Search Result
Results for "
Somatostatin Receptor
" in MedChemExpress (MCE) Product Catalog:
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-108498
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Somatostatin Receptor
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Endocrinology
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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
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- HY-123499
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Somatostatin Receptor
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Cardiovascular Disease
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SRA880 is a non-peptide and selective somatostatin sst(1) receptor antagonist. SRA880 exhibits antidepressant-like effects when in combination with Imipramine (HY-B1490A) .
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- HY-P0036
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Octreotide
Maximum Cited Publications
13 Publications Verification
SMS 201-995
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Somatostatin Receptor
Apoptosis
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Cardiovascular Disease
Inflammation/Immunology
Endocrinology
Cancer
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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 .
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- HY-106103A
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MK 678 acetate; L 36358 acetate
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Somatostatin Receptor
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Cardiovascular Disease
Neurological Disease
Metabolic Disease
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Seglitide acetate (MK 678; L 36358 acetate) is a potent, orally active somatostatin receptor 2 (SSTR2) agonist, and also a competitive antagonist of SSTR14, SSTR25, and SSTR28. Seglitide acetate has antihypertensive effects and can inhibit plasma glucagon and growth hormone. Seglitide acetate can be used for research on diabetes .
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- HY-106103
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- HY-P10920
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Drug Derivative
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Cancer
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DOTAMTATE is a somatostatin analogue. DOTAMTATE marked 212Pb is promising for research of somatostatin receptor positive neuroendocrine tumors .
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- HY-P1207
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- HY-P0036B
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SMS 201-995 pamoate
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Somatostatin Receptor
Apoptosis
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Cardiovascular Disease
Inflammation/Immunology
Endocrinology
Cancer
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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 .
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- HY-P1335
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Opioid Receptor
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Neurological Disease
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CTAP is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC50 of 3.5 nM. CTAP displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .
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- HY-157303
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Somatostatin Receptor
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Cardiovascular Disease
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SSTR5 antagonist 3 (Compound 23) is an orally active somatostatin receptor subtype 5 (SSTR5) antagonist with low hERG inhibition. SSTR5 antagonist 3 exhibits potency with IC50 values of 2.8 nM and 1.4 nM in human and mouse, respectively. SSTR5 antagonist 3 can be used for the research of anti-gallstone .
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- HY-P1335A
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Opioid Receptor
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Neurological Disease
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CTAP TFA is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC50 of 3.5 nM. CTAP TFA displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .
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- HY-111615
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Somatostatin Receptor
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Neurological Disease
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J-2156 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 is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats .
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- HY-111615A
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Somatostatin Receptor
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Neurological Disease
Inflammation/Immunology
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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 .
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- HY-P3954
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Somatostatin Receptor
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Metabolic Disease
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Somatostatin-28 (sheep, human rat mouse) is a biologically active polypeptide, synthesised in the proximal intestinal epithelial cells. Somatostatin-28 (sheep, human rat mouse) suppresses glucose-stimulated insulin secretion without affecting circulating basal insulin concentration. Somatostatin-28 (sheep, human rat mouse) also targets to somatostatin receptor subtype 5 (SSTR5) to regulate GLP-1 secretion .
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- HY-P4469
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- HY-P4957
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Somatostatin Receptor
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Others
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Octreotide dimer parallel is a dimer parallel of Octreotide. Octreotide (HY-P0036) is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue .
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- HY-P1201
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Somatostatin Receptor
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Cancer
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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 .
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- HY-123460
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Somatostatin Receptor
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Cancer
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BN-81674 is a somatostatin analogue and a selective antagonist of the non-peptide human somatostatin sst3 receptor (Ki=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 .
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- HY-P1201A
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Somatostatin Receptor
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Cancer
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Cyclosomatostatin TFA is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin TFA can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells .
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- HY-16381C
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(2R)-SOM230 (diaspartate)
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Endogenous Metabolite
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Others
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(2R)-Pasireotide ((2R)-SOM230) diaspartate exhibits a 40-fold higher affinity for somatostatin receptor 5 than other somatostatin analogs.
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- HY-P1932A
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- HY-125382
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- HY-109155
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CRN00808
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Somatostatin Receptor
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Endocrinology
Cancer
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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 .
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- HY-109155A
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CRN00808 hydrochloride
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Somatostatin Receptor
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Neurological Disease
Endocrinology
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Paltusotine (CRN00808) hydrochloride is an orally active, nonpeptide selective somatostatin type 2 (SST2) receptor agonist. Paltusotine hydrochloride has the potential for maintaining GH and IGF-1 levels after depot somatostatin receptor ligand therapy.Paltusotine hydrochloride can be used in research on acromegaly and neuroendocrine tumors .
