아파민

한글명:아파민

카스 번호24345-16-2

상품명:APAMIN

CBNumberCB4342708

분자식C79H131N31O24S4

포뮬러 무게2027.34

MOL 파일24345-16-2.mol

동의어(한글)

아파민

화학적 성질

끓는 점	847.17°C (rough estimate)
밀도	1.63
굴절률	1.5530 (estimate)
저장 조건	-20°C
용해도	0.05 M 아세트산: 5 mg/mL, 투명, 무색 ~ 희미한 노란색
물리적 상태	어두운 황갈색을 띤 흰색 고체
색상	White to off-white
수용성	Soluble to 1 mg/ml in water
Merck	13,732

위험 및 안전 성명

안전지침서	22-24/25
유엔번호(UN No.)	2811
WGK 독일	3
RTECS 번호	CD6899900
F 고인화성물질	3-10
위험 등급	6.1(b)
포장분류	III
독성	LD50 i.v. in mice: 4 mg/kg (Habermann, Reiz); LD50 intracerebroventricularly in mice: 12 ng/animal (Labbé-Jullié)

그림문자(GHS)

아파민 화학적 특성, 용도, 생산

화학적 성질
Small, highly potent, highly basic polypeptide.
용도
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.
정의
Occurs in the venom of the honey bee, Apis mellifera; molecular weight of 2027.38.
일반 설명
Apamin is a bee venom component and is strongly basic in nature. It has 18 amino acid residues and two disulphide bonds.
위험도
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.
효소 저해제
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.

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