Tertiapin-Q | Alomone Labs STT-170 product information

product summary

company name :

Alomone Labs

product type :

chemical

product name :

Tertiapin-Q

catalog :

STT-170

more info or order :

Alomone Labs product webpage

citations: 22

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
Bidaud I, Chong A, Carcouët A, Waard S, Charpentier F, Ronjat M, et al. Inhibition of G protein-gated K+ channels by tertiapin-Q rescues sinus node dysfunction and atrioventricular conduction in mouse models of primary bradycardia. Sci Rep. 2020;10:9835 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
Fox P, Hentges S. Differential Desensitization Observed at Multiple Effectors of Somatic μ-Opioid Receptors Underlies Sustained Agonist-Mediated Inhibition of Proopiomelanocortin Neuron Activity. J Neurosci. 2017;37:8667-8677 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
Hablitz L, Molzof H, Abrahamsson K, Cooper J, Prosser R, Gamble K. GIRK Channels Mediate the Nonphotic Effects of Exogenous Melatonin. J Neurosci. 2015;35:14957-65 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
Kotecki L, Hearing M, McCall N, Marron Fernandez de Velasco E, Pravetoni M, Arora D, et al. GIRK Channels Modulate Opioid-Induced Motor Activity in a Cell Type- and Subunit-Dependent Manner. J Neurosci. 2015;35:7131-42 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
Farhy Tselnicker I, Tsemakhovich V, Rishal I, Kahanovitch U, Dessauer C, Dascal N. Dual regulation of G proteins and the G-protein-activated K+ channels by lithium. Proc Natl Acad Sci U S A. 2014;111:5018-23 pubmed publisher
Nakamura A, Fujita M, Ono H, Hongo Y, Kanbara T, Ogawa K, et al. G protein-gated inwardly rectifying potassium (KIR3) channels play a primary role in the antinociceptive effect of oxycodone, but not morphine, at supraspinal sites. Br J Pharmacol. 2014;171:253-64 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
Kailey B, van de Bunt M, Cheley S, Johnson P, MacDonald P, Gloyn A, et al. SSTR2 is the functionally dominant somatostatin receptor in human pancreatic ?- and ?-cells. Am J Physiol Endocrinol Metab. 2012;303:E1107-16 pubmed publisher
Jo H, Kim S, Lee S, Jeong S, Kim S, Kang T, et al. Kir3.1 channel is functionally involved in TLR4-mediated signaling. Biochem Biophys Res Commun. 2011;407:687-91 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
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
Young C, Stegen M, Bernard R, Muller M, Bischofberger J, Veh R, et al. Upregulation of inward rectifier K+ (Kir2) channels in dentate gyrus granule cells in temporal lobe epilepsy. J Physiol. 2009;587:4213-33 pubmed publisher

image

image 1 :

Alomone Labs Tertiapin-Q inhibits Kir3.2 channel heterologously expressed inXenopusoocytes. - A continuous current trace recorded at a holding potential of -80 mV. Kir3.2 currents are downward reflections activated by high K+containing solution. While activated increasing concentrations ofTertiapin-Q(#STT-170) were applied (arrows at the bottom of the trace).

image 2 :

Li+modulates GIRK activity in hippocampal neurons. - Incubation of neurons with 1 mM Li+ increased Ibasalin low-K+solution. Ibasalwas measured at ?120 mV (voltage step from the holding potential of ?60 mV) to enhance the sensitivity of measurement. Representative traces recorded in the low-K+solution before (black) and after (pink) application ofTertiapin-Q(#STT-170).Adapted fromFarhy Tselnicker I.et al.(2014) with permission ofProceedings of the National Academy of Sciences.

product information

cat :

STT-170

SKU :

STT-170_0.1 mg

Product Name :

Tertiapin-Q

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, KCNMA1

Product Page - Scientific background :

Tertiapin, the native toxin, was originally isolated from European honey bee Apis mellifera venoM Native and synthetic Tertiapin blocks 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 was 8.6 nM) but with no effect on the Kir2 family member1. In accordance, it was shown to inhibit acetylcholine induced K+ currents in mammalian cardiomyocytes2,3.Tertiapin-Q is a derivative of Tertiapin in which Met13 is substituted by a Gln residue. However, unlike native Tertiapin, Tertiapin-Q is non-oxidizable and therefore is more stable4.Tertiapin-Q inhibits the above-mentioned channels with similar affinities and also inhibits Ca2-activated large conductance BK-type K+ channels in a concentration and voltage-dependent manner5.

Supplier :

Alomone Labs

Target :

Kir1.1, Kir3.2 K+ channels

Long Description :

A Potent Blocker of Inward Rectifier (Kir) K+ Channels

Short Description :

A Potent Blocker of Inward Rectifier (Kir) K+ Channels

MW :

2452 Da

Synonyms :

TPN-Q

Modifications :

Disulfide bonds between: Cys3-Cys14, Cys5-Cys18 Lys21 - C-terminal amidation ATTO Fluor-488

Molecular formula :

C106H175N35O24S4

Effective Concentration :

2 - 200 nM

Activity :

Tertiapin-Q 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 heart2,3. Tertiapin-Q is a derivative of Tertiapin in which Met13 is replaced by Gln. Tertiapin-Q inhibits the above-mentioned channels with similar affinities4.

Storage of solutions :

Lead Time :

1-2 Business Days

Country of origin :

Israel/IL

Purity :

≥98% (HPLC)

CAS No :

910044-56-3

Form :

Lyophilized

Comment :

Contact Alomone Labs for technical support and product customization

Sequence :

ALCNCNRIIIPHQCWKKCGKK-NH2

Is Toxin :

Yes

UNSPSC :

12352202

Bioassay Tested :

yes

Steril endotoxin free :

Cited Application :

Electrophysiology

more info or order :

Alomone Labs product webpage