SML2052
LCAT activator compound A
≥98% (HPLC)
Synonym(s):
3-[[5-(Ethylthio)-1,3,4-thiadiazol-2-yl]thio]-2-pyrazinecarbonitrile, 3-[[5-(Ethylthio)-1,3,4-thiadiazol-2-yl]thio]pyrazine-2-carbonitrile, Compound A
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About This Item
Empirical Formula (Hill Notation):
C9H7N5S3
CAS Number:
Molecular Weight:
281.38
UNSPSC Code:
41106609
NACRES:
NA.77
Assay
≥98% (HPLC)
form
powder
color
white to brown
solubility
DMSO: 2 mg/mL, clear
storage temp.
−20°C
SMILES string
CCSC1=NN=C(S1)SC2=NC=CN=C2C#N
InChI
1S/C9H7N5S3/c1-2-15-8-13-14-9(17-8)16-7-6(5-10)11-3-4-12-7/h3-4H,2H2,1H3
InChI key
UBSFSJMIJHSGDZ-UHFFFAOYSA-N
Biochem/physiol Actions
LCAT activator compound A is an activator of Lecithin:cholesterol acyltransferase (LCAT) including some mutant LCATs found in Familial LCAT Deficiency (FLD). LCAT activator compound A forms a covalent hydrophobic adduct with LCAT Cys 31. The chronic treatment with LCAT activator compound A results in a significant increase in HDLc, HDL particle, size, plasma apolipoprotein A-I level, plasma cholesteryl ester to free cholesterol ratio, and a significant reduction in very low-density lipoprotein cholesterol in hamsters.
Lecithin:cholesterol acyltransferase (LCAT) including some FLD mutant LCATs
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
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Zhu Chen et al.
Metabolism: clinical and experimental, 61(4), 470-481 (2011-10-18)
The objective was to assess whether pharmacological activation of lecithin cholesterol acyltransferase (LCAT) could exert beneficial effects on lipoprotein metabolism. A putative small molecule activator (compound A) was used as a tool compound in in vitro and in vivo studies.
Lita A Freeman et al.
The Journal of pharmacology and experimental therapeutics, 362(2), 306-318 (2017-06-04)
Lecithin:cholesterol acyltransferase (LCAT) catalyzes plasma cholesteryl ester formation and is defective in familial lecithin:cholesterol acyltransferase deficiency (FLD), an autosomal recessive disorder characterized by low high-density lipoprotein, anemia, and renal disease. This study aimed to investigate the mechanism by which compound
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