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- HY-P4452
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- HY-108497
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Somatostatin Receptor
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Neurological Disease
Cancer
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L-803087 is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM. L-803087 is >280-fold higher than other somatostatin receptors. L-803087 facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice .
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- HY-108497A
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Somatostatin Receptor
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Neurological Disease
Cancer
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L-803087 TFA is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM. L-803087 TFA is >280-fold more selective for sst4 receptor than other somatostatin receptors. L-803087 TFA facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice .
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- HY-159825
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- HY-P1932
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- HY-P0024
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DG3173; PTR-3173
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Somatostatin Receptor
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Endocrinology
Cancer
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Veldoreotide (DG3173) a somatostatin analogue, binds to and activate the somatostatin receptors (SSTR) 2, 4, and 5. Veldoreotide inhibits growth hormone (GH) secretion in adenomas compared with Octreotide (HY-P0036). Veldoreotide has the potential to be used as pain modulating agent
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- HY-P4100
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Somatostatin Receptor
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Others
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Cyclic SSTR agonist octreotide is a Octreotide (HY-P0036), serving as the cyclic Somatostatin Receptor SSTR agonist .
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- HY-P0024A
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DG3173 TFA; PTR-3173 TFA
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Somatostatin Receptor
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Endocrinology
Cancer
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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
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- HY-P5126
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Radionuclide-Drug Conjugates (RDCs)
Somatostatin Receptor
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Cancer
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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).
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- HY-P5126A
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Radionuclide-Drug Conjugates (RDCs)
Somatostatin Receptor
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Cancer
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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).
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- HY-P1203
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- HY-P1203A
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- HY-79135
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SOM230 ditrifluoroacetate; Pasireotide TFA salt
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Somatostatin Receptor
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Endocrinology
Cancer
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Pasireotide (SOM230) ditrifluoroacetate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide ditrifluoroacetate exhibits antisecretory, antiproliferative, and proapoptotic activity .
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- HY-16381B
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SOM230 (diaspartate)
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Somatostatin Receptor
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Neurological Disease
Cancer
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Pasireotide (SOM230) diaspartate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide diaspartate exhibits antisecretory, antiproliferative, and proapoptotic activity .
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- HY-108768
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SOM230 pamoate
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Somatostatin Receptor
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Endocrinology
Cancer
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Pasireotide (SOM230) pamoate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide pamoate exhibits antisecretory, antiproliferative, and proapoptotic activity .
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- HY-79136
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SOM230 L-aspartate
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Somatostatin Receptor
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Endocrinology
Cancer
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Pasireotide (SOM230) L-aspartate salt, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide L-aspartate salt exhibits antisecretory, antiproliferative, and proapoptotic activity .
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- HY-P10758
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- HY-164040
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Somatostatin Receptor
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Metabolic Disease
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Zavolosotine (Compound 1) is an orally active agonist for somatostatin receptor type 5 (SST5) with EC50 <1 nM. Zavolosotine inhibits insulin and glucagon secretion, increases levels of glucagon in blood in rat model .
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- HY-160176
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Somatostatin Receptor
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Metabolic Disease
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SSTR5 antagonist 6 is an orally active somatostatin receptor subtype 5 (SSTR5) antagonist with an IC50 of 24 nM. SSTR5 antagonist 6 can be used in the study of type 2 diabetes .
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- HY-114191B
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Somatostatin Receptor
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Metabolic Disease
Endocrinology
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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) .
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- HY-102037
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- HY-16381A
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SOM230 acetate
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Somatostatin Receptor
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Endocrinology
Cancer
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Pasireotide (SOM230) acetate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=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 .
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- HY-16381
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SOM230
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Somatostatin Receptor
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Endocrinology
Cancer
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Pasireotide (SOM230), a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide also exhibits antisecretory, antiproliferative, and proapoptotic activity .
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- HY-110161
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Somatostatin Receptor
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Cardiovascular Disease
Endocrinology
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sst2 Receptor agonist-1 is a potent somatostatin receptor subtype 2 (sst2) agonist with a Ki 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 .
