标签归档：osk

OSK-1

发表于由

OSK-1;

OSK-1 是有效的 Kv 通道阻断剂，对 Kv1.1、Kv1.2、Kv1.3 的 IC50 分别为 0.6 nM、5.4 nM、0.014 nM。OSK1 是 Ca2+ 激活的 KCa3.1 通道的中度阻滞剂，IC50 为 225 nM。OSK-1 属于 α-KTx3 毒素，有潜力用作免疫抑制药物。

OSK-1amp;;

OSK-1 Chemical Structure

CAS No. : 183815-75-0

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生物活性

OSK-1 is a potent Kv channel blocker with IC50s of of 0.6 nM, 5.4 nM, 0.014 nM for Kv1.1, Kv1.2 and Kv1.3, respectively. OSK1 is a moderate blocker of Ca2+-activated KCa3.1 channel with an IC50 of 225 nM. OSK-1 belongs to α-KTx3 toxins and is used as a immunosuppressive drug[1].

IC50 Target

IC50: 0.6 nM (Kv1.1), 5.4 nM (Kv1.2), 0.014 nM (Kv1.3) and 225 nM (KCa3.1)[1]
体外研究
(In Vitro)

OSK1 has no effect on KCa2.1, KCa2.2, KCa2.3 and KCa1.1 channels when in the micromolar concentration range, whereas it shows a moderate activity on KCa3.1 channel (also referred to as IK1 or SK4) with an IC50 value of 225 nM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

OSK1 is lethal in mice by intracerebroventricular injection, with a LD50 (50% lethal dose) value of 2 μg/kg[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

4205.17

Formula

C28H40N4O6
CAS 号

183815-75-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent Solubility
In Vitro:;

H2O

Peptide Solubility and Storage Guidelines:

1.;;Calculate the length of the peptide.

2.;;Calculate the overall charge of the entire peptide according to the following table:

; Contents Assign value
Acidic amino acid Asp (D), Glu (E), and the C-terminal -COOH. -1
Basic amino acid Arg (R), Lys (K), His (H), and the N-terminal -NH2 +1
Neutral amino acid Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) 0

3.;;Recommended solution:

Overall charge of peptide Details
Negative (lt;0) 1.;;Try to dissolve the peptide in water first.
2.;;If water fails, add NH4OH (lt;50 μL).
3.;;If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (gt;0) 1.;;Try to dissolve the peptide in water first.
2.;;If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
3.;;If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0) 1.;;Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
2.;;For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
参考文献

  • [1]. Stéphanie Mouhat, et al. K+ channel types targeted by synthetic OSK1, a toxin from Orthochirus scrobiculosus scorpion venom. Biochem J. 2005 Jan 1;385(Pt 1):95-104.