grpr

PSMA/GRPR ligand 1 (compound 3) is a bispecific ligand with dual targeting capabilities for tumors that express PSMA(+) and GRPR(+).

GRPR antagonist-1 is a potent antagonist of the gastrin-releasing peptide receptor (GRPR) and displays cytotoxicity to certain cancer cells, including PC3 cells (IC50: 4.97 μM), Pan02 cells (IC50: 4.36 μM), and HGC-27 cells (IC50: 3.40 μM). It reduces Bcl-2 levels, increases Bax levels, inhibits HGC-27 cell viability, and induces apoptosis, thereby exhibiting anti-cancer effects.

GRPR antagonist-2 is a potent antagonist of the gastrin-releasing peptide receptor (GRPR) and exhibits anticancer effects with cytotoxicity to HGC-27 cells (IC50: 0.77 μM) and Pan02 cells (IC50: 2.5 μM).

GB-6, a short linear peptide that selectively binds to the gastrin releasing peptide receptor (GRPR), shows potential as a high-contrast imaging probe due to its tumor selectivity and specific accumulation. Overexpression of GRPR in pancreatic cancer enables GB-6, when labeled with near-infrared (NIR) fluorescent dyes or the radionuclide technetium-99m (99mTc), to serve as an effective agent for tumor visualization. Demonstrating excellent in vivo stability, GB-6 yields tumor to pancreatic and intestinal fluorescence signal ratios of 5.2 and 6.3, respectively, in SW1990 subcutaneous xenograft models. Its rapid tumor targeting capability and precise tumor boundary delineation signify GB-6's extensive potential for clinical applications [1].

Rimegepant (BMS 927711) is a highly potent, oral calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki value of 0.027 nM.

CGRP antagonist 1 is a potent CGRP receptor antagonist with Ki values of 35 nM and IC50 values of 57 nM, respectively.CGRP antagonist 1 can be used for the study of cardiovascular and neurovascular diseases.

Adrenomedullin (AM) (22-52), human acetate is an antagonist of calcitonin generelated peptide receptor in the hindlimb vascular bed of the cat and an adrenomedullin receptor.

Olcegepant hydrochloride (BIBN-4096 hydrochloride) is a selective calcitonin gene-related peptide 1 (CGRP1) receptor antagonist with an IC50=0.03 nM and Ki=14.4 pM.

Olcegepant (BIBN-4096) is an effective and selective non-peptide calcitonin gene-related peptide 1 (CGRP1) receptor antagonist (IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP).

Telcagepant (MK-0974) is an oral calcitonin gene-related peptide receptor (CGRP) antagonist that blocks CGRP receptors and reduces neurotransmission in the central nervous system and is used in the study of migraines and for pain relief.

ML230 is a selective ATP-binding cassette (ABC) transporter ABCG2 inhibitor. It 36-fold selective for ABCG2 over ABCB1 (EC50s: 0.13 μM and 4.65 μM, respectively).

Ubrogepant (MK-1602) is a calcitonin gene-related peptide receptor antagonist used in acute migraine treatment studies.

CGRP antagonist 7 is a potent calcitonin gene-related peptide receptor (CGRP) antagonist with a Ki value of 0.029 nM. It effectively inhibits CGRP receptor-mediated cyclic adenosine monophosphate (cAMP) production, with an IC50 value of 1.5 nM. This compound is useful in migraine research.

MK-3207 is a highly potent and orally bioavailable small molecule antagonist of the calcitonin gene-related peptide (CGRP) receptor, demonstrating an in vitro IC50 of 0.12 nM and a Ki of 0.024 nM for the human receptor with exceptional selectivity over the related human AM1, AM2, CTR, and AMY3 receptors, though it exhibits lower affinity for CGRP receptors from other species such as canine and rodent; in vitro studies confirm its potent antagonism of human and rhesus monkey CGRP receptors (K(i) = 0.024 nM), and in vivo models show it produces a concentration-dependent inhibition of dermal vasodilation, requiring plasma concentrations of 0.8 nM and 7 nM to block 50% and 90% of the blood flow increase, respectively.

SUN B8155 is a calcitonin (CT) receptor agonist that selectively mimics the biological effects of calcitonin and induces cAMP formation in cells expressing recombinant human CT receptor.

Atogepant (MK-8031) is an orally available, selective and potent calcitonin gene-related peptide receptor (CGRP) antagonist for the study of migraine.

BI-44370, a CGRP (calcitonin gene-related peptide) receptor antagonist, can be used to treat migraines and other chronic pain.

Kendomycin is a proteasome inhibitor and endothelin receptor antagonist. It induces apoptosis in lymphoma.

Tyr-α-CGRP (rat) is an N-terminally tyrosinated analog of the neuropeptide α-CGRP that induces a fall in resting tension of isolated opossum internal anal sphincter (IAS) with an EC50 value of 178 nM.

Vazegepant (Zavegepant) is an orally available and selective antagonist of the calcitonin gene-related peptide CGRP receptor for pain relief and may be used in the study of migraine.

HTL22562 is a CGRP receptor antagonist designed for the acute treatment of migraine.

MK-3207 Hydrochloride (MK-3207 HCl) is a potent CGRP receptor antagonist with IC50 and Kiof 0.12 nM and 0.022 nM, highly selective versus human AM1, AM2, CTR, and AMY3. Phase 2.

MK-8825 is a CGRP receptor antagonist.

BCTC is a potent TRPV1 antagonist that inhibits capsaicin-induced and acid-induced activation of rat TRPV1 (IC50 of 35 and 6 nM, respectively)