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- HY-P1212
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CST-14 (mouse, rat)
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Somatostatin Receptor
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Neurological Disease
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Cortistatin 14, mouse, rat (CST-14, human, rat), a neuropeptide with neuronal depressant and sleep modulating properties, can bind to all five cloned somatostatin receptors (SSTRs) and ghrelin receptor to exert its biological activities and co-exists with GABA within the cortex and hippocampus .
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- HY-P3294
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- HY-114191
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Somatostatin Receptor
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Metabolic Disease
Endocrinology
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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) .
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- HY-114191A
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Somatostatin Receptor
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Metabolic Disease
Endocrinology
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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) .
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- HY-108499
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- HY-P1202A
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Somatostatin Receptor
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Endocrinology
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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 .
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- HY-P1202
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Somatostatin Receptor
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Endocrinology
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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 .
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- HY-123335
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Somatostatin Receptor
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Others
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L-796,778 is an agonist of the hsst3 receptor. In CHO-K1 cells expressing the hsst3 receptor, L-796,778 is a partial agonist that inhibits forskolin (HY-15371)-stimulated cAMP production with an IC50 value of 18 nM .
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- HY-139347
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- HY-P3958
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- HY-P1206
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Somatostatin Receptor
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Neurological Disease
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CH 275 is a peptide analog of somatostatin and binds preferably to somatostatin receptor 1 (sst1) with a Ki of 52 nM . CH 275 acts as a potent and selective sst1 agonist (IC50=30.9 nM) and also displays IC50 values of 345 nM, >1 μM, >10 μM, >10 μM for human sst3, sst4, sst2 and sst5, respectively . CH 275 can be used for the research of alzheimer’s disease .
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- HY-163317
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Somatostatin Receptor
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Cancer
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MMC(TMZ)-TOC has high binding affinity and selectivity for somatostatin receptor subtype-2 (SSTR2). MMC(TMZ)-TOC targets delivery of TMZ to SSTR2-positive tumor cells. MMC(TMZ)-TOC can be used for the research of cancer .
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- HY-172147
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Somatostatin Receptor
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Neurological Disease
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SSTR4 agonist 5 (Compound 5) is the orally active agonist for somatostatin receptor 4 (SSTR4) with an EC50 of 0.228 nM. SSTR4 agonist 5 exhibits good stability in human/rat liver microsomes. SSTR4 agonist 5 inhibits mechanical hyperalgesia in rat models .
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- HY-P2112
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DOTA-Nal3-octreotide
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Radionuclide-Drug Conjugates (RDCs)
Somatostatin Receptor
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Others
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DOTA-NOC (DOTA-Nal3-octreotide) is a high-affinity ligand of somatostatin receptor subtypes 2, 3 and 5. DOTA-NOC can be used for labeling with various radiometals, and development of radiopeptide imaging . DOTA-NOC can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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- HY-163317A
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Somatostatin Receptor
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Cancer
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MMC(TMZ)-TOC TFA has high binding affinity and selectivity for somatostatin receptor subtype-2 (SSTR2). MMC(TMZ)-TOC TFA targets delivery of TMZ to SSTR2-positive tumor cells. MMC(TMZ)-TOC TFA can be used for the research of cancer .
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- HY-142699
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Somatostatin Receptor
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Inflammation/Immunology
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SSTR4 agonist 2 is a potent agonist of somatostatin receptor subtype 4 (SSTR4). SSTR4 pathway inhibits nociceptive and inflammatory processes. SSTR4 agonist 2 has the potential for the research of medical disorders related to SSTR4 (extracted from patent WO2014184275A1, compound 107) .
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- HY-P5128
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Satoreotide tetraxetan
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Radionuclide-Drug Conjugates (RDCs)
Somatostatin Receptor
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Cancer
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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).
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- HY-103277A
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- HY-103277
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- HY-120287
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Somatostatin Receptor
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Endocrinology
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L-054522 is an agonist for somatostatin receptor subtype 2 with Kd of 0.01 nM. L-054522 inhibits growth hormone release from rat primary pituitary cell (IC50=0.05 nM) and glucagon and insulin release from isolated mouse pancreatic islet cell (IC50=0.05 nM and 12 nM) .
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- HY-P0221C
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PACAP Receptor
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Endocrinology
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PACAP (1-38) free acid is an endogenous neuropeptide. PACAP (1-38) free acid potently stimulates antral motility and somatostatin secretion, inhibits the secretion of gastrin and stimulates the release of vasoactive intestinal polypeptide, gastrin releasing peptide and substance P. PACAP (1-38) free acid also enhances N-methyl-D-aspartate receptor function and expression of brain-derived neurotrophic factor through RACK1 .
