Bombesin Receptor Antagonist

PD176252 is a potent antagonist of neuromedin-B preferring (BB₁) and gastrin-releasing peptide-preferring (BB₂) receptor with K_is 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.

PD 168368 is a potent, competitive, and selective neuromedin B receptor (NMB-R) antagonist with the K_i of 15–45 nM. PD 168368 is neuromedin B receptor (NMBR; IC₅₀=96 nM) / gastrin-releasing peptide receptor (GRPR IC₅₀=3500 nM) antagonist. PD 168368 also is a mixed FPR1/FPR2/FPR3 agonist with EC₅₀s of 0.57, 0.24, and 2.7 nM, respectively.

Bombesin receptor antagonist-1 (Example 32) is a bombesin receptor antagonist with K_i 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.

PD 168368 derivative-1 (Compound 16) is a derivative of PD 168368 (HY-116216), with K_i 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.

RC-3095 TFA is a selective bombesin/gastrin releasing peptide receptor (GRPR) antagonist. RC-3095 TFA exerts protective effects by reducing gastric oxidative injury in the arthritic mice.

ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC₅₀ of 4.8 μM.

BIM-26226 is a selective gastrin-releasing peptide receptor (GRPR) (IC₅₀ = 6 nM) and bombesin receptor (BN receptor) antagonist. BIM-26226 antagonizes BN- or GRP-stimulated amylase release with IC₅₀ values of 0.3 nM and 0.2 nM, respectively. BIM-26226 is specific for the GRP-preferring BN receptor subtype with no interference with GRP receptor system. BIM-26226 can induce the synthesis of somatostatin receptor but has no significant effect on tumor growth.

Kuwanon G is a flavonoid compound and an antagonist of the bombesin receptor. Kuwanon G has multiple activities such as bactericidal, anti-tumor, anti-inflammatory, antioxidant, anti-atherosclerotic, and neuroprotective effects. Kuwanon G exhibits strong antibacterial activity against oral pathogens, especially cariogenic bacteria and periodontal pathogens. Kuwanon G can induce apoptosis and inhibit proliferation, migration, and invasion of tumor cells. Kuwanon G can be used in the research of diseases such as gastric cancer and atherosclerosis.

[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P, a Substance P derivative, is a biased agonist toward neuropeptide and chemokine receptors. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P activates G12. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P binds to IL-8 and GRP receptors. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P inhibits ERK-2 activation, activates JNK activity. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P stimulates an increase in neutrophil migration and Ca²⁺ mobilization. [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P is also a bombesin antagonist, and inhibits the growth of small cell lung cancer

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 K_i 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.

BIM 23042 TFA, 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.

RC-3095 is a bombesin/gastrin releasing peptide receptor (GRPR) antagonist. RC-3095 exerts protective effects by reducing gastric oxidative injury in the arthritic mice.

ICI 216140 is a GRP/bombesin receptor 2 antagonist with the IC₅₀ of 2 nM. ICI 216140 can reduce Bombesin (HY-P0195)-stimulated pancreatic amylase secretion and attenuates Bombesin (HY-P0195)-stimulated increases in blood pressure.

(D-Phe6,Leu-NHEt13,des-Met14)-Bombesin (6-14) is a bombesin (BBN) antagonist and can be used for the research of cancer.

Kuwanon 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 K_i 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.

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).

JMV594 (Compound RM 26) is a bombesin analogue with high affinity and antagonistic effect for gastrin releasing peptide receptor (GRPR).JMV594 can be used for the research of cancer, such as Prostate cancer.

[D-Phe12,Leu14]-Bombesin is an antagonist of Bombesin Receptor. [D-Phe12,Leu14]-Bombesin can be used for the research of cancer.

[D-Phe12]-Bombesin is a derivative of Bombesin (HY-P0195) and an antagonist for bombesin receptor with K_i of 4.7 μM. [D-Phe12]-Bombesin inhibits the Bombesin (HY-P0195)-induced amylase release, with IC₅₀ of 4 μM.

(D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P (acetate) is an antagonist for Substance P (HY-P0201) and Bombesin (HY-P0195) that has effects on ocular inflammatory responses to antidromic trigeminal nerve stimulation.