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Home / Proteins & Peptide

Tertiapin-LQ

SKU : BHP21300296

A Blocker of Kir1.1, Kir3.1 and Kir3.4 K+ Channels

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Mfr.No.	STT-220, STT-220_0.5 mg, STT-220_1 mg, STT-220_10 mg, STT-220_5 mg
Description	A Blocker of Kir1.1, Kir3.1 and Kir3.4 K+ Channels
Reconstitution	Centrifuge the vial (10,000 x g for 5 minutes) before adding solvent to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Gently tap, tilt, and roll the vial to aid dissolution. Avoid vigorous vortexing; light vortexing for up to 3 seconds is acceptable if needed. The product is soluble in pure water at high micromolar concentrations (100 uM - 1 mM). For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in double-distilled water (ddH2O) at a concentration between 100-1000x of the final working concentration. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. Centrifuge all product preparations before use. It is recommended to prepare fresh solutions in working buffers just before use. Avoid multiple freeze-thaw cycles to maintain biological activity.
Molecular Formula	C106H179N33O24S4
Background	Inward-rectifier K+ (Kir) channels play many important biological roles and are emerging as important therapeutic targets. Tertiapin (TPN), a toxin present in honey bee venom (Apis mellifera) inhibits certain subtypes of inward-rectifier K+ channels1. TPN is a highly compact peptide of 21 residues. Its C-terminal portion (histidine 12 to glycine 19) adopts an alpha-helical structure, whereas the N-terminal half acquires extended conformations. Two pairs of disulfide bonds help to hold the two parts together2. Tertiapin inhibits ROMK1 (Kir1.1) and G-protein-gated channel (GIRK1/4) (Kir3.1/3.4) channels with IC50 values of 8.6 and 2.0 nM respectively and is selective over Kir2.1 channels3. In accordance, it was shown to inhibit acetylcholine induced K+ currents in mammalian cardiomyocytes4.Tertiapin-LQ is a tertiapin-Q derivative that blocks Kir1.1 channels. It does so by binding to the external vestibule of the K+-conduction pore that is formed by the linker between the first and second transmembrane (M1-M2) segments1.
Biological Activity	Tertiapin-LQ is a selective blocker of Kir1.1 channels.
Formulation	Lyophilized from double distilled water (ddH2O). May contain TFA as a residual counter ion.
Molecular Weight	2428 Da
Solubility	Centrifuge the vial before adding solvent (10,000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. The product is soluble in pure water at high micromolar concentrations (100 uM - 1 mM). For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in double-distilled water (ddH2O) at a concentration between 100-1000x of the final working concentration. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. Centrifuge all product preparations before use. It is recommended to prepare fresh solutions in working buffers just before use. Avoid multiple freeze-thaw cycles to maintain biological activity.
Source	Synthetic peptide
Concentration	100 nM
Form	Lyophilized
Notes	Bioassay Tested: yes Steril endotoxin free: no Is Toxin: Yes
UNSPSC Code	12352202
Lead Time	1-2 Business Days
Modifications	Disulfide bonds between: Cys3-Cys14 and Cys5-Cys18 Lys21 -C-terminal amidation
Origin	Apis mellifera (Honeybee)

Synonyms	Tertiapin LQ
Gene Id	KCNJ1,KCNJ3,KCNJ5
Sequence	ALCNCNRIIIPLQCWKKCGKK-NH2
Target	Kir1.1, Kir3.1, Kir3.4 K+ channels

Country Of Origin	Israel/IL
Purity	>=98% (HPLC)
Storage	Storage After Reconstitution: The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles. Storage Before Reconstitution: The product is shipped as a lyophilized powder at room temperature. Upon receipt, store the product at -20°C. Protect from moisture. Storage of solutions: The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles.

Applications	Electrophysiology

Reference	Ramu, Y. et al. (2008) Proc Natl Acad Sci U.S.A. 105, 10774. Xu, X. et al. (1993) Proteins 17, 124. Jin, W. and Lu, Z. (1998) Biochemistry 37, 13291. Kitamura, H. et al. (2000) J. Pharmacol. Exp. Therap. 293, 196.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHP21300296-1	STT-220_0.5 mg	0.5 mg	$129		Add to Cart
BHP21300296-2	STT-220_1 mg	1 mg	$167		Add to Cart
BHP21300296-3	STT-220_10 mg	10 mg	$638		Add to Cart
BHP21300296-4	STT-220_5 mg	5 mg	$459		Add to Cart

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