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Merck
CN

U3885

UK-78282 monohydrochloride

≥98% (HPLC)

Synonym(s):

4-[(Diphenylmethoxy)methyl]-1-[3-(4-methoxyphenyl)propyl]-piperidine monohydrochloride

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About This Item

Empirical Formula (Hill Notation):
C29H35NO2HCl
CAS Number:
136647-02-4
Molecular Weight:
466.05
MDL number:
MFCD16875438
UNSPSC Code:
12352200
PubChem Substance ID:
329827628
NACRES:
NA.77

Key Documents

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Quality Level

100

Assay

≥98% (HPLC)

form

solid

storage condition

desiccated

color

white to off-white

solubility

DMSO: >10 mg/mL

shipped in

wet ice

storage temp.

−20°C

SMILES string

Cl.COc1ccc(CCCN2CCC(CC2)COC(c3ccccc3)c4ccccc4)cc1

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

InChI key

ZZSQARULZYQMIG-UHFFFAOYSA-N

Biochem/physiol Actions

UK-78282 blocks both Kv1.3 and Kv1.4. Kv1.3 and Kv1.4 are members of the Shaker family of voltage-gated potassium channels.
UK-78282 blocks both Kv1.3 and Kv1.4. Kv1.3 and Kv1.4 are members of the Shaker family of voltage-gated potassium channels. Kv1.3 is expressed in brain and in effector memory T (Tem) cells, and Kv1.4 is expressed in brain. Both channels are involved in setting the membrane potential of neurons. In addition, Kv1.3 maintains the membrane potential for T memory cells and is up-regulated upon T cell activation, contributing to multiple immune processes and disorders. Blockers of Kv1.3 have long been sought for therapeutic benefit, and they are also valuable tools for studying the immune system. Selective blockers of Kv1.4 are desired, as there are few if any currently available. UK-78282 is valuable for immune system studies, where the absence of Kv1.4 makes it functionally selective for Kv1.3, and it has shown suppression of T cell activation. UK-78282 is also valuable for the study of Kv1.4 function.

Features and Benefits

This compound is featured on the Potassium Channels page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Preparation Note

UK-78282 monohydrochloride dissolves in DMSO at a concentration >10 mg/ml.

Pictograms

Exclamation markEnvironment
GHS07,GHS09

Signal Word

Warning

Hazard Statements

H319,H400

Hazard Classifications

Aquatic Acute 1 - Eye Irrit. 2

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
089K4611V
089K46111
089K4611

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Ruxandra Anton et al.
International journal of molecular sciences, 22(4) (2021-03-07)
(1) Background: As membrane channels contribute to different cell functions, understanding the underlying mechanisms becomes extremely important. A large number of neuronal channels have been investigated, however, less studied are the channels expressed in the glia population, particularly in microglia.

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