Apamin

Pricing Availability Delivery Time Qty
Cat.No. 1652 - Apamin | Cys-Asn-Cys-Lys-Ala-Pro-Glu-Thr-Ala-Leu-Cys-Ala-Arg-Arg-Cys-Gln-Gln-His-NH2 (Disulfide bridges: 1 - 11, 3 - 15) | CAS No. 24345-16-2
Description: KCa2 channel blocker (small conductance)
Datasheet
Citations (18)
Literature

Biological Activity

Prototypical potent and highly selective inhibitor of the small-conductance Ca2+-activated K+-channel (KCa2, SK). Blocks medium after-hyperpolarization in vitro and is brain penetrant and convulsive in vivo.

Technical Data

M. Wt 2027.34
Formula C79H131N31O24S4
Sequence CNCKAPETALCARRCQQH

(Modifications: Disulfide bridge between 1 - 11, 3 - 15, His-18 = C-terminal amide)

Storage Desiccate at -20°C
CAS Number 24345-16-2
PubChem ID 16133797
InChI Key YVIIHEKJCKCXOB-STYWVVQQSA-N
Smiles [H]N[C@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@@H]3CCCN3C(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](C)NC2=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC2=CNC=N2)C(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O)[C@@H](C)O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

SolubilitySoluble to 1 mg/ml in water

Preparing Stock Solutions

The following data is based on the product molecular weight 2027.34. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 0.49 mL 2.47 mL 4.93 mL
5 mM 0.1 mL 0.49 mL 0.99 mL
10 mM 0.05 mL 0.25 mL 0.49 mL
50 mM 0.01 mL 0.05 mL 0.1 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Habermann (1984) Apamin. Pharmacol.Ther. 25 255 PMID: 6095335

Stocker et al (2004) Matching molecules to function: neuronal Ca2+-activated K+ channels and afterhyperpolarizations. Toxicon 43 933 PMID: 15208027

Strong (1990) Potassium channel toxins. Pharmacol.Ther. 46 137 PMID: 2181489

van der Staay et al (1999) Behavioral effects of apamin, a selective inhibitor of the SKCa-channel, in mice and rats. Neurosci.Biobehav.Rev. 23 1087 PMID: 10643819


If you know of a relevant reference for Apamin, please let us know.

View Related Products by Product Action

View all Calcium-Activated Potassium (KCa) Channel Blockers

Keywords: K+ channels blockers small conductance ca2+-activated ca2+-dependent Potassium KCa KCa2 SK venoms Ca2+-Activated Potassium Channels

18 Citations for Apamin

Citations are publications that use Tocris products. Selected citations for Apamin include:

Sargin et al (2016) Chronic social isolation reduces 5-HT neuronal activity via upregulated SK3 calcium-activated potassium channels Elife 5 e21416 PMID: 27874831

Zachary and Fuchs (2015) Re-Emergent Inhibition of Cochlear Inner Hair Cells in a Mouse Model of Hearing Loss. J Neurosci 35 9701 PMID: 26134652

Lee et al (2015) The role of K+ conductances in regulating membrane excitability in human gastric corpus smooth muscle. FASEB J 308 G625 PMID: 25591864

Rau et al (2015) Increased Basolateral Amygdala Pyramidal Cell Excitability May Contribute to the Anxiogenic Phenotype Induced by Chronic Early-Life Stress. Heart Rhythm 35 9730 PMID: 26134655

Henry et al (2015) Cell type-specific transcriptomics of hypothalamic energy-sensing neuron responses to weight-loss. Mol Pain 4 PMID: 26329458

Thompson et al (2015) Small-conductance calcium-activated potassium (SK) channels in the amygdala mediate pain-inhibiting effects of clinically available riluzole in a rat model of arthritis pain. J Neurosci 11 51 PMID: 26311432

Yu et al (2014) Apamin does not inhibit human cardiac Na+ current, L-type Ca2+ current or other major K+ currents. J Neurosci 9 e96691 PMID: 24798465

Turker et al (2013) Amiodarone inhibits apamin-sensitive potassium currents. PLoS One 8 e70450 PMID: 23922993

Alpert and Alford (2013) Synaptic NMDA receptor-dependent Ca2+ entry drives membrane potential and Ca2+ oscillations in spinal ventral horn neurons. PLoS One 8 e63154 PMID: 23646190

Hsueh et al (2013) Proarrhythmic effect of blocking the small conductance calcium activated potassium channel in isolated canine left atrium. Elife 10 891 PMID: 23376397

Few et al (2012) Asynchronous Ca2+ current conducted by voltage-gated Ca2+ (CaV)-2.1 and CaV2.2 channels and its implications for asynchronous neurotransmitter release. Proc Natl Acad Sci U S A 109 E452 PMID: 22308469

Zemkova et al (2011) Norepinephrine causes a biphasic change in mammalian pinealocye membrane potential: role of alpha1B-adrenoreceptors, phospholipase C, and Ca2+. Endocrinology 152 3842 PMID: 21828176

Geier et al (2011) Dynamic interplay of excitatory and inhibitory coupling modes of neuronal L-type calcium channels. Am J Physiol Cell Physiol 300 C937 PMID: 21228322

Meredith et al (2011) Postnatal expression of an apamin-sensitive k(ca) current in vestibular calyx terminals. J Membr Biol 244 81 PMID: 22057903

Chan and Cipolla (2011) Relaxin causes selective outward remodeling of brain parenchymal arterioles via activation of peroxisome proliferator-activated receptor-γ. Sci Rep 25 3229 PMID: 21602449

Lamy et al (2010) Allosteric block of KCa2 channels by apamin. J Neurosci 285 27067 PMID: 20562108

Villalobos and Andrade (2010) Visinin-like neuronal calcium sensor proteins regulate the slow calcium-activated afterhyperpolarizing current in the rat cerebral cortex. Am J Physiol Gastrointest Liver Physiol 30 14361 PMID: 20980592

Han et al (2007) Dopaminergic modulation of spinal neuronal excitability. J Biol Chem 27 13192 PMID: 18045913


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