CYN 154806

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CYN 154806

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

183658-72-2

包装与价格：

包装	价格(元)
1mg	电议
5mg	电议
10mg	电议

产品介绍

CYN 154806 是一种环状八肽，是一种强效的，选择性生长抑素sst2受体的拮抗剂，其对人重组 sst2、sst1、sst3、sst4 和sst5 受体的pIC₅₀值分别为 8.58、5.41、6.07、5.76 和 6.48。

生物活性

CYN 154806, a cyclic octapeptide, is a potent and selectivesomatostatin sst2 receptorantagonist, withpIC₅₀values of 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively^[1]^[2].

IC₅₀& Target

Somatostatin Receptor^[1].

体外研究
(In Vitro)

CYN 154806 inhibits SRIF-induced increases in extracellular acidification (EAR) in CHO-K1 cells expressing human sst2 receptors (pKB 7.92). CYN 154806 also blocks SRIF-induced increases [35S]-GTPγS binding in CHO-K1 cell membranes expressing human sst2 receptors as well as rat sst2(a) and rat sst2(b) receptors (pKB 7.81, 7.68 and 7.96, respectively)^[2].

体内研究
(In Vivo)

CYN 154806 (0.1 mg/kg; i.p.; 20 min before the administration of carbachol (CCh) (30 μg/kg) in M4 KO mice) dose-dependently and significantly reverses the decreases acid response to CCh in M4 but not M3 KO mice^[3].

分子量

1197.34

Formula

C₅₆H₆₈N₁₂O₁₄S₂

CAS 号

183658-72-2

Sequence

Ac-Phe(4-NO2)-Cys-Tyr-Trp-Lys-Thr-Cys-Tyr-NH2 (Disulfide bridge: Cys2-Cys7)

Sequence Shortening

Ac-F(4-NO2)CYWKTCY-NH2 (Disulfide bridge: Cys2-Cys7)

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 (<0)	1. Try to dissolve the peptide in water first. 2. If water fails, add NH₄OH (<50 μL). 3. If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (>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.