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- HY-P0221B
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PACAP Receptor
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Endocrinology
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PACAP (1-38) free acid TFA is an endogenous neuropeptide. PACAP (1-38) free acid TFA potently stimulates antral motility and somatostatin secretion, inhibits the secretion of gastrin and stimulates the release of vasoactive intestinal polypeptide, gastrin releasing peptide and substance P. PACAP (1-38) free acid TFA also enhances N-methyl-D-aspartate receptor function and expression of brain-derived neurotrophic factor through RACK1 .
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- HY-P2090
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Somatostatin Receptor
Adenylate Cyclase
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Cardiovascular Disease
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Angiopeptin, a cyclic octapeptide analogue of somatostatin, is a weak sst2/sst5 receptor partial agonist with IC50 values of 0.26 nM and 6.92 nM, respectively. Angiopeptin is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin inhibits adenylate cyclase or stimulates extracellular acidification. Angiopeptin has the potential for coronary atherosclerosis research .
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- HY-P2090A
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Somatostatin Receptor
Adenylate Cyclase
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Cardiovascular Disease
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Angiopeptin TFA, a cyclic octapeptide analogue of somatostatin, is a weak sst2/sst5 receptor partial agonist with IC50 values of 0.26 nM and 6.92 nM, respectively. Angiopeptin TFA is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin TFA inhibits adenylate cyclase or stimulates extracellular acidification. Angiopeptin TFA has the potential for coronary atherosclerosis research .
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- HY-P2150
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Somatostatin Receptor
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Neurological Disease
Inflammation/Immunology
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Cortistatin-29 is a neuropeptide. Cortistatin-29 alleviates neuropathic pain. Cortistatin-29 binds all somatostatin (SS) receptor subtypes with high affinity and shows IC50 values of 2.8 nM, 7.1 nM, 0.2 nM, 3.0 nM, 13.7 nM for SSTR1, SSTR2, SSTR3, SSTR4, SSTR5, respectively. Cortistatin-29 shows anti-fibrotic effects .
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- HY-P3618
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Somatostatin Receptor
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Neurological Disease
Inflammation/Immunology
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Cortistatin-29 is a neuropeptide. Cortistatin-29 alleviates neuropathic pain. Cortistatin-29 binds all somatostatin (SS) receptor subtypes with high affinity and shows IC50 values of 2.8 nM, 7.1 nM, 0.2 nM, 3.0 nM, 13.7 nM for SSTR1, SSTR2, SSTR3, SSTR4, SSTR5, respectively. Cortistatin-29 shows anti-fibrotic effects .
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- HY-108501
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Somatostatin Receptor
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Neurological Disease
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(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 .
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- HY-P3019
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CRFR
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Cardiovascular Disease
Neurological Disease
Endocrinology
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Urocortin III (human) is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III (human) preferentially binds and activates CRF-R2 and has a discrete central nervous system and peripheral distribution. Urocortin III (human) selectively binds to type 2 CRF receptors with Ki values of 13.5, 21.7, and >100 nM for mCRF2β, rCRF2α, and hCRF1, respectively. Urocortin III (human) mediates somatostatin-dependent negative feedback control of Insulin (human) (HY-P0035) secretion .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P0036
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Octreotide
Maximum Cited Publications
13 Publications Verification
SMS 201-995
|
Somatostatin Receptor
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Endocrinology
Cancer
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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 .
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- HY-106103A
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MK 678 acetate; L 36358 acetate
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Somatostatin Receptor
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Cardiovascular Disease
Neurological Disease
Metabolic Disease
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Seglitide acetate (MK 678; L 36358 acetate) is a potent, orally active somatostatin receptor 2 (SSTR2) agonist, and also a competitive antagonist of SSTR14, SSTR25, and SSTR28. Seglitide acetate has antihypertensive effects and can inhibit plasma glucagon and growth hormone. Seglitide acetate can be used for research on diabetes .
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- HY-106103
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- HY-P1335A
-
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Opioid Receptor
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Neurological Disease
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CTAP TFA is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC50 of 3.5 nM. CTAP TFA displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .
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- HY-111615A
-
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Somatostatin Receptor
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Neurological Disease
Inflammation/Immunology
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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 .
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- HY-P3954
-
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Somatostatin Receptor
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Metabolic Disease
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Somatostatin-28 (sheep, human rat mouse) is a biologically active polypeptide, synthesised in the proximal intestinal epithelial cells. Somatostatin-28 (sheep, human rat mouse) suppresses glucose-stimulated insulin secretion without affecting circulating basal insulin concentration. Somatostatin-28 (sheep, human rat mouse) also targets to somatostatin receptor subtype 5 (SSTR5) to regulate GLP-1 secretion .
