| Identification | Back Directory | [Name]
2-[(2S)-2-Methylpyrrolidin-2-yl]-1H-benimidazole-4- carboxamide hydrochloride (1:2) | [CAS]
912444-01-0 | [Synonyms]
PARP-2/1-IN-2
2-[(2S)-2-methylpyrrolidin-2-yl]-3H-benzimidazole-4-carboxamide
1H-Benzimidazole-7-carboxamide, 2-[(2S)-2-methyl-2-pyrrolidinyl]-
2- (2S)-2-Methylpyrrolidin-2-yl -1H-benimidazole-4- carboxamide hydrochloride (1
2-[(2S)-2-Methylpyrrolidin-2-yl]-1H-benimidazole-4- carboxamide hydrochloride (1:2) | [Molecular Formula]
C13H16N4O | [MDL Number]
MFCD26954827 | [MOL File]
912444-01-0.mol | [Molecular Weight]
244.29 |
| Hazard Information | Back Directory | [Uses]
PARP-2/1-IN-2 (Compound 4a), the enantiomer of Veliparib (HY-10129), is a potent PARP inhibitor with Kis of 2 and 5 nM against PARP-2 and PARP-1, respectively. PARP-2/1-IN-2 has an EC50 of 3 nM in a cell based assay of PARP activity[1]. | [in vivo]
PARP-2/1-IN-2 (Compound 4a) (25 or 50 mg/kg; i.p.) attenuates pain in Cisplatin (HY-17394) and Oxaliplatin (HY-17371)-induced neuropathy in mice[1]. | Animal Model: | Male C57BL6J mice, Cisplatin (HY-17394) and Oxaliplatin (HY-17371)-induced painful neuropathy models[1] | | Dosage: | 25 mg/kg or 50 mg/kg | | Administration: | Intraperitoneal injection, two days prior to treatment with Cisplatin or oxaliplatin, with administration continuing by i.p. injection along with the Cisplatin or oxaliplatin regimen (5 days, followed by 5 days of rest, for two weekly cycles) | | Result: | Does not attenuate Cisplatin and Oxaliplatin-induced body weight loss. Does not Affect the decline in exploratory behavior associated with Cisplatin and Oxaliplatin Treatment. Attenuates mechanical allodynia in Cisplatin and Oxaliplatin-induced neuropathy. Attenuates thermal hyperalgesia in Cisplatin-induced neuropathy. Attenuates cold hyperalgesia associated with Oxaliplatin-induced neuropathy. |
| [IC 50]
PARP2: 2 nM (Ki); PARP1: 5 nM (Ki) | [References]
[1] Ta LE, et al. A novel and selective poly (ADP-ribose) polymerase inhibitor ameliorates chemotherapy-induced painful neuropathy. PLoS One. 2013;8(1):e54161. DOI:10.1371/journal.pone.0054161 |
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