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.
| Molecular Weight | 466.05 |
| Formula | C29H35NO2HCl |
| CAS Number | 136647-02-4 |
| Solubility (25°C) | DMSO: ≥10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] No authors listed. Anagrelide
[2] No authors listed. Carteolol
[3] No authors listed. Atovaquone and Proguanil
| Related Products |
|---|
| M3554 (anti-GD2 ADC)
M3554 is a novel anti-GD2 ADC designed based on humanized ch14.18 anti-GD2 antibody. M3554 has anti-tumor activity. |
| OGT2115
OGT2115 is a potent, cell-permeable and orally active heparanase inhibitor with an IC50 of 0.4 μM. OGT2115 has anti-angiogenic properties (IC50 = 1 μM). |
| DiosMetin 7-O-β-D-Glucuronide
DiosMetin 7-O-β-D-Glucuronide is an antioxidant constituent in the fruits of Luffa cylindrical. |
| Bendazac L-Lysine
Bendazac L-Lysine is an aldose reductase (AR) inhibitor, which can be used to inhibit the activity of AR in the eye to prevent cataracts. |
| Ro5-3335
Ro5-3335 acts as an inhibitor of core binding factor (CBF) leukemia. Ro5-3335 is a RUNX1-CBFβ interaction inhibitor that represses RUNX1/CBFB-dependent transactivation. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
