Mirogabalin besylate

Product Name: Mirogabalin besylate
CAS No.: 1138245-21-2
Chemical Name: Mirogabalin besylate
Synonyms: Mirogabalin Besilate;Mirogabalin besylat;Mirogabalin besylate;Mirogabalin Besylate 10928;Milobarin ptoluenesulfonate;Linagliptin Impurity CD10126;Milo Bahrain benzenesulfonate;Mirogabalin besylate (DS-5565;MIROGABALIN BENZENESULFONIC ACID;Mirogabalin besylate (DS 5565 besylate)
CBNumber: CB73175483
Molecular Formula: C18H25NO5S
Formula Weight: 367.46
MOL File: 1138245-21-2.mol

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Mirogabalin besylate Property

storage temp.: Store at -20°C
solubility: DMSO : 125 mg/mL (340.17 mM)
form: Solid
color: White to off-white
InChI: InChI=1/C12H19NO2.C6H6O3S/c1-2-8-3-9-5-12(7-13,6-11(14)15)10(9)4-8;7-10(8,9)6-4-2-1-3-5-6/h4,9-10H,2-3,5-7,13H2,1H3,(H,14,15);1-5H,(H,7,8,9)/t9-,10-,12-;/s3
InChIKey: OKJXJRVWXYRSAN-QWGAVYBYNA-N
SMILES: S(C1C=CC=CC=1)(O)(=O)=O.C([C@]1(C[C@@]2([H])CC(CC)=C[C@@]12[H])CN)C(=O)O |&1:11,13,20,r|

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0027136
Product name: Mirogabalinbesylate
Purity: 99.98%
Packaging: 5mg
Price: $120
Updated: 2021/12/16

ChemScene

Product number: CS-0027136
Product name: Mirogabalinbesylate
Purity: 99.98%
Packaging: 10mg
Price: $190
Updated: 2021/12/16

ChemScene

Product number: CS-0027136
Product name: Mirogabalinbesylate
Purity: 99.98%
Packaging: 50mg
Price: $490
Updated: 2021/12/16

ChemScene

Product number: CS-0027136
Product name: Mirogabalinbesylate
Purity: 99.98%
Packaging: 100mg
Price: $750
Updated: 2021/12/16

DC Chemicals

Product number: DC10532
Product name: Mirogabalinbesylate
Purity: >98%
Packaging: 250mg
Price: $900
Updated: 2021/12/16

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Mirogabalin besylate Chemical Properties,Usage,Production

Description

Mirogabalin besylate (mirogabalin, Tarlige) is a gabapentinoid therapy developed by Daiichi Sankyo, which is approved in Japan for the treatment of postherpetic neuralgia and painful diabetic peripheral neuropathy. Mirogabalin has a potent pain-modulating effect with a unique high affinity and prolonged dissociation rate for the a2delta-1 subunit of voltage-gated calcium (Ca2+) channels (VGCCs) on the dorsal root ganglion resulting in more sustained analgesia compared with traditional gabapentinoids[1].

Uses

Mirogabalin besylate is an oral gabapentin analogue for the treatment of peripheral neuralgia (PNP), including diabetic PNP and postherpetic neuralgia. The drug has been approved in Japan for the treatment of PNP and has not yet received FDA approval.

brand name

Tarlige

Mechanism of action

Mirogabalin besylate selectively and potently binds to the α2δ subunit of voltage-gated calcium channels. When mirogabalin is bound, the influx of calcium ions to the presynaptic terminal is reduced, thereby inhibiting the release of excitatory neurotransmitters and providing analgesic effects.

Side effects

Mirogabalin has a superior adverse events (AEs) profile due to a rapid dissociation from the a2delta-2 subunit of VGCCs potentially implicated in central nervous system-specific AEs. The most common AEs for mirogabalin are dizziness (approximately 8-16%), somnolence (approximately 6-24%) and headache (approximately 6-14%), with a lower incidence of constipation, nausea, diarrhea, vomiting, edema, fatigue and weight gain[1].

Synthesis

Synthesis of Mirogabalin besylate

Metabolism

Mirogabalin is rapidly absorbed, and clearance is through renal excretion (approximately 80%) with approximately 20% being metabolized. Metabolism is primarily to the biologically inactive14 lactam form (A204-4455) and involves various uridine 5′-diphospho-glucuronosyltransferase (UGT) isoforms acting at the carboxylic acid moiety to produce mirogabalin acylglucuronide, which is then nonenzymatically converted to A204-4455.

References

[1] J Burgess. “Mirogabalin besylate in the treatment of neuropathic pain.” Drugs of today 56 2 (2020): 135–149.

Mirogabalin besylate Preparation Products And Raw materials

Raw materials

Preparation Products

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Mirogabalin besylate Suppliers

China 164 India 7 United States 3 Global 174

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View Lastest Price from Mirogabalin besylate manufacturers

Nanjing Dorra Pharmaceutical Technology Co., Ltd

Product: Mirogabalin Besilate 1138245-21-2
Price: US $0.00/kg
Min. Order: 1kg
Purity: 0.99
Supply Ability: 1
Release date: 2025-11-04

Taizhou Creating Bio-pharm co., ltd.

Product: Mirogabalin besilate 1138245-21-2
Price: US $0.00/KG
Min. Order: 0.10000000149011612KG
Purity: 0.99
Supply Ability: 100KGS
Release date: 2025-09-01

ZHENGZHOU JIUYI TIME NEW MATERIALS CO,.LTD

Product: Mirogabalin besylate 1138245-21-2
Price: US $2.00-5.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 100kg
Release date: 2025-06-13

1138245-21-2, Mirogabalin besylateRelated Search:

Mirogabalin besylate

Mirogabalin besylat

Mirogabalin Besilate

MIROGABALIN BENZENESULFONIC ACID

((1R,5S,6S)-6-(carboxymethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl)methanaminium benzenesulfonate

[(1R,5S,6S)-6-(Aminomethyl)-3-ethylbicyclo[3.2.0] hept-3-en-6-yl]acetic acid benzenesulfonate

2-((1R,5S,6S)-6-(aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl)acetic acid compound with benzenesulfonic acid (1:1)

Mirogabalin Besylate 10928

Mirogabalin besylate (DS 5565 besylate)

2-((1R,5S,6S)-6-(aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl)acetic acid besylate

Linagliptin Impurity CD10126

Milo Bahrain benzenesulfonate

Milobarin ptoluenesulfonate

Mirogabalin besylate (DS-5565

1138245-21-2