SSTR5
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- [2]. Shimon I, et al. Somatostatin receptor subtype specificity in human fetal pituitary cultures. Differential role of SSTR2 and SSTR5 for growth hormone, thyroid-stimulating hormone, and prolactin regulation[J]. The Journal of clinical investigation, 1997, 99(4): 789-798. [Content Brief]
- [3]. Li J, et al. Structural basis for activation of somatostatin receptor 5 by cyclic neuropeptide agonists. Proc Natl Acad Sci U S A. 2024 Jun 25;121(26):e2321710121. [Content Brief]
- [4]. Panetta R, et al. Molecular cloning, functional characterization, and chromosomal localization of a human somatostatin receptor (somatostatin receptor type 5) with preferential affinity for somatostatin-28. Mol Pharmacol. 1994;45(3):417-427. [Content Brief]
- [5]. O'Carroll AM, et al. Characterization of cloned human somatostatin receptor SSTR5. Mol Pharmacol. 1994;46(2):291-298. [Content Brief]
- [6]. Siehler S, et al. Characterisation of human recombinant somatostatin receptors. 3. Modulation of adenylate cyclase activity. Naunyn Schmiedebergs Arch Pharmacol. 1999;360(5):510-521. [Content Brief]
- [7]. Strowski MZ, et al. Somatostatin receptor subtype 5 regulates insulin secretion and glucose homeostasis. Mol Endocrinol. 2003;17(1):93-106. [Content Brief]
- [8]. Ren SG, et al. Functional association of somatostatin receptor subtypes 2 and 5 in inhibiting human growth hormone secretion. J Clin Endocrinol Metab. 2003;88(9):4239-4245. [Content Brief]
- [9]. Rohrer SP, Birzin ET, Mosley RT, Berk SC, Hutchins SM, Shen DM, et al. Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry. Science. 1998;282(5389):737-740. [Content Brief]
- [10]. Schmid HA, et al. Functional activity of the multiligand analog SOM230 at human recombinant somatostatin receptor subtypes supports its usefulness in neuroendocrine tumors. Neuroendocrinology. 2004;80 Suppl 1:47-50. [Content Brief]
- [11]. Wild D, et al. DOTA-NOC, a high-affinity ligand of somatostatin receptor subtypes 2, 3 and 5 for labelling with various radiometals. Eur J Nucl Med Mol Imaging. 2003 Oct;30(10):1338-47. [Content Brief]
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SSTR5 関連製品 (18)
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Octreotide
0 Images別名: SMS 201-995Octreotide (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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Cortistatin-14
0 ImagesCortistatin-14 is a neuropeptide that shares structural similarities with somatostatin, working by binding to somatostatin receptors (sst1-sst5). Cortistatin-14 (TFA) has anticonvulsant, neuroprotective effects, and significant anti-inflammatory properties. -
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Somatostatin-28 (sheep, human rat mouse)
0 ImagesSomatostatin-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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- BIM-23190 hydrochloride
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BIM-23056
0 ImagesBIM 23056, a linear octapeptide, is a potent sst3 and sst5 somatostatin receptor antagonist with Ki values of 10.8, 5.7, respectively. -
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SSTR5 antagonist 4
0 Images製品番号: HY-160156CAS 番号: 916338-03-9SSTR5 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. -
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SSTR5/TGR5-modulator-1
0 Images製品番号: HY-182905CAS 番号: 3069267-46-2SSTR5/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. -
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SSTR5 antagonist 7
0 Images製品番号: HY-183205CAS 番号: 1628744-37-5SSTR5 antagonist 7 is an orally active SSTR5 antagonist, with an IC50 of 6.2 nM against hSSTR5 and an IC50 of 25 nM against mouse-derived SSTR5. SSTR5 antagonist 7 exerts a sustained hypoglycemic effect. SSTR5 antagonist 7 can be used for the research of diabetes. -
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PRL 2915
0 ImagesPRL 2915 is a potent human somatostatin subtype 2 receptor (hsst2) antagonist with a Ki of 12 nM. -
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Angiopeptin TFA
0 ImagesAngiopeptin 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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Cortistatin-29 (reduced)
0 Images製品番号: HY-P3618純度: 98.12%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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PRL 3195
0 Images製品番号: HY-P4469CAS 番号: 341519-04-8PRL 3195 is a somatostatin receptor antagonist with Kis of 6, 17, 66, 1000 and 1000 nM for human somatostatin receptors (sst5, sst2, sst3, sst1 and sst4, respectively). -
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BIM-23056 TFA
0 Images製品番号: HY-P1203ACAS 番号: 1426173-61-6BIM 23056 TFA, a linear octapeptide, is a potent sst3 and sst5 somatostatin receptor antagonist with Ki values of 10.8, 5.7, respectively. -
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- BIM-23190
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Octreotide pamoate
0 Images製品番号: HY-P0036BCAS 番号: 135467-16-2別名: SMS 201-995 pamoateOctreotide (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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Angiopeptin
0 Images製品番号: HY-P2090CAS 番号: 113294-82-9Angiopeptin, 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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Cortistatin-29 (rat)
0 Images製品番号: HY-P2150CAS 番号: 1815618-17-7Cortistatin-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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AP102
0 Images製品番号: HY-P2434CAS 番号: 846569-60-6AP102 is a dual SSTR2/SSTR5-specific somatostatin analog (SSA). AP102 is a disulfide-bridged octapeptide SSA containing synthetic iodinated amino acids. AP102 binds with subnanomolar affinity to SSTR2 and SSTR5 (IC50: 0.63 and 0.65 nM, respectively). AP102 does not bind to SSTR1 or SSTR3. AP102 can be used for acromegaly and neuroendocrine tumors research. -
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