UCL 2077
Based on 1 Customer Validation
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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- Pureté: 98.91%
- CAS No.: 918311-87-2
- Formule: C25H22N2
- Masse moléculaire:350.46
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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.
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.
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Animal Model:hybrid 129/Sv × C57BL/6 (Dbh-/-, norepinephrine/epinephrine-deficient, 3-5 months old, both sexes)[1]
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Dosage:0.5 μg/dorsal hippocampus; 1 μg/dorsal hippocampus; 2 μg/dorsal hippocampus
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Administration:central infusion into dorsal hippocampus; single dose
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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.
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Animal Model:hybrid 129/Sv × C57BL/6 (β1 KO, β1-adrenergic receptor-deficient, 3-5 months old, both sexes)[1]
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Dosage:2 μg/dorsal hippocampus
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Administration:central infusion into dorsal hippocampus; single dose
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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.
Chemical Information
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CAS No. 918311-87-2
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Appearance Solid
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Masse moléculaire 350.46
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Formule C25H22N2
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Color White to off-white
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SMILES
C1(CNC(C2=CC=CC=C2)(C3=CC=CC=C3)C4=CC=CC=C4)=CC=CN=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Zhang L, et al. The slow afterhyperpolarization: a target of β1-adrenergic signaling in hippocampus-dependent memory retrieval. J Neurosci. 2013;33(11):5006-5016. [Content Brief]
[2]. Hsu HT, et al. Characterization of Convergent Suppression by UCL-2077 (3-(Triphenylmethylaminomethyl)pyridine), Known to Inhibit Slow Afterhyperpolarization, of erg-Mediated Potassium Currents and Intermediate-Conductance Calcium-Activated Potassium Channels. Int J Mol Sci. 2020;21(4):1441. Published 2020 Feb 20. [Content Brief]
[3]. Barro-Soria R, et al. KCNE1 divides the voltage sensor movement in KCNQ1/KCNE1 channels into two steps. Nat Commun. 2014;5:3750. Published 2014 Apr 28. [Content Brief]
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 |
UCL 2077 Related Classifications
HY-108592 Related Classifications
Powered by Bioz
- UCL 2077
- 918311-87-2
- UCL2077
- UCL-2077
- Potassium Channel
- erg-mediated potassium channel
- IKCa channel
- pituitary GH3 cell
- L-type Ca2+ currents
- rat hippocampal pyramidal neurons
- hippocampus-dependent contextual fear memory retrieval
- potassium channel
- KCNQ2-containing K+ channels
- rat sAHP channel
- KCNQ1-containing K+ channels
- Inhibitor
- inhibitor
- inhibit