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

Olcegepant hydrochloride  (Synonyms: BIBN-4096 hydrochloride; BIBN4096BS hydrochloride)

Cat. No.: HY-10095A Purity: 99.39%
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Chlorhydrate d’olcegepant (chlorhydrate de BIBN-4096) est un antagoniste non peptidique puissant et sélectif du récepteur du peptide 1 lié au gène de la calcitonine (CGRP1) avec IC50 de 0,03 nM et avec un Ki de 14,4 pM pour le CGRP humain.

Olcegepant hydrochloride (BIBN-4096 hydrochloride) is a 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.

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

Olcegepant hydrochloride Chemical Structure

Olcegepant hydrochloride Chemical Structure

CAS No. : 586368-06-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 323 In-stock
Solution
10 mM * 1 mL in DMSO USD 323 In-stock
Solid
5 mg USD 192 In-stock
10 mg USD 324 In-stock
50 mg USD 980 In-stock
100 mg USD 1560 In-stock
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Customer Review

Based on 35 publication(s) in Google Scholar

Other Forms of Olcegepant hydrochloride:

Olcegepant hydrochloride Related Antibodies

Top Publications Citing Use of Products

34 Publications Citing Use of MCE Olcegepant hydrochloride

WB

    Olcegepant hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2017;41(4):1457-1467.  [Abstract]

    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 hydrochloride (BIBN-4096 hydrochloride) is a 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[1][2].

    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].

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

    Olcegepant hydrochloride Related Antibodies
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    906.11

    Formula

    C38H47Br2N9O5.HCl
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (110.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : ≥ 66.66 mg/mL (73.57 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.1036 mL 5.5181 mL 11.0362 mL
    5 mM 0.2207 mL 1.1036 mL 2.2072 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    C2

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

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

      Solubility: ≥ 5 mg/mL (5.52 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 5 mg/mL (5.52 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.39%

    COA (252 KB) HNMR (474 KB) LCMS (94 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [2]

    125I-hCGRP is used as the radioligand. The incubation buffer contained (in mM): Tris 50, NaCl 150, MgCl2 5 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), GR-85548A (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 GR-85548A (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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 1.1036 mL 5.5181 mL 11.0362 mL 27.5905 mL
    5 mM 0.2207 mL 1.1036 mL 2.2072 mL 5.5181 mL
    10 mM 0.1104 mL 0.5518 mL 1.1036 mL 2.7590 mL
    15 mM 0.0736 mL 0.3679 mL 0.7357 mL 1.8394 mL
    20 mM 0.0552 mL 0.2759 mL 0.5518 mL 1.3795 mL
    25 mM 0.0441 mL 0.2207 mL 0.4414 mL 1.1036 mL
    30 mM 0.0368 mL 0.1839 mL 0.3679 mL 0.9197 mL
    40 mM 0.0276 mL 0.1380 mL 0.2759 mL 0.6898 mL
    50 mM 0.0221 mL 0.1104 mL 0.2207 mL 0.5518 mL
    60 mM 0.0184 mL 0.0920 mL 0.1839 mL 0.4598 mL
    DMSO 80 mM 0.0138 mL 0.0690 mL 0.1380 mL 0.3449 mL
    100 mM 0.0110 mL 0.0552 mL 0.1104 mL 0.2759 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Olcegepant586368-06-1BIBN-4096BIBN4096BSBIBN4096BIBN 4096CGRP ReceptorCalcitonin gene-related peptide receptorInhibitorinhibitorinhibit

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