Tertiapin | Alomone Labs STT-250 product information

product summary

company name :

Alomone Labs

product type :

chemical

product name :

Tertiapin

catalog :

STT-250

more info or order :

Alomone Labs product webpage

citations: 18

Reference
Singh B, Khattab F, Chae H, Desmet L, Herrera P, Gilon P. KATP channel blockers control glucagon secretion by distinct mechanisms: A direct stimulation of α-cells involving a [Ca2+]c rise and an indirect inhibition mediated by somatostatin. Mol Metab. 2021;53:101268 pubmed publisher
Binas S, Knyrim M, Hupfeld J, Kloeckner U, Rabe S, Mildenberger S, et al. miR-221 and -222 target CACNA1C and KCNJ5 leading to altered cardiac ion channel expression and current density. Cell Mol Life Sci. 2020;77:903-918 pubmed publisher
Mann A, Mouledous L, Froment C, O Neill P, Dasgupta P, Gunther T, et al. Agonist-selective NOP receptor phosphorylation correlates in vitro and in vivo and reveals differential post-activation signaling by chemically diverse agonists. Sci Signal. 2019;12: pubmed publisher
Liu Y, LoCaste C, Liu W, Poltash M, Russell D, Laganowsky A. Selective binding of a toxin and phosphatidylinositides to a mammalian potassium channel. Nat Commun. 2019;10:1352 pubmed publisher
Stötzner P, Spahn V, Celik M, Labuz D, Machelska H. Mu-Opioid Receptor Agonist Induces Kir3 Currents in Mouse Peripheral Sensory Neurons - Effects of Nerve Injury. Front Pharmacol. 2018;9:1478 pubmed publisher
Philippart F, Khaliq Z. Gi/o protein-coupled receptors in dopamine neurons inhibit the sodium leak channel NALCN. elife. 2018;7: pubmed publisher
Zhao Y, Wu X, Li X, Jiang L, Gui X, Liu Y, et al. TREM2 Is a Receptor for β-Amyloid that Mediates Microglial Function. Neuron. 2018;97:1023-1031.e7 pubmed publisher
Li W, Zhu X, Ritson E. Mechanosensory Stimulation Evokes Acute Concussion-Like Behavior by Activating GIRKs Coupled to Muscarinic Receptors in a Simple Vertebrate. Eneuro. 2017;4: pubmed publisher
Li Y, Hu H, Butterworth M, Tian J, Zhu M, O Neil R. Expression of a Diverse Array of Ca2+-Activated K+ Channels (SK1/3, IK1, BK) that Functionally Couple to the Mechanosensitive TRPV4 Channel in the Collecting Duct System of Kidney. PLoS ONE. 2016;11:e0155006 pubmed publisher
Yakubovich D, Berlin S, Kahanovitch U, Rubinstein M, Farhy Tselnicker I, Styr B, et al. A Quantitative Model of the GIRK1/2 Channel Reveals That Its Basal and Evoked Activities Are Controlled by Unequal Stoichiometry of Gα and Gβγ. PLoS Comput Biol. 2015;11:e1004598 pubmed publisher
Takasu K, Ogawa K, Nakamura A, Kanbara T, Ono H, Tomii T, et al. Enhanced GABAergic synaptic transmission at VLPAG neurons and potent modulation by oxycodone in a bone cancer pain model. Br J Pharmacol. 2015;172:2148-64 pubmed publisher
Nockemann D, Rouault M, Labuz D, Hublitz P, McKnelly K, Reis F, et al. The K(+) channel GIRK2 is both necessary and sufficient for peripheral opioid-mediated analgesia. EMBO Mol Med. 2013;5:1263-77 pubmed publisher
Borgquist A, Kachani M, Tavitian N, Sinchak K, Wagner E. Estradiol negatively modulates the pleiotropic actions of orphanin FQ/nociceptin at proopiomelanocortin synapses. Neuroendocrinology. 2013;98:60-72 pubmed publisher
Arora D, Haluk D, Kourrich S, Pravetoni M, Fernandez Alacid L, Nicolau J, et al. Altered neurotransmission in the mesolimbic reward system of Girk mice. J Neurochem. 2010;114:1487-97 pubmed publisher
Farhang B, Pietruszewski L, Lutfy K, Wagner E. The role of the NOP receptor in regulating food intake, meal pattern, and the excitability of proopiomelanocortin neurons. Neuropharmacology. 2010;59:190-200 pubmed publisher
Clark B, Kurth Nelson Z, Newman E. Adenosine-evoked hyperpolarization of retinal ganglion cells is mediated by G-protein-coupled inwardly rectifying K+ and small conductance Ca2+-activated K+ channel activation. J Neurosci. 2009;29:11237-45 pubmed publisher
Russo M, Yau H, Nunzi M, Mugnaini E, Martina M. Dynamic metabotropic control of intrinsic firing in cerebellar unipolar brush cells. J Neurophysiol. 2008;100:3351-60 pubmed publisher
Witkowski G, Szulczyk B, Rola R, Szulczyk P. D(1) dopaminergic control of G protein-dependent inward rectifier K(+) (GIRK)-like channel current in pyramidal neurons of the medial prefrontal cortex. Neuroscience. 2008;155:53-63 pubmed publisher

