PBT-1033

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

Hodoodo CAT#: H529024

CAS#: 648896-70-2 (HCl)

Description: PBT-1033, also known as PBT-2, is a neural protective agent potentially for the treatment of Alzheimer's disease and Huntington's Disease.

Chemical Structure

img
PBT-1033
CAS# 648896-70-2 (HCl)
Instruction

Theoretical Analysis

Hodoodo Cat#: H529024
Name: PBT-1033
CAS#: 648896-70-2 (HCl)
Chemical Formula: C12H13Cl3N2O
Exact Mass: 0.00
Molecular Weight: 307.599
Elemental Analysis: C, 46.86; H, 4.26; Cl, 34.57; N, 9.11; O, 5.20

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @hodoodo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Related CAS #: 747408-78-2 (free base)   648896-70-2 (HCl)    

Synonym: PBT-1033; PBT-2; PBT1033; PBT2; PBT 1033; PBT 2

IUPAC/Chemical Name: 5,7-dichloro-2-((dimethylamino)methyl)quinolin-8-ol hydrochloride

InChi Key: VSRSUNAZJQGYCB-UHFFFAOYSA-N

InChi Code: InChI=1S/C12H12Cl2N2O.ClH/c1-16(2)6-7-3-4-8-9(13)5-10(14)12(17)11(8)15-7;/h3-5,17H,6H2,1-2H3;1H

SMILES Code: OC1=C2N=C(CN(C)C)C=CC2=C(Cl)C=C1Cl.[H]Cl

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: >2 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).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 307.60 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

1: Huntington Study Group Reach2HD Investigators.. Safety, tolerability, and efficacy of PBT2 in Huntington's disease: a phase 2, randomised, double-blind, placebo-controlled trial. Lancet Neurol. 2015 Jan;14(1):39-47. doi: 10.1016/S1474-4422(14)70262-5. PubMed PMID: 25467848.

2: Cherny RA, Ayton S, Finkelstein DI, Bush AI, McColl G, Massa SM. PBT2 Reduces Toxicity in a C. elegans Model of polyQ Aggregation and Extends Lifespan, Reduces Striatal Atrophy and Improves Motor Performance in the R6/2 Mouse Model of Huntington's Disease. J Huntingtons Dis. 2012;1(2):211-9. doi: 10.3233/JHD-120029. PubMed PMID: 25063332.

3: Crouch PJ, Savva MS, Hung LW, Donnelly PS, Mot AI, Parker SJ, Greenough MA, Volitakis I, Adlard PA, Cherny RA, Masters CL, Bush AI, Barnham KJ, White AR. The Alzheimer's therapeutic PBT2 promotes amyloid-β degradation and GSK3 phosphorylation via a metal chaperone activity. J Neurochem. 2011 Oct;119(1):220-30. doi: 10.1111/j.1471-4159.2011.07402.x. PubMed PMID: 21797865.

4: Faux NG, Ritchie CW, Gunn A, Rembach A, Tsatsanis A, Bedo J, Harrison J, Lannfelt L, Blennow K, Zetterberg H, Ingelsson M, Masters CL, Tanzi RE, Cummings JL, Herd CM, Bush AI. PBT2 rapidly improves cognition in Alzheimer's Disease: additional phase II analyses. J Alzheimers Dis. 2010;20(2):509-16. doi: 10.3233/JAD-2010-1390. PubMed PMID: 20164561.

5: Lannfelt L, Blennow K, Zetterberg H, Batsman S, Ames D, Harrison J, Masters CL, Targum S, Bush AI, Murdoch R, Wilson J, Ritchie CW; PBT2-201-EURO study group.. Safety, efficacy, and biomarker findings of PBT2 in targeting Abeta as a modifying therapy for Alzheimer's disease: a phase IIa, double-blind, randomised, placebo-controlled trial. Lancet Neurol. 2008 Sep;7(9):779-86. doi: 10.1016/S1474-4422(08)70167-4. Erratum in: Lancet Neurol. 2009 Nov;8(11):981. PubMed PMID: 18672400.

6: Johanssen T, Suphantarida N, Donnelly PS, Liu XM, Petrou S, Hill AF, Barnham KJ. PBT2 inhibits glutamate-induced excitotoxicity in neurons through metal-mediated preconditioning. Neurobiol Dis. 2015 Sep;81:176-85. doi: 10.1016/j.nbd.2015.02.008. PubMed PMID: 25697105.

7: Relkin NR. Testing the mettle of PBT2 for Alzheimer's disease. Lancet Neurol. 2008 Sep;7(9):762-3. doi: 10.1016/S1474-4422(08)70168-6. PubMed PMID: 18672401.

8: Sampson EL, Jenagaratnam L, McShane R. Metal protein attenuating compounds for the treatment of Alzheimer's dementia. Cochrane Database Syst Rev. 2014 Feb 21;(2):CD005380. doi: 10.1002/14651858.CD005380.pub5. Review. PubMed PMID: 24563468.

