sst1

Pasireotide (SOM230) acetate是长效的环己肽生长激素抑制素类似物，具有抗分泌、抗增殖和促凋亡活性。Pasireotide (SOM230) acetate可抑制 GH、IGF-I 和 ACTH 的分泌，可用于研究肢端肥大症和库欣病。Pasireotide (SOM230) acetate还可以提高生长抑素受体的激动剂活性，对sst1、2、3、4、5的pKi 分别为 8.2、9.0、9.1、小于7.0 和 9.9。

L-797,591 hydrochloride 对生长抑素受体亚型 1 (SSTR1)有活性。L-797,591 hydrochloride 常与 AG1478 联合使用来增强表达 SSTR1的细胞中 p-ERK5的表达。L-797,591 hydrochloride 在共转染的细胞中显著增强了 p38的磷酸化，这一作用在与 AG1478联合处理时被逆转。

L-803087 是一种具有高效性和选择性的生长抑素 sst4 受体激动剂，对 sst4 的 Ki 值为 0.7 nM，比其他生长抑素受体的选择性高 280 倍以上。L-803087 在体外诱导 AMPA 介导的海马突触反应，在体内增加了海藻酸盐促使的小鼠癫痫发作。

Cortistatin-14 是一种与生长抑素-14结构相似的神经肽，具有抗惊厥和神经保护作用，通过激活 sst（2）、生长素释放肽和 GABA（A B） 受体损害小鼠的识别记忆巩固，可用于研究脓毒症引发的认知障碍。

PRL 3195 是一种somatostatin receptor 拮抗剂，对人生长抑素受体 sst5、sst2、sst3、sst1和 sst4的Ki 分别为 6、17、66、1000 和 1000 nM。

PRL 2915 是一种有效的人类生长抑素亚型 2 受体拮抗剂 (hsst2)，其Ki 为 12 nM。

Cortistatin-29 is a neuropeptide that is structurally similar to somatostatin-28. It is produced by cleavage of preprocortistatin to procortistatin, which is cleaved at dibasic amino acids to form cortistatin-29 and cortistatin-14 as well as other partial cleavage products. Cortistatin mRNA is expressed in the human brain and in interneurons of the rat hippocampus and cerebral cortex. Cortistatin-29 binds to somatostatin (SST) receptors with IC50 values of 2.8, 7.1, 0.2, 3, and 13.7 nM for SST1-5, respectively. Cortistatin-29 is found at similar levels as cortistatin-14 in mouse AtT20 cells but is secreted at a lower level. Cortistatin-29 corresponds to residues 85-112 of the rat peptide sequence.

Toxic Shock Syndrome Toxin-1 (TSST-1) (58-78)为T细胞增殖激活剂，以剂量依赖性方式增强人外周血单核细胞(PBMC)的体外增殖，适用于癌症与炎症免疫研究。

sst1/sst4 somatostatin receptors agonist

Pasireotide(SOM 230) is a stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1 2 3 4 5, pKi=8.2 9.0 9.1 <7.0 9.9 respectively).

L-796,778 acetate 是一种选择性生长抑素受体激动剂，对 sst3的IC50为24nM，对sst1、sst2、sst4和sst5的IC50大于1000nM。

CYN 154806 TFA(183658-72-2 free base) 是一种环状八肽，是一种有效的选择性生长抑素 sst2 受体拮抗剂。对于重组 sst2、sst1、sst3、sst4 和 sst5 受体，pIC50 值分别为 8.58、5.41、6.07、5.76 和 6.48。

Peptide agonist for sst2 and sst5 somatostatin receptors. IC50/Kd values (nM) at cloned human somatostatin receptors are: > 1000 (sst1), 0.2 - 1.5 (sst2), 27 - 36 (sst3), > 127 (sst4), and 0.06 - 23 (sst5).

SRA880 is a non-peptide antagonist of somatostatin sst1-receptor. SRA880 displayed significantly lower affinity for the other human recombinant somatostatin receptors ( pK(d) < or = 6.0). SRA880 shows a certain binding affinity to the human dopamine D4 re

Pasireotide (SOM230) diaspartate 是一种长效的环己肽生长激素抑制素类似物，可以提高生长抑素受体的激动剂活性，对sst1 2 3 4 5的pKi 分别为 8.2 9.0 9.1 <7.0 9.9。Pasireotide diaspartate 具有抗分泌、抗增殖和促凋亡活性。

Pasireotide pamoate is a stable cyclohexapeptide somatostatin mimic. Pasireotide pamoate exhibits antisecretory, antiproliferative, and proapoptotic activity.

Pasireotide L-aspartate salt is a stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1 2 3 4 5, pKi=8.2 9.0 9.1 <7.0 9.9 respectively).

Pasireotide is a stable cyclohexapeptide somatostatin mimic.

L-803087 TFA is a highly potent and selective agonist of the somatostatin sst4 receptor, exhibiting a Ki value of 0.7 nM. It displays a remarkable selectivity, being over 280-fold more preferential for the sst4 receptor compared to other somatostatin receptors. Furthermore, L-803087 TFA promotes AMPA-mediated synaptic responses in hippocampal preparations and enhances kainate-induced seizures in mice.

Cortistatin-14 acetate 是一种与生长抑素-14结构相似的神经肽，通过生长抑素受体 (sst1-sst5) 结合并发挥作用。Cortistatin-14 acetate 具有抗惊厥、神经保护作用和显著的抗炎作用。

CYN 154806 is a potent and selective somatostatin sst2 receptor antagonist, The pIC50 values are 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively.

Potent somatostatin receptor 1 (sst1) agonist; displays selectivity for sst1 (IC50 values are 30.9 nM, 345 nM, > 1 μM, > 10 μM and > 10μM for human sst1, sst3, sst4, sst2 and sst5 respectively). Attenuates somatostatin release in the rat nucleus accumbens