PBD-150|CAS 790663-33-1|DC Chemicals

Cas No.:	790663-33-1
Chemical Name:	1-(3,4-dimethoxyphenyl)-3-(3-imidazol-1-ylpropyl)thiourea
Synonyms:	PBD 150;PBD150
SMILES:	N(C1=CC=C(OC)C(OC)=C1)C(NCCCN1C=NC=C1)=S
Formula:	C₁₅H₂₀N₄O₂S
M.Wt:	320.409901618958
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	[1]. Buchholz M, et al. The first potent inhibitors for human glutaminyl cyclase: synthesis and structure-activity relationship. J Med Chem. 2006 Jan 26;49(2):664-77. [2]. DiPisa F, et al. The soluble Y115E-Y117E variant of human glutaminyl cyclase is a valid target for X-ray and NMR screening of inhibitors against Alzheimer disease. Acta Crystallogr F Struct Biol Commun. 2015 Aug;71(Pt 8):986-92. [3]. Huang KF, et al. Structures of human Golgi-resident glutaminyl cyclase and its complexes with inhibitors reveal a large loop movement upon inhibitor binding. J Biol Chem. 2011 Apr 8;286(14):12439-49.

Description:	A potent glutaminyl cyclase (QC) inhibitor with Ki of 60 nM; significantly reduces depositions of Aβ3(pGlu)-40/42 in brain in transgenic mouse models and Drosophila model of Alzheimer diseas.
In Vivo:	PBD-150 is able to reduce the deposition of pyroglutamate-modified amyloid-β peptides in brain of transgenic mouse models of Alzheimer disease, leading to a significant improvement of learning and memory in those transgenic animals[3].
References:	[1]. Buchholz M, et al. The first potent inhibitors for human glutaminyl cyclase: synthesis and structure-activity relationship. J Med Chem. 2006 Jan 26;49(2):664-77. [2]. DiPisa F, et al. The soluble Y115E-Y117E variant of human glutaminyl cyclase is a valid target for X-ray and NMR screening of inhibitors against Alzheimer disease. Acta Crystallogr F Struct Biol Commun. 2015 Aug;71(Pt 8):986-92. [3]. Huang KF, et al. Structures of human Golgi-resident glutaminyl cyclase and its complexes with inhibitors reveal a large loop movement upon inhibitor binding. J Biol Chem. 2011 Apr 8;286(14):12439-49.

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