Somatostatin Receptor

SSTRs; SSTR

Somatostatin Receptor

Related Products

Somatostatin receptors (SSTR1, 2A and B, 3, 4 and 5) belong to the G protein coupled receptor family. Somatostatin receptors are expressed in a variety of human tumors, including most tumors of neuroendocrine origin, breast tumors, certain brain tumors, renal cell tumors, lymphomas, and prostate cancer. Somatostatin triggers cytostatic and cytotoxic effects and has a general inhibitory effect on secretion mediated through its interaction with somatostatin receptors.

The SSTRs 1-4 display weak selectivity for somatostatin-14 binding, whereas SSTR5 is somatostatin-28-selective. Based on structural similarity and reactivity for octapeptide and hexapeptide somatostatin receptor analogs, SSTRs 2, 3 and SSTR5 belong to a similar somatostatin receptor subclass; SSTRs 1-4 react poorly with these analogs and belong to a separate subclass. All five somatostatin receptors are functionally coupled to inhibition of adenylyl cyclase via pertussis toxin-sensitive guanosine triphosphate (GTP)-binding proteins. mRNA for SSTRs 1-5 is widely expressed in brain and peripheral organs and displays an overlapping but characteristic pattern that is subtype-selective and tissue- and species-specific. All pituitary cell subsets express SSTR2 and SSTR5, with SSTR5 being more abundant. Individual pituitary cells coexpress multiple somatostatin receptor subtypes.

Somatostatin Receptor Related Products (75)
Antibodies (4)

By Effects:	Inhibitors (4) Agonists (31) Antagonists (21) Modulators (2) Chemical (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-P0036

Octreotide	Agonist	99.64%
Octreotide (SMS 201-995) is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide (SMS 201-995) can bind to the somatostatin receptor and mainly subtypes 2, 3, and 5, increases Gi activity, and reduces intracellular cAMP production. Octreotide (SMS 201-995) has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly.

HY-17365

Octreotide acetate	Agonist	99.93%
Octreotide acetate, a long-acting synthetic analog of native somatostatin, inhibits growth hormone, glucagon, and insulin more potently.

HY-P1932

Cortistatin-14		99.92%
Cortistatin-14, a neuropeptide have structural similarity to somatostatin-14, binds and exerts its function via the somatostatin receptors (sst1-sst5). Cortistatin-14 shows anticonvulsive, neuroprotective effect and remarkable anti-inflammatory properties.

HY-16381A

Pasireotide acetate	Agonist	99.82%
Pasireotide (SOM230) acetate, 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 acetate can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide acetate also exhibits antisecretory, antiproliferative, and proapoptotic activity.

HY-P1202A

CYN 154806 TFA	Antagonist	99.81%
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.

HY-P0024A

Veldoreotide TFA	Agonist	98.37%
Veldoreotide (DG3173) TFA a somatostatin analogue, binds to and activate the somatostatin receptors (SSTR) 2, 4, and 5. Veldoreotide TFA inhibits growth hormone (GH) secretion in adenomas compared with Octreotide (HY-P0036). Veldoreotide has the potential to be used as pain modulating agent

HY-P4992

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

HY-P5014

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

HY-13466

MK-4256	Antagonist	98.01%
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.

HY-P1201

Cyclosomatostatin	Antagonist	99.52%
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.

HY-145778

AGI-41998		99.88%
AGI-41998 is a potent inhibitor of methionine adenosyltransferase 2A (MAT2A). AGI-41998 is a brain-penetrant compound. AGI-41998 has the potential for exploring the effects of SAM modulation in the central nervous system (CNS) and research of cancer disease.

HY-102037

SSTR5 antagonist 1	Antagonist	99.84%
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.

HY-109155

Paltusotine	Agonist	99.52%
Paltusotine (CRN00808) is an orally active, nonpeptide selective somatostatin type 2 (SST2) receptor agonist. Paltusotine has the potential for maintaining GH and IGF-1 levels after depot somatostatin receptor ligand therapy.Paltusotine can be used in research on acromegaly and neuroendocrine tumors.

HY-114191B

SSTR5 antagonist 2 hydrochloride	Antagonist	99.98%
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).

HY-79135

Pasireotide ditrifluoroacetate	Agonist	99.27%
Pasireotide (SOM230) ditrifluoroacetate, 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 ditrifluoroacetate exhibits antisecretory, antiproliferative, and proapoptotic activity.

HY-P1203

BIM-23056	Antagonist	99.94%
BIM 23056, a linear octapeptide, is a potent sst3 and sst5 somatostatin receptor antagonist with K_i values of 10.8, 5.7, respectively.

HY-145777

AGI-43192		99.53%
AGI-43192 is a potent inhibitor of methionine adenosyltransferase 2A (MAT2A). AGI-43192 is a potent, but limited brain-penetrant compound. AGI-43192 has the potential for exploring the effects of SAM modulation in the central nervous system (CNS) and research of cancer disease.

HY-111615A

J-2156 TFA	Agonist	99.72%
J-2156 TFA is a high potent, selective somatostatin receptor type 4 (SST₄ receptor) agonist with IC₅₀s of 0.05 nM and 0.07 nM for human and rat SST₄ receptors, respectively. J-2156 TFA has anti-inflammatory activity and it is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats.

HY-P5126A

DOTA-LM3 TFA	Antagonist	99.30%
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.

HY-P1932A

Cortistatin-14 TFA		99.85%
Cortistatin-14 (TFA), a neuropeptide have structural similarity to somatostatin-14, binds and exerts its function via the somatostatin receptors (sst1-sst5). Cortistatin-14 (TFA) shows anticonvulsive, neuroprotective effect and remarkable anti-inflammatory properties.

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Somatostatin Receptor

Somatostatin Receptor

Somatostatin Receptor Related Products (75)

Antibodies (4)

Somatostatin Receptor Related Products (75):