2. GPCR/G Protein
  3. Bombesin Receptor

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).

Bombesin Receptor Related Products (15):

Cat. No. Product Name Effect Purity
  • HY-14342
    MK-5046 Agonist 99.67%
    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[1][2][3].
  • HY-101844
    ML-18 Antagonist 98.44%
    ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC50 of 4.8 μM.
  • HY-P0107A
    RC-3095 TFA Antagonist 98.03%
    RC-3095 TFA is a selective bombesin/gastrin releasing peptide receptor (GRPR) antagonist[1]. RC-3095 TFA exerts protective effects by reducing gastric oxidative injury in the arthritic mice[2].
  • HY-P0195
    Bombesin Modulator 99.32%
    Bombesin, a tetradecapeptide, plays an important role in the release of gastrin and the activation of G-protein receptors[1].
  • HY-103286
    PD176252 Antagonist
    PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor with Kis of 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM, 16 nM for Rat BB1 and BB2 receptors, respectively; PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells.
  • HY-P1685
    Ranatensin Antagonist
    Ranatensin 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)[1][2].
  • HY-103277
    BIM 23042 Antagonist
    BIM 23042, a certain somatostatin (SS) octapeptide analogue, is a selective neuropeptide neuromedin B receptor (NMB-R, BB1) antagonist. BIM 23042 has 100-fold lower affinity for gastrin-releasing peptide (GRP) receptor (BB2). BIM 23042 inhibits Neuromedin B (HY-P0241), ICI 216140 and DPDM-bombesin ethylamide-induced Ca2+ release[1][2][3].
  • HY-116216
    PD 168368 Antagonist
    PD 168368 is a potent, competitive, and selective neuromedin B receptor (NMB-R) antagonist with the Ki of 15–45 nM[1]. PD 168368 is neuromedin B receptor (NMBR; IC50=96 nM) / gastrin-releasing peptide receptor (GRPR IC50=3500 nM) antagonist[2]. PD 168368 also is a mixed FPR1/FPR2/FPR3 agonist with EC50s of 0.57, 0.24, and 2.7 nM, respectively[3].
  • HY-N4247
    Kuwanon G Antagonist
    Kuwanon G is a flavonoid isolated from Morus alba, acts as a bombesin receptor antagonist, with potential antimicrobial activity[1][2].
  • HY-103281
    Litorin Agonist 99.13%
    Litorin, an amphibian bombesin peptide derivative, is an bombesin receptor agonist. Litorin stimulates the contraction of smooth muscle, stimulates gastrin, gastric acid, and pancreatic secretion, and suppresses the nutriment in vivo[1][2].
  • HY-N2600
    Kuwanon H Antagonist
    Kuwanon H is a flavonoid isolated from Morus alba, which acts as a potent non-peptide bombesin receptor antagonist. Kuwanon H selectively inhibits binding of gastrin releasing peptide CRP to GRP-preferring recepotr, with a Ki value of 290 nM in cells[1].
  • HY-P1423A
    BA 1 TFA Agonist 99.43%
    BA 1 TFA is a potent agonist for the bombesin (BB) family of receptors. BA1 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[1].
  • HY-P0039
    BIM-26226 Antagonist
    BIM-26226, gastrin-releasing peptide, is a potent and selective antagonist of bombesin receptor. BIM-26226 inhibits BN- or GRP-stimulated amylase release with IC50s in the nanomolar range. BIM-26226 can be used for the research of cancer[1][2].
  • HY-P1423
    BA 1 Agonist
    BA 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[1].
  • HY-P0107
    RC-3095 Antagonist
    RC-3095 is a bombesin/gastrin releasing peptide receptor (GRPR) antagonist[1]. RC-3095 exerts protective effects by reducing gastric oxidative injury in the arthritic mice[2].