Apamin CAS: 24345-16-2
MF: C79H131N31O24S4
MW: 2027.34
A potent and highly selective inhibitor of the low conductance Ca2+-activated K+ channel.

Apamin (CAS 24345-16-2)

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Application: Apamin is a potent and highly selective inhibitor of the low conductance Ca2+-activated K+ channel
CAS Number: 24345-16-2
Purity: ≥95%
Molecular Weight: 2027.34
Molecular Formula: C79H131N31O24S4
仅供科研使用。不可用于诊断或治疗。
* 参考分析证明 大量特定数据 (包括水 含量).
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Apamin: Caution! Highly toxic. Handle with care. The smallest neurotoxin known. It is the only polypeptide neurotoxin that is known to pass the blood-brain barrier. Comprises about 2% by weight of the dried venom of the honey bee. It is a potent (1-10 nM) and highly selective inhibitor of the SK (low conductance Ca2+-activated K+ channel). Acts on the central nervous system. SK channel blockers such as apamin can have therapeutic applications, for example on the peripheral cells (e.g. the insulin releasing cells of the pancreas) and on the central nervous system where there is evidence for a role of SK channels in memory processes, both general and specifically hippocampal.


参考文献

1: N.A. Castle et al. Trends Neurosci. 1989 12 59 2: M. Hughes et al. Proc. Natl. Acad. Sci. USA 1982 79 1308 3: P.N. Strong Pharmacol. Therap. 1990 46 137

Appearance :
Powder
Physical State :
Solid
Sequence :
Cys-Asn-Cys-Lys-Ala-Pro-Glu-Thr-Ala-Leu-Cys-Ala-Arg-Arg-Cys-Gln-Gln-His-NH2
Solubility :
Soluble in acetic acid (5mg/ml) and slightly soluble in water (1mg/ml)
Storage :
Store at -20° C
Refractive Index :
n20D 1.72 (Predicted)
IC50 :
apamin-sensitive SKCa channel: IC50 = 0.001 µM (guinea-pig hepatocytes); calcium activated potassium channel: IC50 = 8.6e-06 µM
Ki Data :
[125I]apamin binding to calcium-activated potassium (SK) channel: Ki= 3.8 µM (rat cortex)
仅供科研使用。不可用于诊断或治疗。
WGK Germany :
3
RTECS :
CD6899900
PubChem CID :
16218850
Merck Index :
14: 725
MDL Number :
MFCD00167944
EC Number :
246-182-7
SMILES :
C[[email protected]]1C(=O)N[[email protected]](C(=O)N[[email protected]](C(=O)N[[email protected]@H](CSSC[[email protected]]2C(=O)N[[email protected]](C(=O)N[[email protected]](C(=O)N3CCC[[email protected]]3C(=O)N[[email protected]](C(=O)N[[email protected]](C(=O)N[[email protected]](C(=O)N[[email protected]](C(=O)N[[email protected]@H](CSSC[[email protected]@H](C(=O)N[[email protected]](C(=O)N2)CC(=O)N)N)C(=O)N1)CC(C)C)C)[[email protected]@H](C)O)CCC(=O)O)C)CCCCN)C(=O)N[[email protected]@H](CCC(=O)N)C(=O)N[[email protected]@H](CCC(=O)N)C(=O)N[[email protected]@H](CC4=CN=CN4)C(=O)N)CCCNC(=N)N)CCCNC(=N)N

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Citations 1 to 3 of 3 total

PMID: # 28036359  Estep, CM. et al. 2016. PLoS ONE. 11: e0169044.

PMID: # 25641660  Sung, TS. et al. 2015. J. Physiol. (Lond.). 593: 1169-81.

PMID: # 32086857  FASEB J.

Citations 1 to 3 of 3 total
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