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- HY-P10920
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Drug Derivative
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Cancer
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DOTAMTATE is a somatostatin analogue. DOTAMTATE marked 212Pb is promising for research of somatostatin receptor positive neuroendocrine tumors .
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- HY-P1207
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- HY-P0036B
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SMS 201-995 pamoate
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Somatostatin Receptor
Apoptosis
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Cardiovascular Disease
Inflammation/Immunology
Endocrinology
Cancer
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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 .
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- HY-P1335
-
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Opioid Receptor
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Neurological Disease
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CTAP is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC50 of 3.5 nM. CTAP displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .
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- HY-P4469
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-
- HY-P4957
-
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Somatostatin Receptor
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Others
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Octreotide dimer parallel is a dimer parallel of Octreotide. Octreotide (HY-P0036) is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue .
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- HY-P1201
-
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Somatostatin Receptor
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Cancer
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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 .
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- HY-P1201A
-
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Somatostatin Receptor
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Cancer
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Cyclosomatostatin TFA is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin TFA can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells .
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- HY-P1932A
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-
- HY-P4452
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-
- HY-P1932
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-
- HY-P0024
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DG3173; PTR-3173
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Somatostatin Receptor
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Endocrinology
Cancer
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Veldoreotide (DG3173) a somatostatin analogue, binds to and activate the somatostatin receptors (SSTR) 2, 4, and 5. Veldoreotide inhibits growth hormone (GH) secretion in adenomas compared with Octreotide (HY-P0036). Veldoreotide has the potential to be used as pain modulating agent
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-
- HY-P4100
-
|
Somatostatin Receptor
|
Others
|
Cyclic SSTR agonist octreotide is a Octreotide (HY-P0036), serving as the cyclic Somatostatin Receptor SSTR agonist .
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-
- HY-P0024A
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DG3173 TFA; PTR-3173 TFA
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Somatostatin Receptor
|
Endocrinology
Cancer
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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
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- HY-P5126
-
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Radionuclide-Drug Conjugates (RDCs)
Somatostatin Receptor
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Cancer
|
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).
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- HY-P5126A
-
|
Radionuclide-Drug Conjugates (RDCs)
Somatostatin Receptor
|
Cancer
|
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).
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- HY-P1203
-
-
- HY-P1203A
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-
- HY-108768
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SOM230 pamoate
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Somatostatin Receptor
|
Endocrinology
Cancer
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Pasireotide (SOM230) pamoate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide pamoate exhibits antisecretory, antiproliferative, and proapoptotic activity .
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- HY-P10758
-
-
- HY-16381A
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SOM230 acetate
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Somatostatin Receptor
|
Endocrinology
Cancer
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Pasireotide (SOM230) acetate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=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-16381
-
SOM230
|
Somatostatin Receptor
|
Endocrinology
Cancer
|
Pasireotide (SOM230), a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide also exhibits antisecretory, antiproliferative, and proapoptotic activity .
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-
- HY-P1212
-
CST-14 (mouse, rat)
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Somatostatin Receptor
|
Neurological Disease
|
Cortistatin 14, mouse, rat (CST-14, human, rat), a neuropeptide with neuronal depressant and sleep modulating properties, can bind to all five cloned somatostatin receptors (SSTRs) and ghrelin receptor to exert its biological activities and co-exists with GABA within the cortex and hippocampus .
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-
- HY-P3294
-
-
- HY-P1202A
-
|
Somatostatin Receptor
|
Endocrinology
|
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 .
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-
- HY-P1202
-
|
Somatostatin Receptor
|
Endocrinology
|
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 .
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-
- HY-P3958
-
-
- HY-P1206
-
|
Somatostatin Receptor
|
Neurological Disease
|
CH 275 is a peptide analog of somatostatin and binds preferably to somatostatin receptor 1 (sst1) with a Ki of 52 nM . CH 275 acts as a potent and selective sst1 agonist (IC50=30.9 nM) and also displays IC50 values of 345 nM, >1 μM, >10 μM, >10 μM for human sst3, sst4, sst2 and sst5, respectively . CH 275 can be used for the research of alzheimer’s disease .
