cgrp 1

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.

Calcitonin Gene Related Peptide (CGRP) II, rat (TFA) is a neuropeptide with 37 amino acid.

α-CGRP (human) acetate is a regulatory neuropeptide of 37 amino acids. It is the most potent vasodilator known to date and has inotropic and chronotropic effects.

β-CGRP, human acetate is one of calcitonin peptides and acts via the complex of receptor-activity-modifying protein (RAMP) and calcitonin-receptor-like receptor (CRLR) (IC50s: 1 nM and 300 nM for CRLR/RAMP1 and CRLR/RAMP2 in cells).

α-CGRP (mouse, rat) TFA, a neuropeptide belonging to the calcitonin gene-related peptide (CGRP) family, is predominantly located at neuromuscular junctions and functions as a potent vasodilator. Peripheral administration of α-CGRP (mouse, rat) TFA may result in decreased blood pressure and elevated heart rate, in addition to the relaxation of colonic smooth muscle. This compound shows promising utility in the investigation of cardiovascular, pro-inflammatory, migraine, and metabolic conditions [1] [2] [3].

AC 187 TFA, a potent and orally active amylin receptor antagonist, exhibits an IC50 of 0.48 nM and a Ki of 0.275 nM. It demonstrates greater selectivity for the amylin receptor over calcitonin and CGRP receptors and has been shown to possess neuroprotective effects [1] [2].

α-CGRP(human) TFA is a 37-amino acid regulatory neuropeptide that is extensively located within the central and peripheral nervous system, functioning as a potent vasodilator [1].

Eptinezumab, a human monoclonal antibody, specifically binds to and blocks the calcitonin gene-related peptide (CGRP) from binding to its receptor, thus acting as a preventive treatment for migraine in adults [1].

Cyclo(L-Phe-L-Val) is a metabolite of the sponge bacterium Pseudoalteromonas sp. NJ6-3-1 that can autoinduce production of antibacterial substances active against S. aureus when co-cultured at a low cell density. It induces neurite outgrowth and branching of chick cortical neurons in vitro when used at concentrations of 16 and 32 μM. It increases phosphorylation of the PI3K substrate Akt, and neurite outgrowth induced by cyclo(L-Phe-L-Val) can be blocked by the PI3K inhibitor LY294002 . Cyclo(L-Phe-L-Val) enhances axon sprouting of calcitonin gene-related protein positive (CGRP+) primary afferents in the spinal cord following crush injury and of serotonin neurons in uninjured spinal cord. Cyclo(L-Phe-L-Val) is also a bitter taste component of cocoa and roasted coffee.

Olcegepant hydrochloride is a potent and selective non-peptidethe calcitonin gene-related peptide 1 (CGRP1) receptor antagonist (with IC50 of 0.03 nM for human CGRP).

Adrenotensin (human) (Pro-ADM-153-185 (human)), a 153-185 fragment of the Adrenomedullin precursor peptide, is part of the Multifunctional Adrenomedullin (ADM). This 52-amino acid peptide, a member of the CGRP superfamily, plays a diverse role in vasodilation [1].

Calcitonin Gene-Related Peptide (CGRP) II, rat TFA, functions as a potent and enduring vasodilator by activating CGRP receptors. This compound is utilized in cardiovascular disease research [1].

Fremanezumab (TEV-48125), a humanized IgG2a monoclonal antibody, potently and selectively targets the calcitonin gene-related peptide (CGRP), a 37-amino acid neuropeptide implicated in the central and peripheral mechanisms of migraine. It holds promise for research into chronic migraine treatment [1].

α-CGRP, rat TFA, a neuropeptide (calcitonin gene-related peptide (CGRP)) mainly expressed in neuromuscular junction, is a potent vasodilator. α-CGRP, rat TFA can lead to a fall in blood pressure and an increase in heart rate by peripheral administration, also relax colonie smooth muscle. α-CGRP, rat TFA has the potential in cardiovascular, pro-inflammatory, migraine and metabolic studies [1] [2] [3] .

β-CGRP,human tissue is one of the calcitonin peptide, through complex behavior of calcitonin receptor like receptor (CRLR) - and receptor activity - modifying proteins (increased), and 1 and 300 - nM CRLR IC50s/RAMP1 and CRLR/RAMP2 cells.

MK-3207 is a potent and orally bioavailable CGRP receptor antagonist (IC 50 = 0.12 nM; K i = 0.024 nM); highly selective versus human AM1, AM2, CTR, and AMY3. IC50 Value: 0.024 nM (Ki, Human CGRP) [1] As other CGRP receptor antagonists, MK-3207 shows a lower affinity for human CGRP receptors from other species, including canine and rodent. in vitro: MK-3207 is a potent antagonist of the human and rhesus monkey CGRP receptors (K(i) = 0.024 nM). in vivo: MK-3207 produced a concentration-dependent inhibition of dermal vasodilation, with plasma concentrations of 0.8 and 7 nM required to block 50 and 90% of the blood flow increase, respectively. The tritiated analog [3H]MK-3207 was used to study the binding characteristics on the human CGRP receptor. [3H]MK-3207 displayed reversible and saturable binding (K(D) = 0.06 nM), and the off-rate was determined to be 0.012 min(-1), with a t(1/2) value of 59 min [1]. After the first interim analysis, the two lowest MK-3207 doses (2.5, 5 mg) were identified as showing insufficient efficacy. Per the pre-specified adaptive design decision rule, only the 2.5-mg group was discontinued and the five highest doses (5, 10, 20, 50, 100 mg) were continued into the second stage [2]. Clinical trial: MK-3207 for the treatment of acute migraines. Phase 2b

[Tyr22] Calcitonin Gene Related Peptide (22-37), rat, refers to a fragment (amino acids 22-37) of the rat calcitonin gene-related peptide (CGRP) that targets the CGRP receptor and adenylate cyclase. While calcitonin is primarily produced by thyroid C cells, CGRP is predominantly secreted and stored within the nervous system [1].

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).

DD04107 is a novel inhibitor of α-calcitonin gene-related peptide (α-CGRP) exocytotic release from primary sensory neurons, selectively interacting with Synaptotagmin 1.

Human β-CGRP TFA (β-CGRP, human TFA) is a calcitonin peptide that functions through interaction with the calcitonin-receptor-like receptor (CRLR) and receptor-activity-modifying protein (RAMP) complex, demonstrating IC50 values of 1 nM and 300 nM for CRLR/RAMP1 and CRLR/RAMP2, respectively, in cellular assays [1].