sstr

Octreotide (SMS 201-995) 是一种有效的生长激素、胰高血糖素和胰岛素抑制剂。它主要与生长抑素 2、3 和 5 亚型受体结合，可增强 Gi 活性，降低胞内 cAMP 的产生。

Octreotide Acetate (Sandostatin) 是一种长期有效的合成生长抑素八肽类似物，可抑制生长激素的分泌。

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。

Paltusotine 是一种口服有效的，非肽选择性生长抑素 2 型受体激动剂。在长效生长抑素受体配体作用后，Paltusotine 仍可维持 GH 和 IGF-1 水平。

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

SSTR5 antagonist 1 is a selective, and orally available antagonist of somatostatin receptor subtype 5 (SSTR5)(IC50s of 9.6 and 57 nM for hSSTR5 and mSSTR5, respectively).

SSTR5 antagonist 2 is a highly potent, oral active and selective antagonist of somatostatin (receptor) subtype 5 (SSTR5),with potential to treat type 2 diabetes mellitus (T2DM).

SSTR5 antagonist 2 TFA is a highly potent, oral active and selective antagonist of somatostatin (receptor) subtype 5 (SSTR5), with potential to treat type 2 diabetes mellitus (T2DM).

Cyclic SSTR agonist octreotide 是一种 Octreotide ，可作为生长抑素受体 (SSTR) 的激动剂。

SSTR4agonist-1 (Compound 47) 是一种选择性激活生长抑素受体 4 (SSTR4) 的激动剂，EC50为 4.7 nM，并且在人体肝微粒体中的半衰期超过 130 分钟。

SSTR4 agonist5 (Compound 5) 是一种口服有效的生长抑素受体 4 (SSTR4) 激动剂，EC50为 0.228 nM。在人和大鼠肝微粒体中，SSTR4 agonist5 显示出良好的稳定性，并且能够在大鼠模型中抑制机械痛觉过敏。

SSTR4 agonist 2 是有效的生长抑素受体亚型 4 (SSTR4) 激动剂，在 SSTR4 相关的医学疾病研究中具有潜力。SSTR4 通路抑制痛觉和炎症。

SSTR4 agonist 4 是一种有效的SSTR4激动剂，具有用于疼痛研究的潜力。SSTR4 激动剂在与急性和慢性相关的抗外周伤害感受和抗炎活性相关疼痛的啮齿动物模型中有效。SSTR4 在海马和新皮质、记忆和学习区域以及阿尔茨海默病病理学中的表达水平相对较高。

SSTR4 agonist 3 is a potent compound that activates the SSTR4 receptor. The SSTR4 receptor is highly expressed in the hippocampus and neocortex, which are regions associated with memory, learning, and Alzheimer's disease pathology. SSTR4 agonists demonstrate strong efficacy in rodent models of pain, both acute and chronic, by reducing peripheral nociception and inflammation. Considering its potential application in pain research, SSTR4 agonist 3 is of interest[1].

SSTR5 antagonist 2 hydrochloride 是一种强效的、口服具有活力的、选择性的生长激素抑制激素(受体)亚型 5 (SSTR5) 拮抗剂，对 2 型糖尿病表现出研究潜力。

SSTR5agonist 3（Compound 23）作为一种SSTR5（生长抑素受体亚型 5）拮抗剂，展示了低hERG抑制作用及良好的口服活性。其在人体和小鼠中的IC50值分别为2.8 nM和1.4 nM。SSTR5agonist 3主要应用于抗胆结石研究领域。

SSTR5 antagonist 6, an orally active antagonist specific to the somatostatin receptor subtype 5 (SSTR5), exhibits an IC50 value of 24 nM. This compound is utilized in researching type 2 diabetes [1].

Leupeptin hemisulfate 是一种蛋白酶抑制剂，具有细胞膜渗透性、可逆性、竞争性和口服活性。Leupeptin hemisulfate 可以抑制 Cathepsin B、Cathepsin H、Cathepsin L 的活性，阻断两性溶酶体的融合。Leupeptin hemisulfate 还具有抗炎活性。

Kanamycin sulfate (Kanamycin monosulfate) 属于氨基糖苷类抗生素，通过与细菌 70S 核糖体亚基结合来干扰蛋白质合成。Kanamycin sulfate 具有抗菌活性，对革兰氏阳性菌和阴性菌及支原体都有抑制作用。

Veldoreotide (DG3173) TFA，一种生长抑素类似物，能够结合并激活SSTR 2 4 5。其在腺瘤中抑制生长激素分泌的效果相较于Octreotide更为显著。此外，Veldoreotide亦展现出作为镇痛剂的潜力。

BN-81,674 is a bioactive chemical.

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.

Tidutamab (XmAb-18087) 是一种人源化靶向生长抑素受体2 （SSTR2）和 T 细胞结合域 (CD3)的双特异性抗体，具有抗肿瘤活性，可用于研究胃神经分泌肿瘤。

Veldoreotide, also known as Somatoprim, is a unique somatostatin receptor subtypes 2-, 4- and 5-selective analogue which effectively reduces GH secretion in human GH-secreting pituitary adenomas, even in Octreotide non-responsive tumours.