???
|
|
??? ??
- ?? ?
- 847.17°C (rough estimate)
- ??
- 1.63
- ???
- 1.5530 (estimate)
- ?? ??
- -20°C
- ???
- 0.05 M ????: 5 mg/mL, ??, ?? ~ ??? ???
- ??? ??
- ??? ???? ? ?? ??
- ??
- White to off-white
- ???? ??
- synthetic
- ???
- Soluble to 1 mg/ml in water
- Merck
- 13,732
- ???
- Cys-Asn-Cys-Lys-Ala-Pro-Glu-Thr-Ala-Leu-Cys-Ala-Arg-Arg-Cys-Gln-Gln-His-NH2 (Disulfide bridge: Cys1-Cys11;Cys3-Cys15)
- InChIKey
- YVIIHEKJCKCXOB-STYWVVQQSA-N
??
- ?? ? ?? ??
- ?? ? ???? ?? (GHS)
| ????? | 22-24/25 | ||
|---|---|---|---|
| ????(UN No.) | 2811 | ||
| WGK ?? | 3 | ||
| RTECS ?? | CD6899900 | ||
| F ?????? | 3-10 | ||
| ?? ?? | 6.1(b) | ||
| ???? | III | ||
| ???? ??? | 11 - Combustible Solids | ||
| ?? | LD50 i.v. in mice: 4 mg/kg (Habermann, Reiz); LD50 intracerebroventricularly in mice: 12 ng/animal (Labbé-Jullié) |
| ????(GHS): |
|
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|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| ?? ?: | Danger | ||||||||||||||
| ??·?? ??: |
|
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| ??????: |
|
??? C??? ??, ??, ??
??? ??
Small, highly potent, highly basic polypeptide.??
Apamin has been used:- As a selective inhibitor of small conductance (SKCa) channels in HEK cells.
- To inhibit endothelium-derived relaxing factor (EDHF) mediated responses.
- To block small-conductance Ca2-activated K current (ISK) in electrophysiological studies in hyperstriatum ventrale, pars caudalis (HVc) neurons.
??
Occurs in the venom of the honey bee, Apis mellifera; molecular weight of 2027.38.?? ??
Apamin is a bee venom component and is strongly basic in nature. It has 18 amino acid residues and two disulphide bonds.???
Central nervous system poison able to cross the blood–brain barrier; neurotoxic; poison.Safety Profile
Poison by intravenous, parenteral,intracerebral, and intraperitoneal routes. When heated todecomposition it emits toxic fumes of SOx and NOx.?? ???
This bee venom octadecapeptide toxin (FW = 2027.34 g/mol; CAS 24345- 16-2; NCBI Reference Sequence: NP_001011612.1) potently blocks the small-conductance Ca 2+ -activated potassium ion (or SK) channels hSK1 as well as rSK2, with IC50 values of 3.3 nM and 83 pM. It shows greater effectiveness at the SK2 channel (IC50 = 0.06-0.4 nM) than SK1 (IC50 = 1- 12 nM). SK3 (IC50 = 1-13 nM), and SK4 (IC50 = 1 μM) channels, and is active against channels within neurons, vascular endothelium, bladder smooth muscle, and certain cancers. Apamin does not inhibit human cardiac Na + current, L-type Ca 2+ current or other major K+ currents. Structurally, apamin forms a stable structure, consisting of a C-terminal a- helix and two reverse turns, that is stabilized by two disulfide bonds connecting Cys-1 to Cys-11 and Cys-3 to Cys-15. A minor constituent of venom of the bee (Apis mellifera), apamin amounts to only 2-3% (w/w) of its dry venom. The smallest known neurotoxic polypeptide, apamin is derived by proteolytic processing of the 48-residue pre-pro-protein. The precursors of the bee venom constituents apamin and MCD peptide are encoded by two genes in tandem which share the same 3'-exon.??? ?? ?? ? ???
???
?? ??
??? ?? ??
???( 180)?? ??
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??? ?? ??:
Glibenclamide
Nicorandil
CHARYBDOTOXIN
TRAM-34
5-HYDROXYDECANOIC ACID SODIUM SALT
CLOFILIUM TOSYLATE
Gabapentin-lactam
PAXILLINE
N-(4-PHENYLSULFONYLPHENYL)-3,3,3-TRIFLUORO-2-HYDROXY-2-METHYLPROPANAMIDE
APAMIN
Honey
apamin receptor
APAMIN, ALEXA FLUOR(R) 488 CONJUGATE
APAMIN, BODIPY(R) FL CONJUGATE
APAMIN (DRY ICE)
Kca2.2, SK2, Kcnn2, SKCa2 (Apamin-Sensitive Small Conductance Ca2+ -dependent K+ Channel), Rabbit anti-Rat, WB/IH
ANTI-POTASSIUM CHANNEL SK2 (APAMIN-SENSITIVE CONDUCTANCE CA2+-DEPENDENT K+ CHANNEL, KCA2, KCNN2, SKCA2)
APAMIN, [125I]-HIS18-NH2