Calciseptine

貨號 Cat. No.
C-500
規格 Size
70 μg 5x70 μg

Description

 


Calciseptine

Specific L-type Cav channel blocker









Product#: C-500













Sizes:
70 mg
5 x 70 mg














M.W.: 7036










Sequence: RICYI HKASL PRATK TCVEN TCYKM FIRTQ REYIS ERGCG CPTAM WPYQT ECCKG DRCNK










Purity: >98%












Bioassay:
Calciseptine was tested for its ability to inhibit L-type Ca2+ channels (Cav1.2, b3) heterologously expressed in Xenopus oocytes. 1 mM Calciseptine blocked 50% of these L-type currents.




















References:






















1.


Schweitz, H. et al. (1990) Toxicon 28, 847.


2.


De Weille, J.R. et al. (1991) PNAS 88, 2437.


3.

Garcia, M.C. et al. (2001) J. Membr. Biol. 184, 121.

4.

Teramoto, N. et al. (1996) Pflugers Arch. 432, 462


Calciseptine is a natural peptide isolated from the Dendroaspis p. polylepsis black mamba venom, by a modification to the procedure of Schweitz et al. 1 and purified to homogenity. Calciseptine was shown to be a specific L-type Cav channel blocker.2 In contrast, it increases L-type currents in skeletal muscle.3 Calciseptine blocks spontaneous or K+-induced contraction of cardiac and smooth muscle cells.2 Using patch clamp, it was also shown to block specifically L-type Cav channel current in neuronal cells in culture.2 For these variety of effects, the IC50's were in the range of 15-500 nM. Using the outside-out configuration of patch clamp, it was shown to reduce single L-type channels open probability and availability as recorded from Guinea pig portal vein.4

 

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