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Datasheet of Mirogabalin

Description:
Mirogabalin (DS-5565) is a novel, preferentially selective 2-1 ligand characterized by high potency and selectivity to the
2-1 subunit of voltage-sensitive calcium-channel complexes in the CNS. Mirogabalin (DS-5565) is a novel, preferentially
selective 2 -1 ligand characterized by high potency and selectivity to the 2 -1 subunit of voltage-sensitive

calcium-channel complexes in the central nervous system (CNS). In vitro experiments using membrane preparations from human
and rat 2 subunit-expressed cells show that Mirogabalin had a slower dissociation rate from 2-1 than 2-2, in

particular, 2 -1 compared with Pregabalin. Additionally, Mirogabalin shows potent, sustained analgesic effects in

streptozotocin-induced diabetic rats with induces pain, and the superior analgesic effects and wider CNS safety margin relative to
Pregabalin are attributed to its selectivity for and slow dissociation from 2-1 compared with Pregabalin[1]. Mirogabalin

(DS-5565) is an 2-1 ligand being developed for pain associated with diabetic peripheral neuropathy, fibromyalgia, and
postherpetic neuralgia. Mirogabalin targets 2-1, an auxiliary protein associated with voltage-sensitive calcium channel

complexes in the central nervous system. This binding reduces calcium influx at nerve terminals, therefore reducing the release
of several pain neurotransmitters. The ED50 (on the transformed scale) for Mirogabalin is estimated to be 20.5 mg with a 90%
confidence interval (CI) of 10.1-41.7 mg. InVivo: Additionally, Mirogabalin shows potent, sustained analgesic effects in
streptozotocin-induced diabetic rats with induced pain, and the superior analgesic effects and wider central nervous system (CNS)
safety margin relative to Pregabalin are attributed to its selectivity for and slow dissociation from 2-1 compared with

Pregabalin.
Chemical Information
Catalog DC10013

Purity of current batch: >98%

Molecular Weight (MW) 209.28

Molecular Formula C12H19NO2

CAS No. 1138245-13-2

Solubility (25C) DMSO

Storage Store at -20C (desiccating conditions).

Handling:
Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in
advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable
for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room
temperature for at least 1 hour.