image

image 1 :

Western blot analysis of rat (lanes 1 and 3) and mouse (lanes 2 and 4)brainlysates: - 12.Anti-CACNG7(extracellular) Antibody(#ACC-109) (1:1000).34. Anti-CACNG7(extracellular) Antibodypreincubated with the negative control antigen.

image 2 :

Alomone Labs Tertiapin inhibits Kir3.2 channels expressed in Xenopus oocytes. - A continuous current trace recorded at a holding potential of -80 mV. Channel activation was achieved by high K+solution perfusion. 50 nMTertiapin(#STT-250) was applied during the period (2 minutes each) marked as a green trace.

product information

cat :

STT-250

SKU :

STT-250_0.1 mg

Product Name :

Tertiapin

Group Type :

Non Antibodies

Product Type :

Proteins

Accession :

P56587

Accession Number :

https://www.uniprot.org/uniprotkb/P56587/entry

Applications :

Electrophysiology

Formulation :

Lyophilized from double distilled water (ddH2O). May contain TFA as a residual counter ion.

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.

Reconstitution and Solubility :

Centrifuge the vial (10,000 × 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 µM - 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.

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 µM - 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.

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.

Origin :

Apis mellifera (Honeybee)

Source :

Synthetic peptide

Gene ID :

KCNJ1,KCNJ3,KCNJ5,KCNJ6

Product Page - Scientific background :

Tertiapin is a 21 amino acid long toxin, originally isolated from Apis mellifera bee venoM Native and synthetic Tertiapin block a range of inward rectifier K+ channels. (Kir), in particular ROMK1 (Kir1.1, IC50 = 2 nM) and GIRK (Kir3 family, IC50 for the Kir3.1/3.4 heteromer is 8.6 nM) but with no effect on Kir2 family members1. In addition, it was shown to inhibit acetylcholine-induced K+ currents in the heart2,3.Tertiapin is as active as Tertiapin-Q (#STT-170), a derivative of Tertiapin in which the oxidation-liable methionine is replaced by a glutamine residue4.

Supplier :

Alomone Labs

Target :

Kir1.1, Kir3.2 K+ channels

Long Description :

A Blocker of Inward Rectifier (Kir) K+ Channels

Short Description :

A Blocker of Inward Rectifier (Kir) K+ Channels

MW :

2455 Da

Synonyms :

TPN

Modifications :

Disulfide bonds between: Cys3-Cys14, and Cys5-Cys18 Lys21 -C-terminal amidation

Molecular formula :

C106H176N34O23S5

Effective Concentration :

10 - 100 nM

Activity :

Tertiapin blocks a range of inward rectifier K+ channels (Kir) in particular ROMK1 and GIRK but with no effect on Kir2 family members1. In addition, it was shown to inhibit acetylcholine induced K+ currents in the heart2,3.

Storage of solutions :

Lead Time :

1-2 Business Days

Country of origin :

Israel/IL

Purity :

≥98% (HPLC)

CAS No :

58694-52-3

Form :

Lyophilized

Comment :

Contact Alomone Labs for technical support and product customization

Sequence :

ALCNCNRIIIPHMCWKKCGKK-NH2

Is Toxin :

Yes

UNSPSC :

12352202

Bioassay Tested :

yes

Steril endotoxin free :

more info or order :

Alomone Labs product webpage