MedKoo Cat#: 531380 | Name: ABT-384
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Description:

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

ABT-384 is an inhibitor of 11β-hydroxysteroid dehydrogenase type 1, the enzyme that regenerates cortisol in several tissues. Pharmacologic effects included increases of adrenocorticotrophic hormone levels, cortisol production and androgen and estradiol levels. ABT-384 has a wide therapeutic index relative to full hepatic target engagement which is relevant for indications such as diabetes and metabolic syndrome, and one milligram of ABT-384 daily fully inhibited hepatic HSD-1 with a favorable safety profile.

Chemical Structure

ABT-384
ABT-384
CAS#868623-40-9

Theoretical Analysis

MedKoo Cat#: 531380

Name: ABT-384

CAS#: 868623-40-9

Chemical Formula: C25H34F3N5O2

Exact Mass: 493.2665

Molecular Weight: 493.58

Elemental Analysis: C, 60.84; H, 6.94; F, 11.55; N, 14.19; O, 6.48

Price and Availability

Size Price Availability Quantity
1mg USD 90.00 Ready to ship
5mg USD 350.00 Ready to ship
10mg USD 550.00 Ready to ship
25mg USD 1,150.00 Ready to ship
50mg USD 2,050.00 Ready to ship
100mg USD 3,650.00 Ready to ship
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Related CAS #
No Data
Synonym
ABT-384; ABT 384; ABT384;
IUPAC/Chemical Name
4-[[2-methyl-2-[4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl]propanoyl]amino]adamantane-1-carboxamide
InChi Key
CLHMYBJIOZXCEX-UHFFFAOYSA-N
InChi Code
InChI=1S/C25H34F3N5O2/c1-23(2,33-7-5-32(6-8-33)19-4-3-18(14-30-19)25(26,27)28)22(35)31-20-16-9-15-10-17(20)13-24(11-15,12-16)21(29)34/h3-4,14-17,20H,5-13H2,1-2H3,(H2,29,34)(H,31,35)
SMILES Code
O=C(C12CC3C(NC(C(N4CCN(C5=NC=C(C(F)(F)F)C=C5)CC4)(C)C)=O)C(C2)CC(C3)C1)N
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:
ABT-384 is a potent, selective 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor that exhibits high affinity (Ki 0.1-2.7 nM) against rodent, monkey, and human 11β-HSD1 and blocks regeneration of active cortisol.
In vitro activity:
TBD
In vivo activity:
TBD
Solvent mg/mL mM
Solubility
DMSO 0.0 0.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 493.58 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:
TBD
In vitro protocol:
TBD
In vivo protocol:
TBD
1: An G, Liu W, Dutta S. Small-molecule compounds exhibiting target-mediated drug disposition - A case example of ABT-384. J Clin Pharmacol. 2015 Oct;55(10):1079-85. doi: 10.1002/jcph.531. Epub 2015 Jun 16. PMID: 25931139. 2: Katz DA, Liu W, Locke C, Jacobson P, Barnes DM, Basu R, An G, Rieser MJ, Daszkowski D, Groves F, Heneghan G, Shah A, Gevorkyan H, Jhee SS, Ereshefsky L, Marek GJ. Peripheral and central nervous system inhibition of 11β-hydroxysteroid dehydrogenase type 1 in man by the novel inhibitor ABT-384. Transl Psychiatry. 2013 Aug 27;3(8):e295. doi: 10.1038/tp.2013.67. PMID: 23982627; PMCID: PMC3756293. 3: An G, Liu W, Katz DA, Marek G, Awni W, Dutta S. Effect of ketoconazole on the pharmacokinetics of the 11β-hydroxysteroid dehydrogenase type 1 inhibitor ABT-384 and its two active metabolites in healthy volunteers: population analysis of data from a drug-drug interaction study. Drug Metab Dispos. 2013 May;41(5):1035-45. doi: 10.1124/dmd.112.049742. Epub 2013 Feb 19. PMID: 23431112. 4: An G, Liu W, Katz DA, Marek GJ, Awni W, Dutta S. Population pharmacokinetics of the 11β-hydroxysteroid dehydrogenase type 1 inhibitor ABT-384 in healthy volunteers following single and multiple dose regimens. Biopharm Drug Dispos. 2014 Oct;35(7):417-29. doi: 10.1002/bdd.1912. Epub 2014 Aug 30. PMID: 25041811. 5: Marek GJ, Katz DA, Meier A, Greco N 4th, Zhang W, Liu W, Lenz RA. Efficacy and safety evaluation of HSD-1 inhibitor ABT-384 in Alzheimer's disease. Alzheimers Dement. 2014 Oct;10(5 Suppl):S364-73. doi: 10.1016/j.jalz.2013.09.010. Epub 2014 Jan 10. PMID: 24418055. 6: Liu W, Katz DA, Locke C, Daszkowski D, Wang Y, Rieser MJ, Awni W, Marek GJ, Dutta S. Clinical Safety, Pharmacokinetics, and Pharmacodynamics of the 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitor ABT-384 in Healthy Volunteers and Elderly Adults. Clin Pharmacol Drug Dev. 2013 Apr;2(2):133-51. doi: 10.1002/cpdd.5. Epub 2013 Feb 21. PMID: 27121668. 7: An G. Concept of Pharmacologic Target-Mediated Drug Disposition in Large- Molecule and Small-Molecule Compounds. J Clin Pharmacol. 2020 Feb;60(2):149-163. doi: 10.1002/jcph.1545. Epub 2019 Dec 2. PMID: 31793004; PMCID: PMC7472685. 8: An G, Katz DA. Importance of Target-Mediated Drug Disposition (TMDD) of Small-Molecule Compounds and Its Impact on Drug Development-Example of the Class Effect of HSD-1 Inhibitors. J Clin Pharmacol. 2023 May;63(5):526-538. doi: 10.1002/jcph.2185. Epub 2022 Dec 28. PMID: 36479709.