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-
- HY-P2112
-
DOTA-Nal3-octreotide
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Radionuclide-Drug Conjugates (RDCs)
Somatostatin Receptor
|
Others
|
DOTA-NOC (DOTA-Nal3-octreotide) is a high-affinity ligand of somatostatin receptor subtypes 2, 3 and 5. DOTA-NOC can be used for labeling with various radiometals, and development of radiopeptide imaging . DOTA-NOC can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
|
-
- HY-P5128
-
Satoreotide tetraxetan
|
Radionuclide-Drug Conjugates (RDCs)
Somatostatin Receptor
|
Cancer
|
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).
|
-
- HY-103277A
-
-
- HY-103277
-
-
- HY-P0221C
-
|
PACAP Receptor
|
Endocrinology
|
PACAP (1-38) free acid is an endogenous neuropeptide. PACAP (1-38) free acid potently stimulates antral motility and somatostatin secretion, inhibits the secretion of gastrin and stimulates the release of vasoactive intestinal polypeptide, gastrin releasing peptide and substance P. PACAP (1-38) free acid also enhances N-methyl-D-aspartate receptor function and expression of brain-derived neurotrophic factor through RACK1 .
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-
- HY-P0221B
-
|
PACAP Receptor
|
Endocrinology
|
PACAP (1-38) free acid TFA is an endogenous neuropeptide. PACAP (1-38) free acid TFA potently stimulates antral motility and somatostatin secretion, inhibits the secretion of gastrin and stimulates the release of vasoactive intestinal polypeptide, gastrin releasing peptide and substance P. PACAP (1-38) free acid TFA also enhances N-methyl-D-aspartate receptor function and expression of brain-derived neurotrophic factor through RACK1 .
|
-
- HY-P2090
-
|
Somatostatin Receptor
Adenylate Cyclase
|
Cardiovascular Disease
|
Angiopeptin, a cyclic octapeptide analogue of somatostatin, is a weak sst2/sst5 receptor partial agonist with IC50 values of 0.26 nM and 6.92 nM, respectively. Angiopeptin is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin inhibits adenylate cyclase or stimulates extracellular acidification. Angiopeptin has the potential for coronary atherosclerosis research .
|
-
- HY-P2090A
-
|
Somatostatin Receptor
Adenylate Cyclase
|
Cardiovascular Disease
|
Angiopeptin TFA, a cyclic octapeptide analogue of somatostatin, is a weak sst2/sst5 receptor partial agonist with IC50 values of 0.26 nM and 6.92 nM, respectively. Angiopeptin TFA is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin TFA inhibits adenylate cyclase or stimulates extracellular acidification. Angiopeptin TFA has the potential for coronary atherosclerosis research .
|
-
- HY-P2150
-
|
Somatostatin Receptor
|
Neurological Disease
Inflammation/Immunology
|
Cortistatin-29 is a neuropeptide. Cortistatin-29 alleviates neuropathic pain. Cortistatin-29 binds all somatostatin (SS) receptor subtypes with high affinity and shows IC50 values of 2.8 nM, 7.1 nM, 0.2 nM, 3.0 nM, 13.7 nM for SSTR1, SSTR2, SSTR3, SSTR4, SSTR5, respectively. Cortistatin-29 shows anti-fibrotic effects .
|
-
- HY-P3618
-
|
Somatostatin Receptor
|
Neurological Disease
Inflammation/Immunology
|
Cortistatin-29 is a neuropeptide. Cortistatin-29 alleviates neuropathic pain. Cortistatin-29 binds all somatostatin (SS) receptor subtypes with high affinity and shows IC50 values of 2.8 nM, 7.1 nM, 0.2 nM, 3.0 nM, 13.7 nM for SSTR1, SSTR2, SSTR3, SSTR4, SSTR5, respectively. Cortistatin-29 shows anti-fibrotic effects .
|
-
- HY-P3019
-
|
CRFR
|
Cardiovascular Disease
Neurological Disease
Endocrinology
|
Urocortin III (human) is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III (human) preferentially binds and activates CRF-R2 and has a discrete central nervous system and peripheral distribution. Urocortin III (human) selectively binds to type 2 CRF receptors with Ki values of 13.5, 21.7, and >100 nM for mCRF2β, rCRF2α, and hCRF1, respectively. Urocortin III (human) mediates somatostatin-dependent negative feedback control of Insulin (human) (HY-P0035) secretion .
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- HY-P10758
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Alkynes
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Alkyne-βAG-TOCA, an octreotide derivative, targets somatostatin receptor type 2 (SST2) . Alkyne-βAG-TOCA can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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