9: Adlard PA, Bica L, White AR, Nurjono M, Filiz G, Crouch PJ, Donnelly PS, Cappai R, Finkelstein DI, Bush AI. Metal ionophore treatment restores dendritic spine density and synaptic protein levels in a mouse model of Alzheimer's disease. PLoS One. 2011 Mar 11;6(3):e17669. doi: 10.1371/journal.pone.0017669. PubMed PMID: 21412423; PubMed Central PMCID: PMC3055881.

10: Adlard PA, Sedjahtera A, Gunawan L, Bray L, Hare D, Lear J, Doble P, Bush AI, Finkelstein DI, Cherny RA. A novel approach to rapidly prevent age-related cognitive decline. Aging Cell. 2014 Apr;13(2):351-9. doi: 10.1111/acel.12178. PubMed PMID: 24305557; PubMed Central PMCID: PMC4331782.

11: Sampson EL, Jenagaratnam L, McShane R. Metal protein attenuating compounds for the treatment of Alzheimer's dementia. Cochrane Database Syst Rev. 2012 May 16;(5):CD005380. doi: 10.1002/14651858.CD005380.pub4. Review. Update in: Cochrane Database Syst Rev. 2014;(2):CD005380. PubMed PMID: 22592705; PubMed Central PMCID: PMC4165331.

12: Ryan TM, Roberts BR, McColl G, Hare DJ, Doble PA, Li QX, Lind M, Roberts AM, Mertens HD, Kirby N, Pham CL, Hinds MG, Adlard PA, Barnham KJ, Curtain CC, Masters CL. Stabilization of nontoxic Aβ-oligomers: insights into the mechanism of action of hydroxyquinolines in Alzheimer's disease. J Neurosci. 2015 Feb 18;35(7):2871-84. doi: 10.1523/JNEUROSCI.2912-14.2015. PubMed PMID: 25698727.

13: McColl G, Roberts BR, Pukala TL, Kenche VB, Roberts CM, Link CD, Ryan TM, Masters CL, Barnham KJ, Bush AI, Cherny RA. Utility of an improved model of amyloid-beta (Aβ₁₋₄₂) toxicity in Caenorhabditis elegans for drug screening for Alzheimer's disease. Mol Neurodegener. 2012 Nov 21;7:57. doi: 10.1186/1750-1326-7-57. PubMed PMID: 23171715; PubMed Central PMCID: PMC3519830.

14: Fu CL, Hsu LS, Liao YF, Hu MK. New Hydroxyquinoline-Based Derivatives as Potent Modulators of Amyloid-β Aggregations. Arch Pharm (Weinheim). 2016 May;349(5):327-41. doi: 10.1002/ardp.201500453. PubMed PMID: 27027880.

15: Adlard PA, Bush AI. Metal chaperones: a holistic approach to the treatment of Alzheimer's disease. Front Psychiatry. 2012 Mar 2;3:15. doi: 10.3389/fpsyt.2012.00015. PubMed PMID: 22403554; PubMed Central PMCID: PMC3291880.

16: Haigh CL, Tumpach C, Collins SJ, Drew SC. A 2-Substituted 8-Hydroxyquinoline Stimulates Neural Stem Cell Proliferation by Modulating ROS Signalling. Cell Biochem Biophys. 2016 Sep;74(3):297-306. doi: 10.1007/s12013-016-0747-4. PubMed PMID: 27329646.

17: Adlard PA, Cherny RA, Finkelstein DI, Gautier E, Robb E, Cortes M, Volitakis I, Liu X, Smith JP, Perez K, Laughton K, Li QX, Charman SA, Nicolazzo JA, Wilkins S, Deleva K, Lynch T, Kok G, Ritchie CW, Tanzi RE, Cappai R, Masters CL, Barnham KJ, Bush AI. Rapid restoration of cognition in Alzheimer's transgenic mice with 8-hydroxy quinoline analogs is associated with decreased interstitial Abeta. Neuron. 2008 Jul 10;59(1):43-55. doi: 10.1016/j.neuron.2008.06.018. PubMed PMID: 18614028.

18: Adlard PA, Parncutt J, Lal V, James S, Hare D, Doble P, Finkelstein DI, Bush AI. Metal chaperones prevent zinc-mediated cognitive decline. Neurobiol Dis. 2015 Sep;81:196-202. doi: 10.1016/j.nbd.2014.12.012. PubMed PMID: 25549871.

19: Bush AI. Drug development based on the metals hypothesis of Alzheimer's disease. J Alzheimers Dis. 2008 Oct;15(2):223-40. Review. PubMed PMID: 18953111.

20: Oliveri V, Vecchio G. 8-Hydroxyquinolines in medicinal chemistry: A structural perspective. Eur J Med Chem. 2016 Sep 14;120:252-74. doi: 10.1016/j.ejmech.2016.05.007. Review. PubMed PMID: 27191619.