Somatostatin Receptor Antagonist

SSTR5 antagonist 4 (compound 1) is a potent, selective and orally active somatostatin subtype 5 (SSTR5) antagonist (hSSTR5 IC₅₀ = 1.3 nM, mSSTR5 IC₅₀ = 1.0 nM). SSTR5 antagonist 4 shows efficacy in mouse oral glucose tolerance test (OGTT) in high fat diet (HFD)-mice. SSTR5 antagonist 4 can be used for type 2 diabetes research.

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

MK-4256 is a potent and selective SSTR3 antagonist with IC₅₀s of 0.66 nM and 0.36 nM in human and mouse receptor binding assays, respectively.

DOTA-LM3 is a somatostatin receptor (SSTR) antagonist. LM3 refers to p-Cl-Phe- cyclo(D-Cys-Tyr-D-4-amino-Phe(carbamoyl)-Lys-Thr-Cys)D-Tyr- NH2, as well as a somatostatin antagonist. DOTA-LM3 is often isotopically labeled for tracing tumors in vivo, such as 177Lu-DOTA-LM3 and 68 Ga-DOTA-LM3. 68 Ga-DOTA-LM3 shows favorable biodistribution, high tumor uptake, good tumor retention, and few safety concerns. 177Lu-DOTA-LM3 can be used for research in DOTATOC-negative liver metastases, such as pancreatic NET and extensive tumor thrombosis. DOTA-LM3 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).

DOTA-JR11 is a somatostatin receptor 2 （SSTR2）antagonist. DOTA-JR11 can be labeled by 68Ga, used for paired imaging in neuroendocrine tumors (NETs) research. DOTA-JR11 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).

Satoreotide (JR11) is a somatostatin receptor subtype 2 (sstr2)-selective antagonist. Satoreotide can be used as a PET imaging agent when labeled with ⁶⁸Ga. Satoreotide can be used for cancer research.

Cyclosomatostatin is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells.

SSTR5 antagonist 1 (compound 25a) is a selective and orally available somatostatin receptor subtype 5 (SSTR5) antagonist with IC₅₀s of 9.6 and 57 nM for hSSTR5 and mSSTR5, respectively.

NODAGA-LM3 is a ligand that can cross the blood-brain barrier and targets somatostatin receptor SSTR2 with high affinity (IC₅₀ = 1.3 nM). NODAGA-LM3 does not trigger the internalization of SSTR2 and can inhibit agonist-induced internalization processes. NODAGA-LM3 shows low uptake in normal tissues such as the liver and spleen, but high uptake in the lungs and blood pool. ⁶⁸Ga-labeled NODAGA-LM3 can serve as a PET imaging agent for well-differentiated neuroendocrine tumors, and is applied in studies related to small cell lung cancer and well-differentiated neuroendocrine tumors.

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

BIM 23056, a linear octapeptide, is a potent sst3 and sst5 somatostatin receptor antagonist with K_i values of 10.8, 5.7, respectively.

SRA880 is a non-peptide and selective somatostatin sst(1) receptor antagonist. SRA880 exhibits antidepressant-like effects when in combination with Imipramine (HY-B1490A) .

PRL 2915 is a potent human somatostatin subtype 2 receptor (hsst₂) antagonist with a K_i of 12 nM.

DOTA-LM3 TFA is a somatostatin receptor (SSTR) antagonist. LM3 refers to p-Cl-Phe- cyclo(D-Cys-Tyr-D-4-amino-Phe(carbamoyl)-Lys-Thr-Cys)D-Tyr- NH2, as well as a somatostatin antagonist. DOTA-LM3 TFA is often isotopically labeled for tracing tumors in vivo, such as 177Lu-DOTA-LM3 TFA and 68 Ga-DOTA-LM3 TFA. 68 Ga-DOTA-LM3 TFA shows favorable biodistribution, high tumor uptake, good tumor retention, and few safety concerns. 177Lu-DOTA-LM3 TFA can be used for research in DOTATOC-negative liver metastases, such as pancreatic NET and extensive tumor thrombosis. DOTA-LM3 (TFA) can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).

SSTR5 antagonist 2 hydrochloride is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential for the research of type 2 diabetes mellitus (T2DM).

NODAGA-LM3 TFA is a ligand that can cross the blood-brain barrier and targets somatostatin receptor SSTR2 with high affinity (IC₅₀ = 1.3 nM). NODAGA-LM3 TFA does not trigger the internalization of SSTR2 and can inhibit agonist-induced internalization processes. NODAGA-LM3 TFA shows low uptake in normal tissues such as the liver and spleen, but high uptake in the lungs and blood pool. ⁶⁸Ga-labeled NODAGA-LM3 TFA can serve as a PET imaging agent for well-differentiated neuroendocrine tumors, and is applied in studies related to small cell lung cancer and well-differentiated neuroendocrine tumors.

PRL 3195 is a somatostatin receptor antagonist with K_is of 6, 17, 66, 1000 and 1000 nM for human somatostatin receptors (sst₅, sst₂, sst₃, sst₁ and sst₄, respectively).

SSTR5 antagonist 2 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential for the research of treat type 2 diabetes mellitus (T2DM).

SSTR5 Antagonist 1 (compound 10) is a highly potent, oral active and selective somatostatin (receptor) subtype 5 (SSTR5) antagonist and has potential for the research of treat type 2 diabetes mellitus (T2DM).

BN-81674 is a somatostatin analogue and a selective antagonist of the non-peptide human somatostatin sst₃ receptor (K_i=0.92 nM). In addition, BN-81674 reversed the inhibition of cyclic AMP accumulation induced by 1 nM somatostatin through the sst₃ receptor with an IC₅₀ value of 0.84 nM. BN-81674 can be used in cancer research.