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Chemical Structure| 1138245-13-2 Chemical Structure| 1138245-13-2

Structure of Mirogabalin
CAS No.: 1138245-13-2

Chemical Structure| 1138245-13-2

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Mirogabalin is a 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.

Synonyms: DS5565

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Product Details of Mirogabalin

CAS No. :1138245-13-2
Formula : C12H19NO2
M.W : 209.28
SMILES Code : O=C(O)C[C@]1(CN)[C@]2([H])C=C(CC)C[C@]2([H])C1
Synonyms :
DS5565
MDL No. :MFCD28411425
InChI Key :FTBQORVNHOIASH-CKYFFXLPSA-N
Pubchem ID :59509752

Safety of Mirogabalin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
pituitary tumor GH3 cells 0.3-100 μM 30 ms Mirogabalin suppressed the peak (transient, INa(T)) and sustained (late, INa(L)) components of the voltage-gated Na+ current (INa) in a concentration-dependent manner, with IC50 values of 19.5 and 7.3 μM, respectively. Int J Mol Sci. 2022 Mar 31;23(7):3845

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NC/Nga mice Spontaneous atopic dermatitis model Oral 10 mg/kg Single administration, observed for 12 hours Mirogabalin significantly inhibited spontaneous scratching behavior in AD mice without affecting motor function in healthy mice Front Pharmacol. 2024 Jun 26;15:1382281
Female Sprague Dawley rats Tear-deficient dry-eye rat model Oral 10 mg/kg or 3 mg/kg 5 consecutive days Mirogabalin significantly suppressed capsaicin-induced eye-wiping behavior, indicating the suppression of ocular hyperalgesia. Administration of 10 mg/kg mirogabalin significantly reduced c-Fos expression in the trigeminal nucleus, indicating the amelioration of chronic ocular pain. Invest Ophthalmol Vis Sci. 2023 May 1;64(5):27
Mice Neuropathic pain model (chronic constriction injury of the sciatic nerve) Intraperitoneal injection 10, 20, 40 mg/kg Single injection (on day 11 post-surgery) or repeated administration (16 h and 1 h before CCI and then twice daily for 7 days) To evaluate the analgesic effects of Mirogabalin on neuropathic pain and its mechanisms. Results showed that both single and repeated administration significantly alleviated CCI-induced tactile and thermal hypersensitivity. Repeated administration also inhibited spinal microglia/macrophage activation, reduced p38MAPK levels, and decreased pronociceptive chemokines CCL2 and CCL5 levels. Pharmaceuticals (Basel). 2023 Jul 19;16(7):1023
Mice Diabetic neuropathic pain model (STZ-induced), paclitaxel-induced neuropathic pain model, oxaliplatin-induced neuropathic pain model Intraperitoneal injection 10 mg/kg and 30 mg/kg Single dose Mirogabalin significantly elevated mechanical and heat nociceptive thresholds in the STZ-induced diabetic neuropathic pain model; attenuated tactile allodynia in the paclitaxel-induced neuropathic pain model; and reduced cold-exacerbated pain in the oxaliplatin-induced neuropathic pain model. Molecules. 2023 Nov 30;28(23):7862
Mice Chronic constriction injury (CCI) model Intraperitoneal injection 1, 10, 20, 40 mg/kg Single or repeated administration (16 h and 1 h before CCI and then twice daily for 7 days) To evaluate the effect of Mirogabalin on pain-related behaviors in a mouse model of neuropathic pain, showing that Mirogabalin significantly attenuated tactile and thermal hypersensitivity. Pharmaceuticals (Basel). 2022 Jan 13;15(1):88
Mice Distal infraorbital nerve chronic constriction injury model Intraperitoneal injection 2 mg/kg Single dose To evaluate the effect of mirogabalin on neuropathic pain-related aversion, results showed that mirogabalin treatment significantly increased conditioned place preference in dIoN-CCI mice. Molecules. 2021 Apr 2;26(7):2035

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.78mL

0.96mL

0.48mL

23.89mL

4.78mL

2.39mL

47.78mL

9.56mL

4.78mL

References

 

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