UK 78282 hydrochlorideBlocker of KV1.3 and KV1.4 channels CAS# 136647-02-4 |
- AR-C155858
Catalog No.:BCC1367
CAS No.:496791-37-8
Quality Control & MSDS
3D structure
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| Cas No. | 136647-02-4 | SDF | Download SDF |
| PubChem ID | 53393337 | Appearance | Powder |
| Formula | C29H36ClNO2 | M.Wt | 466.05 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 50 mM in DMSO and to 30 mM in ethanol | ||
| Chemical Name | 4-(benzhydryloxymethyl)-1-[3-(4-methoxyphenyl)propyl]piperidine;hydrochloride | ||
| SMILES | COC1=CC=C(C=C1)CCCN2CCC(CC2)COC(C3=CC=CC=C3)C4=CC=CC=C4.Cl | ||
| Standard InChIKey | ZZSQARULZYQMIG-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C29H35NO2.ClH/c1-31-28-16-14-24(15-17-28)9-8-20-30-21-18-25(19-22-30)23-32-29(26-10-4-2-5-11-26)27-12-6-3-7-13-27;/h2-7,10-17,25,29H,8-9,18-23H2,1H3;1H | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Blocker of the KV1.3 and KV1.4 voltage-gated potassium channels in T lymphocytes (IC50 values are 0.28 and 0.17 μM respectively). Suppresses T lymphocyte mitogenesis; leads to membrane depolarization. Also blocks KV1.4 expressed in heart and brain. |
UK 78282 hydrochloride Dilution Calculator
UK 78282 hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.1457 mL | 10.7285 mL | 21.4569 mL | 42.9139 mL | 53.6423 mL |
| 5 mM | 0.4291 mL | 2.1457 mL | 4.2914 mL | 8.5828 mL | 10.7285 mL |
| 10 mM | 0.2146 mL | 1.0728 mL | 2.1457 mL | 4.2914 mL | 5.3642 mL |
| 50 mM | 0.0429 mL | 0.2146 mL | 0.4291 mL | 0.8583 mL | 1.0728 mL |
| 100 mM | 0.0215 mL | 0.1073 mL | 0.2146 mL | 0.4291 mL | 0.5364 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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K+ channels as targets for specific immunomodulation.[Pubmed:15120495]
Trends Pharmacol Sci. 2004 May;25(5):280-9.
The voltage-gated Kv1.3 channel and the Ca(2+)-activated IKCa1 K(+) channel are expressed in T cells in a distinct pattern that depends on the state of lymphocyte activation and differentiation. The channel phenotype changes during the progression from the resting to the activated cell state and from naive to effector memory cells, affording promise for specific immunomodulatory actions of K(+) channel blockers. In this article, we review the functional roles of these channels in both naive cells and memory cells, describe the development of selective inhibitors of Kv1.3 and IKCa1 channels, and provide a rationale for the potential therapeutic use of these inhibitors in immunological disorders.
UK-78,282, a novel piperidine compound that potently blocks the Kv1.3 voltage-gated potassium channel and inhibits human T cell activation.[Pubmed:10372812]
Br J Pharmacol. 1999 Apr;126(8):1707-16.
1. UK-78,282, a novel piperidine blocker of the T lymphocyte voltage-gated K+ channel, Kv1.3, was discovered by screening a large compound file using a high-throughput 86Rb efflux assay. This compound blocks Kv1.3 with a IC50 of approximately 200 nM and 1:1 stoichiometry. A closely related compound, CP-190,325, containing a benzyl moiety in place of the benzhydryl in UK-78,282, is significantly less potent. 2 Three lines of evidence indicate that UK-78,282 inhibits Kv1.3 in a use-dependent manner by preferentially blocking and binding to the C-type inactivated state of the channel. Increasing the fraction of inactivated channels by holding the membrane potential at - 50 mV enhances the channel's sensitivity to UK-78,282. Decreasing the number of inactivated channels by exposure to approximately 160 mM external K+ decreases the sensitivity to UK-78,282. Mutations that alter the rate of C-type inactivation also change the channel's sensitivity to UK-78,282 and there is a direct correlation between tau(h) and IC50 values. 3. Competition experiments suggest that UK-78,282 binds to residues at the inner surface of the channel overlapping the site of action of verapamil. Internal tetraethylammonium and external charybdotoxin do not compete UK-78,282's action on the channel. 4. UK-78,282 displays marked selectivity for Kv1.3 over several other closely related K+ channels, the only exception being the rapidly inactivating voltage-gated K+ channel, Kv1.4. 5. UK-78,282 effectively suppresses human T-lymphocyte activation.
