Olcegepant hydrochloride|cas: 586368-06-1

Cas No.:	586368-06-1
Synonyms:	BIBN-4096 hydrochloride; BIBN-4096BS hydrochloride; BIBN4096BS hydrochloride; BIBN 4096BS hydrochloride
SMILES:	O=C1N(CC2=C(N1)C=CC=C2)C3CCN(C(N[C@@H](C(N[C@H](C(N4CCN(C5=CC=NC=C5)CC4)=O)CCCCN)=O)CC6=CC(Br)=C(C(Br)=C6)O)=O)CC3.Cl
Formula:	C₃₈H₄₇Br₂N₉O₅^.HCl
M.Wt:	906.11
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

Olcegepant possesses higher affinity for the human CGRP receptor than the endogenous ligand CGRP and 150-fold higher affinity compared to the peptidic antagonist CGRP8-37. Olcegepant reverses CGRP-mediated vasodilation in human cerebral vessels and inhibits neurogenic vasodilation in a surrogate animal model of migraine pathophysiology. Olcegepant (BIBN4096BS) is extremely potent at primate CGRP receptors exhibiting an affinity (Ki) for human CGRP receptors of 14.4±6.3 (n=4) pM. Several lines of evidence suggest that a calcitonin-gene related peptide (CGRP) receptor antagonist may serve as a novel abortive migraine treatment. Olcegepant (BIBN4096BS) exhibits competitive antagonism at the CGRP receptor present in SK-N-MC cells. Isolated human cerebral, coronary, and omental arteries are studied with a sensitive myograph technique. CGRP induces a concentration-dependent relaxation that is antagonized by Olcegepant in a competitive manner.Olcegepant (BIBN4096BS) in doses between 1 and 30 μg/kg (i.v.) inhibits the effects of CGRP, released by stimulation of the trigeminal ganglion, on facial blood flow in marmoset monkeys. Pre-treatment with Olcegepant (900 μg/kg) inhibits the capsaicin-induced expression of Fos throughout the spinal trigeminal nucleus by 57%. In contrast, the expression of phosphorylated extracellular signal-regulated kinase in the trigeminal ganglion is not changed by Olcegepant pre-treatment. Olcegepant (0.3 to 0.9 mg/kg, i.v.) markedly reduces mechanical allodynia in CCI-ION rats. Olcegepant (0.6 mg/kg, i.v.) significantly reduces the number of c-Fos immunolabeled cells in spinal nucleus of the trigeminal nerve and upregulation of ATF3 transcript (a marker of neuron injury) but not that of interleukin-6 in trigeminal ganglion of CCI-ION rats[5].

Cat. No.	Product name	Field of application
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DC41849	Adrenomedullin (16-31), human TFA	Adrenomedullin (16-31), human TFA is amino acid residues 16-31 fragment of human adrenomedullin (hADM). Adrenomedullin has appreciable affinity for the CGRP1 receptor. Adrenomedullin (16-31), human TFA possesses pressor activity in the systemic vascular bed of the rat, but not the cat.
DC41560	PHM-27 (human)	PHM-27 (human) is a human prepro-vasoactive intestinal polypeptide (27 amino acid). PHM-27 (human) is a potent the human calcitonin receptor agonist with an EC50 of 11 nM. PHM-27 (human) efficiently enhances glucose-induced insulin secretion from beta cells by an autocrine mechanism.
DC29116	Adrenomedullin (AM) (22-52), human TFA	Adrenomedullin (AM) (22-52), human (22-52-Adrenomedullin human) TFA, an NH2 terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist. Adrenomedullin (AM) (22-52), human also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat.
DC10370	Olcegepant hydrochloride	Olcegepant hydrochloride is the first potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and with a Ki of 14.4 pM for human CGRP.
DC9397	MK-3207 (Hydrochloride)	MK-3207 is a potent and orally bioavailable CGRP receptor antagonist (IC50= 0.12 nM; Ki value= 0.024 nM); highly selective versus human AM1, AM2, CTR, and AMY3.