ABT-288

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

MedKoo CAT#: 531378

CAS#: 948845-91-8

Description: ABT-288 is a histamine receptor 3 (H3) antagonist potentially for the treatment of Alzhermer's disease.


Price and Availability

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ABT-288 is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 531378
Name: ABT-288
CAS#: 948845-91-8
Chemical Formula: C23H24N4O
Exact Mass: 372.195
Molecular Weight: 372.472
Elemental Analysis: C, 74.17; H, 6.49; N, 15.04; O, 4.30


Synonym: ABT-288; ABT288; ABT 288

IUPAC/Chemical Name: 2-[4-[4-[(3aR,6aR)-5-methyl-2,3,3a,4,6,6a-hexahydropyrrolo[3,2-c]pyrrol-1-yl]phenyl]phenyl]pyridazin-3-one

InChi Key: GNIRITULTPTAQW-KNQAVFIVSA-N

InChi Code: InChI=1S/C23H24N4O/c1-25-15-19-12-14-26(22(19)16-25)20-8-4-17(5-9-20)18-6-10-21(11-7-18)27-23(28)3-2-13-24-27/h2-11,13,19,22H,12,14-16H2,1H3/t19-,22+/m1/s1

SMILES Code: O=C1C=CC=NN1C2=CC=C(C3=CC=C(N4CC[C@]5([H])CN(C)C[C@@]54[H])C=C3)C=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:
>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).

Harmonized System Code:
293490


References

1: Kubo M, Kishi T, Matsunaga S, Iwata N. Histamine H3 Receptor Antagonists for Alzheimer's Disease: A Systematic Review and Meta-Analysis of Randomized Placebo-Controlled Trials. J Alzheimers Dis. 2015;48(3):667-71. doi: 10.3233/JAD-150393. Review. PubMed PMID: 26402104.

2: Haig GM, Pritchett Y, Meier A, Othman AA, Hall C, Gault LM, Lenz RA. A randomized study of H3 antagonist ABT-288 in mild-to-moderate Alzheimer's dementia. J Alzheimers Dis. 2014;42(3):959-71. doi: 10.3233/JAD-140291. PubMed PMID: 25024314.

3: Haig GM, Bain E, Robieson W, Othman AA, Baker J, Lenz RA. A randomized trial of the efficacy and safety of the H3 antagonist ABT-288 in cognitive impairment associated with schizophrenia. Schizophr Bull. 2014 Nov;40(6):1433-42. doi: 10.1093/schbul/sbt240. PubMed PMID: 24516190; PubMed Central PMCID: PMC4193706.

4: Othman AA, Haig G, Florian H, Locke C, Gertsik L, Dutta S. The H3 antagonist ABT-288 is tolerated at significantly higher exposures in subjects with schizophrenia than in healthy volunteers. Br J Clin Pharmacol. 2014 Jun;77(6):965-74. doi: 10.1111/bcp.12281. PubMed PMID: 24215171; PubMed Central PMCID: PMC4093922.

5: Hudzik TJ, Basso A, Boyce-Rustay JM, Bracken W, Browman KE, Drescher K, Esbenshade TA, Loberg LI, Lynch JJ 3rd, Brioni JD. Assessment of the abuse liability of ABT-288, a novel histamine H₃ receptor antagonist. Psychopharmacology (Berl). 2013 Jul;228(2):187-97. doi: 10.1007/s00213-013-3027-7. PubMed PMID: 23455597.

6: Othman AA, Haig G, Florian H, Locke C, Zhang J, Dutta S. Safety, tolerability and pharmacokinetics of the histamine H3 receptor antagonist, ABT-288, in healthy young adults and elderly volunteers. Br J Clin Pharmacol. 2013 May;75(5):1299-311. doi: 10.1111/j.1365-2125.2012.04472.x. PubMed PMID: 23016924; PubMed Central PMCID: PMC3635600.

7: Esbenshade TA, Browman KE, Miller TR, Krueger KM, Komater-Roderwald V, Zhang M, Fox GB, Rueter L, Robb HM, Radek RJ, Drescher KU, Fey TA, Bitner RS, Marsh K, Polakowski JS, Zhao C, Cowart MD, Hancock AA, Sullivan JP, Brioni JD. Pharmacological properties and procognitive effects of ABT-288, a potent and selective histamine H3 receptor antagonist. J Pharmacol Exp Ther. 2012 Oct;343(1):233-45. doi: 10.1124/jpet.112.194126. PubMed PMID: 22815533.

8: Brioni JD, Esbenshade TA, Garrison TR, Bitner SR, Cowart MD. Discovery of histamine H3 antagonists for the treatment of cognitive disorders and Alzheimer's disease. J Pharmacol Exp Ther. 2011 Jan;336(1):38-46. doi: 10.1124/jpet.110.166876. Review. PubMed PMID: 20864505.