Olcegepant
Olcegepant
CAS: 204697-65-4
Molecular Formula: C38H47Br2N9O5
Olcegepant - Names and Identifiers
Olcegepant - Physico-chemical Properties
| Molecular Formula | C38H47Br2N9O5 |
| Molar Mass | 869.65 |
| Density | 1.497 |
| Boling Point | 1091.9±65.0 °C(Predicted) |
| pKa | 6.80±0.25(Predicted) |
| Storage Condition | -20℃ |
| Use | Olcegepant(BIBN 4096; BIBN 4096BS) is a non-peptide CGRP1 receptor selective antagonist, IC50 is 0.03 nM. |
| In vitro study | 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 (K i ) 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. |
| In vivo study | 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. |
Olcegepant - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.15 ml | 5.749 ml | 11.499 ml |
| 5 mM | 0.23 ml | 1.15 ml | 2.3 ml |
| 10 mM | 0.115 ml | 0.575 ml | 1.15 ml |
| 5 mM | 0.023 ml | 0.115 ml | 0.23 ml |
Last Update：2024-01-02 23:10:35
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