| Identification | Back Directory | [Name]
Setmelanotide | [CAS]
1294000-61-5 | [Synonyms]
UCB-0942
Setmelanotide
2-Pyrrolidinone, 4-(2-chloro-2,2-difluoroethyl)-1-[[2-(methoxymethyl)-6-(trifluoromethyl)imidazo[2,1-b]-1,3,4-thiadiazol-5-yl]methyl]-, (4R)- | [Molecular Formula]
C14H14ClF5N4O2S | [MOL File]
1294000-61-5.mol | [Molecular Weight]
432.8 |
| Chemical Properties | Back Directory | [density ]
1.69±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 100 mg/mL (231.05 mM);Water : < 0.1 mg/mL (insoluble) | [form ]
Solid | [pka]
-1.44±0.40(Predicted) | [color ]
White to off-white | [InChI]
InChI=1S/C14H14ClF5N4O2S/c1-26-6-9-22-24-8(11(14(18,19)20)21-12(24)27-9)5-23-4-7(2-10(23)25)3-13(15,16)17/h7H,2-6H2,1H3/t7-/m1/s1 | [InChIKey]
DCXFIOLWWRXEQH-SSDOTTSWSA-N | [SMILES]
N1(CC2N3N=C(COC)SC3=NC=2C(F)(F)F)C[C@@H](CC(Cl)(F)F)CC1=O |
| Hazard Information | Back Directory | [Uses]
Padsevonil (UCB0942) is a potent antiepileptic agent that selectively acts on presynaptic and postsynaptic targets. Padsevonil binds to synaptic vesicular protein 2 (SV2) with high affinity. Padsevonil is also a positive allosteric modulator and partial agonist of GABAAR, with high potency against α1 and α5 receptors. Padsevonil has antiepileptic effects in a variety of rodent models[1][2]. | [in vivo]
Padsevonil (0.014-181.4 mg/kg; intraperitoneal injection; single dose) has protective effects on the mouse model of acute epilepsy induced by 6Hz stimulation, acoustic stimulation and pilarine (HY-B0726A), with the ED50 values of 0.16, 0.17 and 0.19 mg/kg, respectively[2].
Padsevonil (0.14-30 mg/kg; intraperitoneal injection; single dose) has a protective effect in a rodent model of chronic epilepsy [2]. | Animal Model: | Kainate treated male C57BL/6 mice[2] | | Dosage: | 1, 3, 10 and 30 mg/kg | | Administration: | Intraperitoneal injection (i.p.); single dose | | Result: | Significantly decreased the number of hippocampal paroxysmal discharges in dose-dependent manner.
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| Animal Model: | Platinum electrodes treated male Wistar rats[2] | | Dosage: | 0.14, 0.43, 1.38 and 4.33 mg/kg | | Administration: | Intraperitoneal injection (i.p.); single dose | | Result: | Produced dose-related suppression in the cumulative duration of spontaneous spike and wave discharges, and the suppression was almost complete at a dose of 4.33 mg/kg.
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| [storage]
Store at -20°C | [References]
[1] Niespodziany I, et al. Functional characterization of the antiepileptic drug candidate, padsevonil, on GABAA receptors. Epilepsia. 2020 May;61(5):914-923. DOI:10.1111/epi.16497
[2] Leclercq K, et al. Pharmacological Profile of the Novel Antiepileptic Drug Candidate Padsevonil: Characterization in Rodent Seizure and Epilepsy Models. J Pharmacol Exp Ther. 2020 Jan;372(1):11-20. DOI:10.1124/jpet.119.261222 |
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