Apamin (Synonyms: Ro 23-6721) |
رقم الكتالوجGC14893
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Apamin (Apamine) عبارة عن سم عصبي ببتيد مكون من 18 حمض أميني موجود في الأبيتوكسين (سم النحل) ، ويُعرف بأنه مانع انتقائي لقنوات Ca2 +- نشاط ليفي
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Cas No.: 24345-16-2
Sample solution is provided at 25 µL, 10mM.
Apamin is a polypeptide neurotoxin derived from bee (Apis mellifera) venom [1-2]. Apamin is a highly selective small-conductance calcium-activated potassium channel (SK channel, especially the SK2 subtype; IC₅₀=0.06–0.4nM) blocker. Apamin enhances neuronal excitability and synaptic plasticity by preventing the hyperpolarization phase following neuronal action potentials, thereby influencing physiological functions such as learning and memory[3-4].
In vitro, Apamin (0.1μM) treatment of differentiated N1E 115 neuroblastoma cells for 2 minutes selectively blocks Ca²⁺-dependent K⁺ channels, increasing neuronal excitability[5]. In SH-SY5Y human neuroblastoma cells pretreated with Apamin (0.5μg/mL) for 1 hour, followed by stimulation with 1-methyl-4-phenyl pyridinium (MPP⁺; 3mM) for 12–24 hours, Apamin significantly inhibits the downregulation of tyrosine hydroxylase (TH) expression and abnormal aggregation of α-synuclein (αSYN), while reducing mitochondrial membrane potential disruption and apoptosis by blocking SK2 channel-mediated calcium overload[6].
In vivo, in a cholestatic liver fibrosis model induced by 3,5-Diethoxycarbonyl-1,4-Dihydrocollidine (DDC) diet, intraperitoneal injection of Apamin (0.1mg/kg) twice weekly for 4 weeks in 8-week-old C57BL/6 male mice significantly alleviates DDC-induced liver tissue damage and collagen deposition[7]. In a lipopolysaccharide (LPS; 10mg/kg)-induced acute kidney injury model, a single intraperitoneal injection of Apamin (0.1mg/kg) in 8-week-old C57BL/6N male mice significantly improves LPS-induced renal dysfunction and kidney tissue damage[8].
References:
[1] Gu H, Han SM, Park KK. Therapeutic Effects of Apamin as a Bee Venom Component for Non-Neoplastic Disease. Toxins (Basel). 2020 Mar 19;12(3):195.
[2] Laurindo LF, de Lima EP, Laurindo LF, et al. The therapeutic potential of bee venom-derived Apamin and Melittin conjugates in cancer treatment: A systematic review. Pharmacol Res. 2024 Nov;209:107430.
[3] Strong PN, Stocker M, Jenkinson DH. Apamin binding proteins and oligosaccharyltransferases. Toxicon. 1996 May;34(5):507-9.
[4] Lazdunski M, Fosset M, Hughes M, et al. The apamin-sensitive Ca2+-dependent K+ channel molecular properties, differentiation and endogenous ligands in mammalian brain. Biochem Soc Symp. 1985;50:31-42.
[5] Hugues M, Romey G, Duval D, et al. Apamin as a selective blocker of the calcium-dependent potassium channel in neuroblastoma cells: voltage-clamp and biochemical characterization of the toxin receptor. Proc Natl Acad Sci U S A. 1982 Feb;79(4):1308-12.
[6] Park J, Jang KM, Park KK. Effects of Apamin on MPP+-Induced Calcium Overload and Neurotoxicity by Targeting CaMKII/ERK/p65/STAT3 Signaling Pathways in Dopaminergic Neuronal Cells. Int J Mol Sci. 2022 Dec 3;23(23):15255.
[7] Kim JY, An HJ, Kim WH, et al. Apamin suppresses biliary fibrosis and activation of hepatic stellate cells. Int J Mol Med. 2017 May;39(5):1188-1194.
[8] Kim JY, Leem J, Park KK. Antioxidative, Antiapoptotic, and Anti-Inflammatory Effects of Apamin in a Murine Model of Lipopolysaccharide-Induced Acute Kidney Injury. Molecules. 2020 Dec 3;25(23):5717.
| Cell experiment [1]: | |
Cell lines | SH-SY5Y cells (human dopaminergic neuroblastoma cell line) |
Preparation Method | SH-SY5Y cells were cultured in Dulbecco’s Modified Eagle’s Medium (DMEM) supplemented with 10% fetal bovine serum (FBS). Cells were treated with Apamin (0.5μg/mL) for 1 hour, followed by exposure to MPP⁺ (3mM) for 12–24 hours. |
Reaction Conditions | 0.5μg/mL; 1h pretreatment |
Applications | Apamin significantly attenuated MPP⁺-induced cytotoxicity by restoring mitochondrial membrane potential and reducing apoptotic markers. Apamin suppressed calcium overload and downregulated SK2 channel (KCa2.2) expression, inhibiting CaMKII phosphorylation. Apamin also mitigated oxidative stress and endoplasmic reticulum stress, while blocking pro-inflammatory cytokine production via ERK/NF-κB/STAT3 pathway inhibition. |
| Animal experiment [2]: | |
Animal models | C57BL/6N male mice |
Preparation Method | Mice were intraperitoneally injected with a single dose of lipopolysaccharide (LPS; 10mg/kg). Apamin (0.1mg/kg) was administered intraperitoneally 1 hour after LPS injection. Mice were sacrificed 24 hours post-LPS injection for renal and plasma analysis. |
Dosage form | 0.1mg/kg; i.p.; Single injection 1 hour post-LPS. |
Applications | Apamin significantly ameliorated LPS-induced acute kidney injury, reducing plasma creatinine and blood urea nitrogen (BUN) levels. Apamin attenuated renal tubular injury, including brush border loss and suppressed expression of injury markers. Apamin inhibited oxidative stress by downregulating NOX4 and enhancing HO-1 expression, reduced lipid peroxidation (4-HNE, MDA), and restored GSH/GSSG ratio. Apamin suppressed apoptosis and inhibited inflammation by reducing TNF-α and IL-6 levels, downregulating TLR4/NF-κB signaling, and attenuating immune cell infiltration and vascular adhesion molecule. |
References: | |
| Cas No. | 24345-16-2 | SDF | |
| المرادفات | Ro 23-6721 | ||
| Formula | C79H131N31O24S4 | M.Wt | 2027.34 |
| الذوبان | Water: 1 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 493.3 μL | 2.4663 mL | 4.9326 mL |
| 5 mM | 98.7 μL | 493.3 μL | 986.5 μL |
| 10 mM | 49.3 μL | 246.6 μL | 493.3 μL |
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 17 reference(s) in Google Scholar.)