Somatostatin Receptor Modulator

SSTR5/TGR5-modulator-1 is an orally active and dual-target small molecule, balanced in vitro activity at human TGR5 and human SSTR5. SSTR5/TGR5-modulator-1 activates human TGR5 to promote cAMP accumulation. SSTR5/TGR5-modulator-1 blocks human SSTR5 to inhibit agonist-induced calcium mobilization. SSTR5/TGR5-modulator-1 improves glucose tolerance in mice. SSTR5/TGR5-modulator-1 alleviates gallbladder filling in mice at pharmacologically relevant doses. SSTR5/TGR5-modulator-1 has suboptimal physicochemical and metabolic properties.SSTR5/TGR5-modulator-1 can be used for the research of type 2 diabetes mellitus.

Cortistatin-17 (human) is a somatostatin neuropeptide with potential for studying diseases such as cancer, inflammation, autoimmunity, fibrosis, and pain.

Cortistatin-29 (human) is a somatostatin neuropeptide with potential for studying diseases such as cancer, inflammation, autoimmunity, fibrosis, and pain.

Seglitide (MK-678) is an orally active, selective SSTR2 agonist and somatostatin analog. Seglitide also acts as a competitive Somatostatin receptor antagonist, with pA2 values of 6.50, 6.24 and 6.09 against SS₁₄, SS₂₅ and SS₂₈, respectively. Seglitide produces only weak, transient inhibition of myocardial contractility in isolated right atria of guinea pigs. Seglitide inhibits glucagon secretion and reduces circulating insulin levels. Seglitide causes a sustained, reversible reduction in elevated systolic blood pressure in streptozotocin (HY-13753)-induced diabetic rats, but exerts no effect on spontaneously hypertensive rats. Seglitide induces membrane hyperpolarization and inhibits electrical excitability. Seglitide induces concentration-dependent contraction and significant desensitization in isolated distal colon of rats. Seglitide can be used in research related to hypertension complicated with insulin-dependent diabetes mellitus.