Bombesin Receptor
The bombesin (Bn) receptor family includes the gastrin-releasing peptide (GRPR) and neuromedin B (NMBR) receptors, Bn receptor subtype 3 (BRS-3) and Bn receptor subtype 4 (BB4). Activation of these receptors mediates a wide spectrum of biological activities including important changes in the central nervous system including satiety, control of circadian rhythm, thermoregulation, and in peripheral tissues including stimulation of gastrointestinal hormone release, activation of macrophages, and effects on development. Bn-related peptides also have potent growth effects causing proliferation of bothnormal cells and various tumor cell lines.
BRS-3 is receiving increased attention, because not only is it important in a number of gastrointestinal (GI) tract and central nervous system (CNS) processes, but also because it is one of the G-protein coupling receptor families most frequently ectopically or overexpressed by a different tumors, including prostate cancer, small cell lung cancer, breast cancer, CNS tumors, and carcinoids (intestinal, thymic, and bronchial).
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Bombesin Receptor Related Products (53)
Related Products (53)
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[Tyr4]-Bombesin
![[Tyr4]-Bombesin](https://file.medchemexpress.com/product_pic/hy-w343750.gif "Click to View [Tyr4]-Bombesin Product Detail")
0 Images[Tyr4]-Bombesin is a Bombesin analogue, is a ligand of gastrin-releasing peptide receptor (GRPR).
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NOTA-P2-RM26
0 ImagesCat. No.: HY-P10896CAS No.: 1446005-10-2NOTA-P2-RM26 is an antagonist of Bombesin (HY-P0195) analogs, and the gastrin-releasing peptide receptor (GRPR/BB2) is a molecular target for prostate cancer visualization. NOTA-P2-RM26 is labeled with 111In and 68Ga for prostate cancer imaging studies using PET and SPECT/CT.
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(R)-MK-5046
0 Images(R)-MK-5046 is the isomer of MK-5046 (HY-14342), and can be used as an experimental control. MK-5046 is a potent, selective and orally active Bombesin receptor subtype-3 (BRS-3) allosteric agonist with an IC50 and an EC50 value of 27 and 25 nM for hBRS-3, respectively. MK-5046 inhibits food intake and reduces body weight of diet-induced obese (DIO) mouse models. MK-5046 can be used for the research of obesity.
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Bombesin receptor antagonist-1
0 ImagesCat. No.: HY-17674CAS No.: 204067-06-1Bombesin receptor antagonist-1 (Example 32) is a bombesin receptor antagonist with Ki values for neurotide B (NMB receptor) and gastrin-releasing peptide receptor (GRP receptor) of 0.17 and 20 nM respectively. Bombesin receptor antagonist-1 can be used to study various diseases, such as cancer, depression, and eating disorders.
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(D-Phe6,Leu-NHEt13,des-Met14)-Bombesin (6-14)
0 ImagesCat. No.: HY-P4541CAS No.: 124199-90-2(D-Phe6,Leu-NHEt13,des-Met14)-Bombesin (6-14) is a bombesin (BBN) antagonist and can be used for the research of cancer.
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GB-6
0 ImagesCat. No.: HY-P5520CAS No.: 2413262-74-3GB-6 is a short linear peptide that targets the gastrin releasing peptide receptor (GRPR). GRPR is overexpressed in pancreatic cancer. Based on the tumor selectivity and tumor-specific accumulation properties of GB-6, GB-6 labeled with near infrared (NIR) fluorescent dyes or radionuclide netium-99m (99mTc) can be used as a high-contrast imaging probe. GB-6 has excellent in vivo stability, with tumor to pancreatic and intestinal fluorescence signal ratios of 5.2 and 6.3, respectively, in SW199 0 subcutaneous xenograft models. GB-6 can rapidly target tumors and accurately delineate tumor boundaries, which has broad application prospects.
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GRPR antagonist-1
0 ImagesGRPR antagonist-1 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 4.97, 4.36 and 3.40 μM in PC3, Pan02 and HGC-27 cells, respectively). GRPR antagonist-1 inhibits HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis, with anticancer activity.
