Somatostatin Receptor Agonist

L-817818 is a potent and subtype-selective agonist of the somatostatin receptor. L-817818 provides a direct approach to defining somatostatin receptor physiological functions

NNC 26-9100 is a selective somatostatin sst4 receptor full agonist (K_i: 6 nM, EC₅₀: 2 nM). NNC 26-9100 decreases total soluble Aβ42, increases brain neprilysin activity and improves learning.

Pasireotide (SOM230) pamoate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pK_i=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide pamoate exhibits antisecretory, antiproliferative, and proapoptotic activity.

(1R,1'S,3'R/1R,1'R,3'S)-L-054,264 is a selective non-peptide human somatostatin receptor subtype 2 (sst₂) agonist. (1R,1'S,3'R/1R,1'R,3'S)-L-054,264 can be used in the study of retinal neuromodulation.

BIM-23027 is a selective agonist of sst₂ receptor (EC₅₀=0.32 nM), with similar effect to somatostatin (SRIF), a cyclic tetradecapeptide. BIM-23027 stimulates dopamine release, which is mediated by a Glu-dependent mechanism.

SSTR4 agonist 6 (Compound 1) is a SSTR4 agonist. SSTR4 agonist 6 can be used for pain research.

(R)-Verapamil (Dexverapamil) is an optically enantiomer of the oral-active Verapamil (HY-14275). (R)-Verapamil has a relatively low affinity for L-type calcium channels (Ca_v1.2) (IC₅₀ > 300 μM), and its IC₅₀ for sodium channels (sodium channel) is 3.19 μM. (R)-Verapamil exhibits SSTR2 agonistic activity, with an EC₅₀ of 1.3 μM. (R)-Verapamil significantly downregulates the expression of TXNIP protein in diabetic mouse models and significantly inhibits β-cell apoptosis (apoptosis), effectively controlling blood sugar. (R)-Verapamil can be used as a PET tracer for the function of P-glycoprotein (P-gp).

L-796778 is an agonist of the hsst3 receptor. In CHO-K1 cells expressing the hsst3 receptor, L-796778 is a partial agonist that inhibits forskolin (HY-15371)-stimulated cAMP production with an IC₅₀ value of 18 nM.

SSTR3 Agonist-1 (Compound EX 38) is an orally active SSTR3 agonist, with an EC₅₀ of 0.14 nM. SSTR3 Agonist-1 reduces the kidney cystic index. SSTR3 Agonist-1 can be used in the research of autosomal dominant polycystic kidney disease.

BIM 23052 is a somatostatin receptor 5 agonist. BIM 23052 can induce gastric emptying.

(D-Phe5,Cys6,11,N-Me-D-Trp8)-Somatostatin-14 (5-12) amide (Compound 4) is a somatostatin analog with K_ds of 0.61, 11.05, 23.5, 1200 and >1000 nM for SSTR5, SSTR3, SSTR2, SSTR1 and SSTR4, respectively.

BIM-23197 is a selective SST2 (IC₅₀ = 0.19 nM) agonist. BIM-23197 can effectively stimulate intracellular calcium mobilization in cells expressing SST2. BIM-23197 can be used for research on endocrine related conditions.

Octreotide (SMS 201-995) hydrochloride is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide hydrochloride can bind to the somatostatin receptors which are mainly subtypes 2, 3 and 5. Octreotide hydrochloride increases Gi activity and reduces intracellular cAMP production. Octreotide hydrochloride has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly.

Tyr-(D-Dab4,Arg5,D-Trp8)-cyclo-Somatostatin-14 (4-11) is a somatostatin agonist that can be used in cancer research.

BIM-23190, a somatostatin analog, a selective SSTR2 and SSTR5 agonist, exhibits K_i values of 0.34 nM and 11.1 nM for SSTR2 and SSTR5, respectively. BIM-23190 can be used in the study for cancer and acromegaly.

Octreotide (SMS 201-995) pamoate is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide pamoate can bind to the somatostatin receptors which are mainly subtypes 2, 3 and 5. Octreotide pamoate increases Gi activity and reduces intracellular cAMP production. Octreotide pamoate has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly.

sst2 Receptor agonist-1 is a potent somatostatin receptor subtype 2 (sst₂) agonist with a K_i value of 0.025 nM and a cAMP IC₅₀ value of 4.8 nM. sst2 Receptor agonist-1 can inhibit rat growth hormone (GH) secretion and ocular neovascular lesion formation. Antiangiogenic effect.

TT-232 TFA (CAP-232 TFA) is an analogue of somatostatin. TT-232 TFA can induce apoptosis of pancreatic tumor cell lines, inhibit tyrosine kinase activity and stimulate tyrosine phosphatase activity in colon tumor cell lines. TT-232 TFA inhibits the proliferation of tumor cells, induces apoptosis of tumor cells and shows strong anti-tumor effects. TT-232 TFA can be used in the development of anti-tumor drugs and the study of apoptosis mechanism.

L803 is a selective Somatostatin Receptor Subtype 4 (SST4) agonist. L803 inhibits L-type calcium channel currents (I_Ca). L803 is promising for research of retinal ganglion cell (RGC) degenerative diseases (e.g., glaucoma).

L-779976 is a compound with bradykinin agonist activity. Injection into the amygdala and septum of the rat brain can produce anxiolytic effects. Its bradykinin agonist activity has been verified by relevant experiments.