 0.5 μg/dorsal hippocampus (p < 0.05).
Produced further significant increases in freezing percentage at 1 μg/dorsal hippocampus and 2 μg/dorsal hippocampus (p < 0.001).
Rescued contextual fear memory retrieval in a dose-dependent manner with an estimated ED50 of 0.5 μg/dorsal hippocampus.
Animal Model: hybrid 129/Sv × C57BL/6 (β1 KO, β1-adrenergic receptor-deficient, 3-5 months old, both sexes)[1]
Dosage: 2 μg/dorsal hippocampus
Administration: central infusion into dorsal hippocampus; single dose
Result: Fully rescued contextual freezing behavior in β1 KO mice (p < 0.0002), restoring freezing to levels comparable to wild-type mice.
Had no effect on freezing in pseudo-conditioned β1 KO mice (p = 0.71), indicating no non-specific enhancement of fear or freezing.
Molecular Weight

350.46

Formula

C25H22N2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C1(CNC(C2=CC=CC=C2)(C3=CC=CC=C3)C4=CC=CC=C4)=CC=CN=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (285.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8534 mL 14.2670 mL 28.5339 mL
5 mM 0.5707 mL 2.8534 mL 5.7068 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8534 mL 14.2670 mL 28.5339 mL 71.3348 mL
5 mM 0.5707 mL 2.8534 mL 5.7068 mL 14.2670 mL
10 mM 0.2853 mL 1.4267 mL 2.8534 mL 7.1335 mL
15 mM 0.1902 mL 0.9511 mL 1.9023 mL 4.7557 mL
20 mM 0.1427 mL 0.7133 mL 1.4267 mL 3.5667 mL
25 mM 0.1141 mL 0.5707 mL 1.1414 mL 2.8534 mL
30 mM 0.0951 mL 0.4756 mL 0.9511 mL 2.3778 mL
40 mM 0.0713 mL 0.3567 mL 0.7133 mL 1.7834 mL
50 mM 0.0571 mL 0.2853 mL 0.5707 mL 1.4267 mL
60 mM 0.0476 mL 0.2378 mL 0.4756 mL 1.1889 mL
80 mM 0.0357 mL 0.1783 mL 0.3567 mL 0.8917 mL
100 mM 0.0285 mL 0.1427 mL 0.2853 mL 0.7133 mL
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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.

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UCL 2077
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