1. Membrane Transporter/Ion Channel
  2. Calcium Channel

Mirogabalin (Synonyms: DS5565)

Cat. No.: HY-12650 Purity: 99.31%
Handling Instructions

Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS.

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

Mirogabalin Chemical Structure

Mirogabalin Chemical Structure

CAS No. : 1138245-13-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 184 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
1 mg USD 80 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 220 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 320 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
25 mg USD 600 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 940 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 1300 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS.

IC50 & Target

α2δ-1 Calcium Channel[1]

In Vitro

Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium-channel complexes in the central nervous system (CNS). In vitro experiments using membrane preparations from human and rat α2δ subunit-expressed cells show that Mirogabalin had a slower dissociation rate from α2δ-1 than α2δ-2, in particular, α2δ-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 α2δ-1 compared with Pregabalin[1]. Mirogabalin (DS-5565) is an α2δ-1 ligand being developed for pain associated with diabetic peripheral neuropathy, fibromyalgia, and postherpetic neuralgia. Mirogabalin targets α2δ-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[2].

In Vivo

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 α2δ-1 compared with Pregabalin[1].

Clinical Trial
Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.7783 mL 23.8914 mL 47.7829 mL
5 mM 0.9557 mL 4.7783 mL 9.5566 mL
10 mM 0.4778 mL 2.3891 mL 4.7783 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

209.28

Formula

C₁₂H₁₉NO₂

CAS No.

1138245-13-2

SMILES

O=C(O)C[[email protected]]1(CN)[[email protected]]2([H])C=C(CC)C[[email protected]]2([H])C1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Mirogabalin
Cat. No.:
HY-12650
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Mirogabalin

Cat. No.: HY-12650