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

Name: Olcegepant
Brand: MedChemExpress
SKU: HY-10095
Rating: 5.0 (36 reviews)

Cat. No.: HY-10095 Purity: 99.83%: FAQs
Data Sheet SDS COA Handling Instructions

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Olcegepant (BIBN-4096) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC₅₀ of 0.03 nM and K_i of 14.4 pM for human CGRP.

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

Olcegepant Chemical Structure

CAS No. : 204697-65-4

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10 mM * 1 mL in DMSO ready for reconstitution	USD 182	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 182	In-stock	Estimated Time of Arrival: December 31
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5 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 190	In-stock	Estimated Time of Arrival: December 31
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Based on 36 publication(s) in Google Scholar

Other Forms of Olcegepant:

Olcegepant hydrochloride In-stock

35 Publications Citing Use of MCE Olcegepant

: Olcegepant 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).

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Biological Activity
Protocol
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References
Customer Review

Description

IC₅₀ & Target

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

Cellular Effect

Cell Line	Type	Value	Description	References
SK-N-MC	IC₅₀	0.004 μM Compound: BIBN4096	Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay	[PMID: 24405707]
SK-N-MC	EC₅₀	0.026 nM Compound: 1, BIBN-4096BS	Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassay Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassay	[PMID: 24794104]

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 (K_i) 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.

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

869.65

Formula

C₃₈H₄₇Br₂N₉O₅

CAS No.

204697-65-4

Appearance

Solid

Color

White to off-white

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

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

1M HCl : 50 mg/mL (57.49 mM; ultrasonic and adjust pH to 1 with HCl)

*"≥" 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

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% Corn Oil
Solubility: ≥ 2.5 mg/mL (2.87 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 3

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (2.87 mM); Clear solution
Protocol 4

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (2.87 mM); Suspended solution; Need ultrasonic
Protocol 5

Add each solvent one by one: 1% DMSO 99% Saline
Solubility: 0.5 mg/mL (0.57 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.83%

Select Batch:

Data Sheet (282 KB) SDS (252 KB)

COA (250 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Rudolf K, et al. Development of human calcitonin gene-related peptide (CGRP) receptor antagonists. 1. Potent and selective small molecule CGRP antagonists. 1-[N2-[3,5-dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-l-lysyl]-4-(4-pyridinyl)piperazine: the first CGRP antagonist for clinical trials in acute migraine. J Med Chem. 2005 Sep 22;48(19):5921-31. [Content Brief]

[2]. Doods H, et al. Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist. Br J Pharmacol. 2000 Feb;129(3):420-3. [Content Brief]

[3]. Edvinsson L, et al. Effect of the CGRP receptor antagonist BIBN4096BS in human cerebral, coronary and omentalarteries and in SK-N-MC cells. Eur J Pharmacol. 2002 Jan 2;434(1-2):49-53. [Content Brief]

[4]. Sixt ML, et al. Calcitonin gene-related peptide receptor antagonist Olcegepant acts in the spinal trigeminal nucleus. Brain. 2009 Nov;132(Pt 11):3134-41. [Content Brief]

[5]. Michot B, et al. Differential effects of calcitonin gene-related peptide receptor blockade by Olcegepant on mechanical allodynia induced by ligation of the infraorbital nerve vs the sciatic nerve in the rat. Pain. 2012 Sep;153(9):1939-48. [Content Brief]

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), 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	[1]. Rudolf K, et al. Development of human calcitonin gene-related peptide (CGRP) receptor antagonists. 1. Potent and selective small molecule CGRP antagonists. 1-[N2-[3,5-dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-l-lysyl]-4-(4-pyridinyl)piperazine: the first CGRP antagonist for clinical trials in acute migraine. J Med Chem. 2005 Sep 22;48(19):5921-31. [Content Brief] [2]. Doods H, et al. Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist. Br J Pharmacol. 2000 Feb;129(3):420-3. [Content Brief] [3]. Edvinsson L, et al. Effect of the CGRP receptor antagonist BIBN4096BS in human cerebral, coronary and omentalarteries and in SK-N-MC cells. Eur J Pharmacol. 2002 Jan 2;434(1-2):49-53. [Content Brief] [4]. Sixt ML, et al. Calcitonin gene-related peptide receptor antagonist Olcegepant acts in the spinal trigeminal nucleus. Brain. 2009 Nov;132(Pt 11):3134-41. [Content Brief] [5]. Michot B, et al. Differential effects of calcitonin gene-related peptide receptor blockade by Olcegepant on mechanical allodynia induced by ligation of the infraorbital nerve vs the sciatic nerve in the rat. Pain. 2012 Sep;153(9):1939-48. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / 1M HCl	1 mM	1.1499 mL	5.7494 mL	11.4989 mL	28.7472 mL
	5 mM	0.2300 mL	1.1499 mL	2.2998 mL	5.7494 mL
	10 mM	0.1150 mL	0.5749 mL	1.1499 mL	2.8747 mL
	15 mM	0.0767 mL	0.3833 mL	0.7666 mL	1.9165 mL
	20 mM	0.0575 mL	0.2875 mL	0.5749 mL	1.4374 mL
	25 mM	0.0460 mL	0.2300 mL	0.4600 mL	1.1499 mL
	30 mM	0.0383 mL	0.1916 mL	0.3833 mL	0.9582 mL
	40 mM	0.0287 mL	0.1437 mL	0.2875 mL	0.7187 mL
	50 mM	0.0230 mL	0.1150 mL	0.2300 mL	0.5749 mL

Olcegepant Related Classifications

Neurological Disease

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Do most proteins show cross-species activity?
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:

Olcegepant204697-65-4BIBN-4096 BIBN 4096BSBIBN4096BIBN 4096CGRP ReceptorCalcitonin gene-related peptide receptorInhibitorinhibitorinhibit

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

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Olcegepant Related Antibodies

35 Publications Citing Use of MCE Olcegepant

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Olcegepant Related Antibodies

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Complete Stock Solution Preparation Table

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