1. GPCR/G Protein
    Neuronal Signaling
  2. CGRP Receptor
  3. Olcegepant

Olcegepant (Synonyms: BIBN-4096; BIBN 4096BS)

Cat. No.: HY-10095 Purity: 99.65%
Handling Instructions

Olcegepant is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP.

For research use only. We do not sell to patients.

Olcegepant Chemical Structure

Olcegepant Chemical Structure

CAS No. : 204697-65-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 310 In-stock
Estimated Time of Arrival: December 31
2 mg USD 120 In-stock
Estimated Time of Arrival: December 31
5 mg USD 192 In-stock
Estimated Time of Arrival: December 31
10 mg USD 324 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1355 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of Olcegepant:

Top Publications Citing Use of Products

    Olcegepant purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2017;41(4):1457-1467.

    In terms of the p-ERK1/2 expressions, there is no significant difference between the model and the NC groups, however, rats in the model and NC groups show substantially higher p-ERK1/2 levels than those in the sham surgery group (P < 0.05). The level of p-ERK1/2 in rats in the NPY inhibitors group and CGRP inhibitors group are significantly lower compared with the model group (P < 0.05).
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Olcegepant is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP.

    IC50 & Target

    IC50: 0.03 nM (CGRP1)[1]
    Ki: 14.4 pM (hCGRP)[2]

    In Vitro

    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[1]. 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[2]. 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[3].

    In Vivo

    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[2]. 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[4]. 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].

    Molecular Weight

    869.65

    Formula

    C₃₈H₄₇Br₂N₉O₅

    CAS No.

    204697-65-4

    SMILES

    O=C1N(CC2=C(N1)C=CC=C2)C3CCN(C(N[[email protected]@H](C(N[[email protected]](C(N4CCN(C5=CC=NC=C5)CC4)=O)CCCCN)=O)CC6=CC(Br)=C(C(Br)=C6)O)=O)CC3

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (57.49 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.1499 mL 5.7494 mL 11.4989 mL
    5 mM 0.2300 mL 1.1499 mL 2.2998 mL
    10 mM 0.1150 mL 0.5749 mL 1.1499 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (2.87 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (2.87 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Kinase Assay
    [2]

    125I-hCGRP is used as the radioligand. The incubation buffer contained (in mM): Tris 50, NaCl 150, MgCl25 and EDTA 1, (ethylene diamine tetra-acetic acid) pH 7.4. Membrane homogenates are incubated for 180 min at room temperature with 50 pM 125I -hCGRP and increasing concentrations of Olcegepant (BIBN4096BS). The incubation is terminated by filtration through GF/B glass fibre filters using a cell harvester. The protein-bound radioactivity is determined in a gamma counter. The nonspecific binding is defined as radioactivity bound in the presence of 1 μM CGRP. The IC50 values are obtained by non-linear regression analysis on the basis of a one binding site model [2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [3]

    Cells are washed with phosphate-buffered saline then pre-incubated with 300 μM isobutylmethylxanthine in serum-free MEM for 30 min at 37 °C α-CGRP-(S-37) or Olcegepant (BIBN4096BS) is added and the cells are incubated for 10 min before the addition of CGRP. The incubation is continued for another 15 min, then the cells are washed with PBS and processed for cAMP determination. Maximal stimulation over basal is defined by using 100 nM CGRP. Dose–response curves are generated by using Prism[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [5]

    Rats are treated acutely with Olcegepant (0.3, 0.6, and 0.9 mg/kg, intravenously [i.v.] in a tail vein), Naratriptan (0.1 and 0.3 mg/kg subcutaneously [s.c.]), or their respective vehicle. For combined treatment, Olcegepant (0.3 mg/kg, i.v.) is administered 30 minutes before Naratriptan (0.1 mg/kg, s.c.). The doses and routes of administration are based on previous reports.
    For subchronic treatment, CCI-ION and sham-operated rats are injected twice per day for 4 days (at 10 am and 6 pm) with Olcegepant (0.6 mg/kg, i.v.) or its vehicle, starting on the 15th day after ligature. A further injection of Olcegepant (0.6 mg/kg, i.v.) or vehicle is performed at 10 am the subsequent day (19th day after ligature), just before von Frey filament testing.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.65%

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