| Identification | Back Directory | [Name]
3-[({3-[(thiophen-2-ylcarbonyl)amino]phenyl}carbonyl)amino]benzoic acid | [CAS]
313482-91-6 | [Synonyms]
CZL80
Benzoic acid, 3-[[3-[(2-thienylcarbonyl)amino]benzoyl]amino]-
3-[({3-[(thiophen-2-ylcarbonyl)amino]phenyl}carbonyl)amino]benzoic acid | [Molecular Formula]
C19H14N2O4S | [MOL File]
313482-91-6.mol | [Molecular Weight]
366.39 |
| Chemical Properties | Back Directory | [Boiling point ]
462.4±35.0 °C(Predicted) | [density ]
1.470±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
4.05±0.10(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
CZL80, a brain-penetrable caspase-1 inhibitor with an IC50 of 0.01 μM, could be used in the study of febrile seizures and later enhanced epileptogenic susceptibility[1]. | [in vivo]
CZL80 (7.5 mg/kg, i.v., qod) markedly reduces neuronal excitability and incidence of FS generation, and, in adult mice, relieved later enhanced epileptogenic susceptibility[1].
CZL80 delayed-administration is a competent to attenuate the progressive neurological dysfunction induced by photothrombosis[2].
| Animal Model: | Male C57BL/6 mice and Caspase-1 gene knockout (Caspase-1?/?) mice weighing 23-26?g (9-10 weeks old)[2]. | | Dosage: | 10, 30?mg/kg/d, 7 days. | | Administration: | i.p. | | Result: | Rescued motor dysfunction after photothrombotic stroke in mice. |
| Animal Model: | Mice pups of caspase-1 knockout (Casp1?/?, RRID:IMSR_JAX:004947) and littermate controls (wild-type [WT], Casp1+/+)[1]. | | Dosage: | 0.0075, 0.075, 0.75 and 7.5 mg/kg (2% DMSO in saline), qod (every other day). | | Administration: | Intravenously injected. | | Result: | Reduced seizure incidence, prolonged seizure latency and increased threshold to FS generation in a dose-dependent manner. |
| [IC 50]
Caspase-1: 0.01 μM (IC50) | [References]
[1] Yangshun Tang, et al. Structure-based discovery of CZL80, a caspase-1 inhibitor with therapeutic potential for febrile seizures and later enhanced epileptogenic susceptibility. Br J Pharmacol. 2020 Aug;177(15):3519-3534. DOI:10.1111/bph.15076
[2] Ling Pan, et al. Novel Caspase-1 inhibitor CZL80 improves neurological function in mice after progressive ischemic stroke within a long therapeutic time-window. Acta Pharmacol Sin. 2022 Nov;43(11):2817-2827. DOI:10.1038/s41401-022-00913-7 |
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