UK-78,282 hydrochloride salt form · hydrochloride · Parent UK-78,282 hydrochloride · Synonyms: UK-78282 hydrochloride
UK-78282, a novel piperidine, potent and selective Kv1.3 blocker with an IC50 of 200 nM.
For research use only. Not for human or veterinary use.
UK-78,282 hydrochloride structure
CAS No.: 136647-02-4
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 250 mg | USD 440.00 | BP-02177A-250mg | In stock | Get quote |
| 500 mg | USD 700.00 | BP-02177A-500mg | In stock | Get quote |
| 1 g | USD 1,120.00 | BP-02177A-1g | In stock | Get quote |
| 2 g | USD 1,800.00 | BP-02177A-2g | In stock | Get quote |
| 3 g | USD 2,160.00 | BP-02177A-3g | In stock | Get quote |
| 5 g | USD 2,800.00 | BP-02177A-5g | In stock | Get quote |
Need another size or custom synthesis? Request a quote.
Description
UK-78282, a novel piperidine, potent and selective Kv1.3 blocker with an IC50 of 200 nM. UK-78,282 effectively suppresses human T-lymphocyte activation in vitro. UK-78,282 binds to residues at the inner surface of the channel overlapping the site of action of verapamil[1].
Biological activity
In Vitro UK‑78282 hydrochloride blocks Kv1.3 channel function in various cell models. Under acute administration conditions, this compound blocks native Kv1.3 channels in human peripheral blood T lymphoblasts (IC50 = 202 nM), recombinant Kv1.3 channels in L929 cells (IC50 = 280 nM), and Kv1.3 channels in RBL cells (IC50 = 333 nM); it inhibits Kv1.3-mediated 86Rb efflux in human T cells (IC50 = 0.4 μM); and it inhibits the binding of 125I‑ChTX to Kv1.3 expressed in HeLa cells (IC50 = 0.7 μM)[1]. UK‑78282 hydrochloride produces use-dependent block of Kv1.3 channels in human peripheral blood T lymphoblasts; the longer the duration of depolarizing pulses, the faster the establishment of steady-state block. Maintaining the holding potential at -50 mV to increase the proportion of C-type inactivated channels enhances the blocking efficacy of this compound[1]. UK-78282 hydrochloride binds to an internal site of the Kv1.3 channel in human peripheral blood T lymphoblasts. This site overlaps with the binding site of verapamil, but does not overlap with the binding sites of extracellular ChTX or intracellular TEA[1]. UK-78282 hydrochloride exhibits selectivity for Kv1.3 and Kv1.4 channels over other Kv family channels, with negligible activity on T cell KCa channels at concentrations up to 30 μM[1]. UK‑78282 (100 nM; ≥2 min) hydrochloride selectively inhibits action potential firing only in striatal projection neurons of the nucleus accumbens shell in low-motivation (lowS) rats, and slows the inactivation of their A-type potassium currents; this compound reduces the amplitude of A-type potassium currents in such neurons across three groups of rats, namely low-motivation (lowS), high-motivation (highS), and moderate-motivation (midS) rats[1]. UK‑78282 hydrochloride inhibits PHA-induced proliferation of purified human peripheral blood T cells (IC50 = 2.0 μM) by acting on the late G1/early S phase of the cell cycle; it also suppresses PHA-stimulated IL‑2 production (IC50 = 2.9 μM). In Vivo UK-78282 (1-100 nM, bilateral intracerebroventricular microinfusion, 0.5 μl per side, infusion duration 2 min + diffusion for 1 min) hydrochloride selectively enhances effort-based motivation for sucrose rewards in low-motivation Sprague-Dawley rats, with no significant effects on rats with moderate or high motivation.
Identifiers
- SMILES
-
COC1=CC=C(C=C1)CCCN2CCC(CC2)COC(C3=CC=CC=C3)C4=CC=CC=C4.Cl - InChIKey
-
ZZSQARULZYQMIG-UHFFFAOYSA-N
Specifications
- MW (average)
- 466.0550
- Formula
- C29H36ClNO2
- CAS No.
- 136647-02-4
- Physical state
- Solid
- Color
- White to off-white
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder -20°C, sealed storage, away from moisture; In solvent -20℃, 1 month;
Solubility
soluble in DMSO