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Kuwanon H (Standard)
0 ImagesCat. No.: HY-N2600RCAS No.: 76472-87-2Kuwanon H (Standard) is the analytical standard of Kuwanon H. This product is intended for research and analytical applications. Kuwanon H is a selective non-peptide bombesin receptor antagonist and platelet activation inhibitor. Kuwanon H also acts as a specific antagonist of GRP-preferring receptors, with a Ki value of 290 nM for mouse GRP-R and 6500 nM for rat NMB-R. Kuwanon H inhibits the phosphorylation of AKT, mTOR, ERK, cPLA2 and p38, and upregulates TRIB3. It induces endoplasmic reticulum stress, apoptosis and autophagosome formation. Kuwanon H blocks calcium mobilization, mitogenic signaling, DNA synthesis, dense granule secretion, thromboxane A2 generation and integrin αIIb/β3 activity. It inhibits collagen-induced platelet aggregation and fibronectin adhesion, and delays clot retraction. Kuwanon H inhibits melanoma cell growth in vitro and in vivo, and enhances the sensitivity of melanoma cells to CDDP. It can be used in research related to melanoma, small cell lung cancer and thrombosis.
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MK-7725
0 ImagesCat. No.: HY-18612CAS No.: 1034152-93-6MK-7725 is a selective, orally active, and blood-brain barrier-permeable agonist of the subtype 3 of the frog skin peptide receptor (BRS-3). MK-7725 has a high affinity for the human BRS-3 (hBRS-3), with an IC50 of 3 nM, and its functional activity in the mouse-derived BRS-3 (mBRS-3) model with an EC50 of 22 nM (105% agonistic). MK-7725 significantly reduces the body weight of obese rats and obese dogs. MK-7725 can be used for the treatment of obesity.
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Neuromedin (B-30)
0 ImagesCat. No.: HY-P10267CAS No.: 98537-35-0Neuromedin B-30 is the neuropeptide, which is orignally isolated from porcine brain and spinal cord. , and may exhibit activity in stimulating smooth-muscle. Neuromedin B causes local vasodilation, increases vascular permeability and local hyperalgesia, thereby participating in neurogenic inflammation. Neuromedin B regulates appetite, body temperature, and behavioral responses to stress. Neuromedin B is also involved in regulating smooth muscle contraction and secretory function in the gastrointestinal tract.
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Ranatensin
0 ImagesCat. No.: HY-P1685CAS No.: 29451-71-6Ranatensin is a undecapeptide and a Bombesin Receptor angonist, can be isolated from amphibian skin, such as the frog, Rana pipiens. Ranatensin could maintain the dynamic balance of animal blood pressure, without cross-tachyphylaxis with Angiotensin amide (HY-P2212),Bradykinin (HY-P0206), or Norepinephrine (HY-13715).
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[D-Phe12,Leu14]-Bombesin
![[D-Phe12,Leu14]-Bombesin](https://file.medchemexpress.com/product_pic/hy-103287.gif "Click to View [D-Phe12,Leu14]-Bombesin Product Detail")
0 ImagesCat. No.: HY-103287CAS No.: 108437-88-3[D-Phe12,Leu14]-Bombesin is an antagonist of Bombesin Receptor. [D-Phe12,Leu14]-Bombesin can be used for the research of cancer.
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[D-Phe12]-Bombesin
![[D-Phe12]-Bombesin](https://file.medchemexpress.com/product_pic/hy-103282.gif "Click to View [D-Phe12]-Bombesin Product Detail")
0 ImagesCat. No.: HY-103282CAS No.: 108437-87-2[D-Phe12]-Bombesin is a derivative of Bombesin (HY-P0195) and an antagonist for bombesin receptor with Ki of 4.7 μM. [D-Phe12]-Bombesin inhibits the Bombesin (HY-P0195)-induced amylase release, with IC50 of 4 μM.
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PD 168368 derivative-1
0 ImagesCat. No.: HY-17673CAS No.: 216319-58-3PD 168368 derivative-1 (Compound 16) is a derivative of PD 168368 (HY-116216), with Ki values of 0.46 and 3.7 nM for the subtypes of bombesin receptor (BB₁ and BB₂). PD 168368 derivative-1 can be used for the study of various diseases, such as cancer, depression, and eating disorders.
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BRS-3 receptor agonist-2
0 ImagesCat. No.: HY-W681071CAS No.: 1021937-07-4BRS-3 receptor agonist-2 (compound 2) is a potent BRS-3 receptor agonist, with an EC50 of 2.5 nM for mouse BRS-3 receptor.
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BA 1
0 ImagesCat. No.: HY-P1423CAS No.: 183241-31-8BA 1 is a potent agonist for the bombesin (BB) family of receptors. BA 1 binds with high affinity to Bombesin receptor subtype-3 (BRS3), gastrin releasing peptide receptor (GRPR), neuromedin B receptor (NMBR) with IC50s of 6, 0.4, 2.5 nM.
