ABT-288

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

MedKoo CAT#: 531378

CAS#: 948845-91-8 (free base)

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

Chemical Structure

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ABT-288
CAS# 948845-91-8 (free base)
Instruction

Theoretical Analysis

MedKoo Cat#: 531378
Name: ABT-288
CAS#: 948845-91-8 (free base)
Chemical Formula: C23H24N4O
Exact Mass: 372.20
Molecular Weight: 372.472
Elemental Analysis: C, 74.17; H, 6.49; N, 15.04; O, 4.30

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 @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Related CAS #: 948845-91-8 (free base)   948846-43-3 (tartrate)  

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

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 372.47 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:

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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.