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Olcegepant hydrochloride (BIBN-4096 hydrochloride) is a selective calcitonin gene-related peptide 1 (CGRP1) receptor antagonist with an IC50=0.03 nM and Ki=14.4 pM.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $107 | Inquiry | Inquiry |
| Description | Olcegepant hydrochloride (BIBN-4096 hydrochloride) is a selective calcitonin gene-related peptide 1 (CGRP1) receptor antagonist with an IC50=0.03 nM and Ki=14.4 pM. |
| Targets&IC50 | CGRP:0.03 nM |
| In vitro | Olcegepant hydrochloride shows high binding affinity to human CGRP receptors (IC₅₀ = 0.03 nM) and pure antagonist behavior (pA₂ = 11.1) in SK-N-MC cells[1]. |
| In vivo | In Wistar rats, Olcegepant hydrochloride (900 μg/kg, i.v.) reduced capsaicin-induced Fos expression in the spinal trigeminal nucleus by 57%, with no effect on trigeminal ganglion pERK, indicating a central site of CGRP receptor inhibition[4]. |
| Synonyms | BIBN4096BS hydrochloride, BIBN-4096 hydrochloride, BIBN4096 hydrochloride, BIBN 4096BS hydrochloride |
| Molecular Weight | 906.11 |
| Formula | C38H48Br2ClN9O5 |
| Cas No. | 586368-06-1 |
| Smiles | O=C1N(CC=2C(N1)=CC=CC2)C3CCN(C(N[C@H](CC4=CC(Br)=C(O)C(Br)=C4)C(N[C@H](C(=O)N5CCN(CC5)C=6C=CN=CC6)CCCCN)=O)=O)CC3.Cl |
| Relative Density. | 1.31g/cm3 |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 80 mg/mL (88.29 mM), Sonication is recommended. H2O: 50 mg/mL (55.18 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 5 mg/mL (5.52 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
H2O/DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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