rTertiapin-Q
- 貨號 Cat. No.
- RTT-170
- 規格 Size
- 5 μg 5x5 μg 10μg 10μgx10μg 0.1mg
Description
rTertiapin-Q
A Potent Blocker of Kir (Inward Rectifier) K+ Channels
| Product#: | RTT-170 |
| Sizes: |
| 5 mg |
| 5 x 5 mg |
| 10 mg |
| 5 x 10 mg |
| 0.1 mg |
Native Tertiapin Q was originally isolated from Apis mellifera bee venom.
Native and synthetic Tertiapin blocks a range of inward rectifier K+ channels (Kir),
in particular ROMK1 (Kir1.1, IC50=2nM) and GIRK (Kir3 family, IC50 for the
Kir3.1/3.4 heteromer was 8.6 nM) but with no effect on Kir2 family member.1
In accordance, it was shown to inhibit acetylcholine induced K+ currents in heart.2,3
Tertiapin-Q is a derivative of tertiapine in which a methionine is replaced by glutamine residue.
Tertiapin-Q inhibits the above-mentioned channels with similar affinities.4
| M.W.: | 2453 |
| Sequence: | ALCNC NRIII PHQCW KKCGK K |
| Purity: | >98% |
| Bioassay: |
| The biological activity of rTertiapin-Q was tested using two-electrode voltage clamp recording from Xenopus oocytes expressed Kir3.1/Kir3.4. |
 |
| A continuous current trace recorded at ?0 mV holding potential, from an oocyte injected with Kir3.1/3.4 combination. Kir currents are downward deflections, activated by perfusion of High K+ containing solution (HK (in mM): 74 NaCl, 24 KCl, 1 MgCl2, 1.8 CaCl2 and 5 HEPES, pH=7.4), the point of application is indicated at the top of the trace with a black arrow. For example of the use of this protocol to activate these channels see5. While activated, increasing concentrations (in nM) of rTertiapin-Q, were applied (arrows at the bottom of the trace). Control recordings (before activation of Kir channels) were carried with ND 96 solution. |
| References: |
1. | Jin, W. and Lu, Z. (1998) Biochemistry 37, 13291. |
2. | Drici, M.D. et al. (2000) ) British J. Pharmacol. 131, 569. |
3. | Kitamura, H. et al. (2000) J. Pharmacol. Exp. Therap. 293, 196. |
4. | Jin, W. et al. (1999) ) Biochemistry 38, 14294. |
5. | Peleg, S. et al. (2002) Neuron 33, 87. |