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Mirogabalin besylate (DS 5565 besylate)

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Mirogabalin besylate (DS 5565 besylate)
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Cat #: V25560 CAS #: 1138245-21-2 Purity ≥ 98%

Description: Mirogabalin besylate (DS-5565) is a potent, selective and orally bioavailable α2δ-1 ligand under development for treating pain associated with diabetic peripheral neuropathy, fibromyalgia, and postherpetic neuralgia.

References: Domon Y, et al. Binding Characteristics and Analgesic Effects of Mirogabalin, a Novel Ligand for the α2δ Subunit of Voltage-Gated Calcium Channels. J Pharmacol Exp Ther. 2018 Jun;365(3):573-582.

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Molecular Weight (MW)367.46
Molecular FormulaC18H25NO5S
CAS No.1138245-21-2
Synonyms DS-5565; DS 5565; DS5565; A-2000700; A2000700; A 2000700
ProtocolIn VitroMirogabalin besylate is a ligand for the α2δ subunit of voltage-gated calcium channels, with Kds of 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM for human α2δ-1, human α2δ-2, rat α2δ-1, and rat α2δ-2, respectively. Mirogabalin shows binding affinity for the gabapentin binding site in rat cortical brain homogenates with the IC50 value of 16.0 nM. Mirogabalin has no effect on any other receptors, channels, transporters, or enzymes at 50 μM
In VivoMirogabalin besylate (3 and 10 mg/kg) markedly increases AUC0-8 hours values in a dose-dependent manner in partial sciatic nerve ligation model rats. Mirogabalin (2.5, 5, and 10 mg/kg) causes significant and dose-dependent increase in AUC0-12 hours values and enhances analgesic effects, with estimated ED50 of 4.4, 3.1, and <2.5 mg/kg on day 1, day 3, and day 5, respectively. Moreover, Mirogabalin besylate shows no obvious effect on rota-rod performance and locomotor activity at 3 and 10 mg/kg via oral administration, exhibits significant inhibition on rota-rod performance at 10, 30, and 100 mg/kg, and decreases locomotor activity at 30 and 100 mg/kg in rats
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.7214 mL13.6069 mL27.2138 mL54.4277 mL
5mM0.5443 mL2.7214 mL5.4428 mL10.8855 mL
10mM0.2721 mL1.3607 mL2.7214 mL5.4428 mL
20mM0.1361 mL0.6803 mL1.3607 mL2.7214 mL
Quality Control Documentation
The molarity calculator equation
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Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
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Note:
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