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首页-小分子抑制剂&激动剂-GPCR-Somatostatin Receptor-Abantide
Abantide

Chemical Structure : Abantide

CAS No.: 1683515-77-6

Abantide (Cortistatin analogue A5)

货号: PC-28505Not For Human Use, Lab Use Only.

Abantide (Cortistatin analogue A5) is a cortistatin analogue with anti-inflammatory and immunomodulator effects, shows potent and preferential binding to somatostatin receptors SSTR3, SSTR4 and SSTR5 with binding IC50 of 5.1 nM, 4.1 nM and 1.12 nM respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Abantide (Cortistatin analogue A5) is a cortistatin analogue with anti-inflammatory and immunomodulator effects, shows potent and preferential binding to somatostatin receptors SSTR3, SSTR4 and SSTR5 with binding IC50 of 5.1 nM, 4.1 nM and 1.12 nM respectively.
Abantide (Cortistatin analogue A5) shows much lower binding to SSTR1 and SSTR2 with binding IC50 of 47.3 nM and 35 nM.
Abantide (Cortistatin analogue A5) reduces Th1 and Th17 cells and induces regulatory T cells in mice with ulcerative colitis.
Abantide (Cortistatin analogue A5) displaysa 10-fold stability increase in serum while preserving the pattern of immunosuppressive and anti-inflammatory activity of CST in vitro and in animal models of inflammatory bowel disease.

物理化学性质&存储条件

分子量 1903.32
分子式 C93H135N19O20S2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

L-Lysine, 1-(1-oxooctyl)-L-prolyl-L-cysteinyl-L-lysyl-L-asparaginyl-2,4,6-trimethyl-L-phenylalanyl-L-phenylalanyl-D-tryptophyl-L-lysyl-L-threonyl-L-phenylalanyl-L-threonyl-L-seryl-L-cysteinyl-, cyclic (2→13)-disulfide

参考文献

1. Patent WO2015040089 A1.

2. Álvaro Rol, et al. Nat Commun. 2021 Mar 25;12(1):1869.

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