KR-33494

Cas No.:	1021497-97-1
Chemical Name:	Unii-nch0QD81ZR
Synonyms:	KR-33494;KR 33494;4-(2-(4-bromophenylthio)acetamido)-1-phenethyl-1H-pyrazole-3-carboxylic acid;KR-33493;NCH0QD81ZR;4-[[2-[(4-Bromophenyl)thio]acetyl]amino]-1-(2-phenylethyl)-1H-pyrazole-3-carboxylic acid;BCP19823;4-((2-(4-Bromophenylsulfanyl)acetyl)amino)-1-phenethyl-1H-pyrazole-3-carboxylic acid;4-(2-((4-bromophenyl)thio)acetamido)-1-phenethyl-1H-pyrazole-3-carboxylic acid;4-[[2-(4-b;Unii-nch0QD81ZR
SMILES:	BrC1C([H])=C([H])C(=C([H])C=1[H])SC([H])([H])C(N([H])C1C(C(=O)O[H])=NN(C=1[H])C([H])([H])C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H])=O
Formula:	C20H18BrN3O3S
M.Wt:	460.3442
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	KR-33493 is a potent inhibitor of Fas-mediated cell death (FAF1).
In Vivo:	Body weight changes of both sexes are not related to KR-33493 in all doses. In rats administrated KR-33493 for 4 weeks, no test article-related changes in any treated groups of either sex are found in hematology, serum biochemistry, and urinalysis. In dogs administrated KR-33493 for 2 weeks, red blood cell count (RBC) value in males is significantly higher at the 1000 mg/kg/day dose than that of the control group (i.e., 6.96±0.323 vs. 6.12±0.418). However, the change of RBC is recovered after the end of the administration period. The dose-normalized AUClast is not significantly different between the groups, suggesting that KR-33493 is governed by linear kinetics[1].
Animal Administration:	A total of 93 male and 93 female specific pathogen-free rats (6 weeks of age), and 16 male and 16 female beagle dogs (8 months of age) are used in this study. In a toxicokinetic study, rat blood samples (approximately 0.6 mL) are collected into tubes containing heparin from the lateral tail vein at 0, 0.5, 1, 2, 4, 8, 12, and 24 h after dosing with KR-33493 at doses of 50, 150, and 500 mg/kg/day on Day 1 and Week 4. Dog blood samples (approximately 0.6 mL) are collected into tubes containing EDTA-2K from the cephalic vein at 0, 0.5, 1, 2, 4, 6, 8, and 24 h after dosing at KR-33493 doses of 50, 250, and 1000 mg/kg/day on Day 1 and Week 2. The plasma is separated by centrifugation (approximately 132,000 g, 3 min, 4°C) and stored at approximately -80°C until analysis. The KR-33493 concentration in plasma is quantified[1].
References:	[1]. Jeong JW, et al. Subacute toxicity evaluation of KR-33493, FAF1 inhibitor for a new anti-parkinson's disease agent, after oral administration in rats and dogs. Regul Toxicol Pharmacol. 2016 Nov;81:387-396.