PBD-150
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 555670

CAS#: 790663-33-1

Description: PBD-150 is a potent glutaminyl cyclase (QC) inhibitor with Ki of 60 nM.


Price and Availability

Size
Price

100mg
USD 350
1g
USD 2250
Size
Price

200mg
USD 650
2g
USD 3850
Size
Price

500mg
USD 1450
5g
USD 5950

PBD-150, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 555670
Name: PBD-150
CAS#: 790663-33-1
Chemical Formula: C15H20N4O2S
Exact Mass: 320.1307
Molecular Weight: 320.411
Elemental Analysis: C, 56.23; H, 6.29; N, 17.49; O, 9.99; S, 10.01


Synonym: PBD-150; PBD 150; PBD150;

IUPAC/Chemical Name: 1-(3,4-dimethoxyphenyl)-3-(3-imidazol-1-ylpropyl)thiourea

InChi Key: FZQXMGLQANXZRP-UHFFFAOYSA-N

InChi Code: InChI=1S/C15H20N4O2S/c1-20-13-5-4-12(10-14(13)21-2)18-15(22)17-6-3-8-19-9-7-16-11-19/h4-5,7,9-11H,3,6,8H2,1-2H3,(H2,17,18,22)

SMILES Code: S=C(NCCCN1C=CN=C1)NC2=CC=C(OC)C(OC)=C2


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>3 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
2934.99.90.01


References

1: Pozzi C, Di Pisa F, Benvenuti M, Mangani S. The structure of the human glutaminyl cyclase-SEN177 complex indicates routes for developing new potent inhibitors as possible agents for the treatment of neurological disorders. J Biol Inorg Chem. 2018 Dec;23(8):1219-1226. doi: 10.1007/s00775-018-1605-1. Epub 2018 Aug 21. PubMed PMID: 30132075.

2: Brooks AF, Jackson IM, Shao X, Kropog GW, Sherman P, Quesada CA, Scott PJ. Synthesis and evaluation of [(11)C]PBD150, a radiolabeled glutaminyl cyclase inhibitor for the potential detection of Alzheimer's disease prior to amyloid β aggregation. Medchemcomm. 2015 Jun 1;6(6):1065-1068. PubMed PMID: 26101580; PubMed Central PMCID: PMC4474278.

3: Huang KF, Hsu HL, Karim S, Wang AH. Structural and functional analyses of a glutaminyl cyclase from Ixodes scapularis reveal metal-independent catalysis and inhibitor binding. Acta Crystallogr D Biol Crystallogr. 2014 Mar;70(Pt 3):789-801. doi: 10.1107/S1399004713033488. Epub 2014 Feb 22. PubMed PMID: 24598748.

4: Koch B, Buchholz M, Wermann M, Heiser U, Schilling S, Demuth HU. Probing secondary glutaminyl cyclase (QC) inhibitor interactions applying an in silico-modeling/site-directed mutagenesis approach: implications for drug development. Chem Biol Drug Des. 2012 Dec;80(6):937-46. doi: 10.1111/cbdd.12046. Epub 2012 Oct 11. PubMed PMID: 22967026.

5: Koch B, Kolenko P, Buchholz M, Carrillo DR, Parthier C, Wermann M, Rahfeld JU, Reuter G, Schilling S, Stubbs MT, Demuth HU. Crystal structures of glutaminyl cyclases (QCs) from Drosophila melanogaster reveal active site conservation between insect and mammalian QCs. Biochemistry. 2012 Sep 18;51(37):7383-92. doi: 10.1021/bi300687g. Epub 2012 Sep 5. PubMed PMID: 22897232.

6: Chen YL, Huang KF, Kuo WC, Lo YC, Lee YM, Wang AH. Inhibition of glutaminyl cyclase attenuates cell migration modulated by monocyte chemoattractant proteins. Biochem J. 2012 Mar 1;442(2):403-12. doi: 10.1042/BJ20110535. PubMed PMID: 22060158.

7: Ruiz-Carrillo D, Koch B, Parthier C, Wermann M, Dambe T, Buchholz M, Ludwig HH, Heiser U, Rahfeld JU, Stubbs MT, Schilling S, Demuth HU. Structures of glycosylated mammalian glutaminyl cyclases reveal conformational variability near the active center. Biochemistry. 2011 Jul 19;50(28):6280-8. doi: 10.1021/bi200249h. Epub 2011 Jun 27. PubMed PMID: 21671571.

8: Huang KF, Liaw SS, Huang WL, Chia CY, Lo YC, Chen YL, Wang AH. 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. doi: 10.1074/jbc.M110.208595. Epub 2011 Feb 1. PubMed PMID: 21288892; PubMed Central PMCID: PMC3069447.

9: Cynis H, Scheel E, Saido TC, Schilling S, Demuth HU. Amyloidogenic processing of amyloid precursor protein: evidence of a pivotal role of glutaminyl cyclase in generation of pyroglutamate-modified amyloid-beta. Biochemistry. 2008 Jul 15;47(28):7405-13. doi: 10.1021/bi800250p. Epub 2008 Jun 21. PubMed PMID: 18570439.