ABT-384 | CAS#868623-40-9 | HSD-1 inhibitor

ABT-384
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 531380

CAS#: 868623-40-9

Description: 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

CAS# 868623-40-9

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 531380
Name: ABT-384
CAS#: 868623-40-9
Chemical Formula: C25H34F3N5O2
Exact Mass: 493.27
Molecular Weight: 493.575
Elemental Analysis: C, 60.84; H, 6.94; F, 11.55; N, 14.19; O, 6.48

Price and Availability

Size	Price	Availability
1mg	USD 90	Ready to ship
5mg	USD 350	Ready to ship
10mg	USD 550	Ready to ship
25mg	USD 1150	Ready to ship
50mg	USD 2050	Ready to ship
100mg	USD 3650	Ready to ship
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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:

Product Data:

Product Data

Certificate of Analysis:

View CoA: current batch, Lot#S21S12C14

QC Data:

View QC data: current batch, Lot#S21S12C14

Safety Data Sheet (SDS):

View Safety Data Sheet (SDS)

Instruction:

View handling instruction

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

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	0.0	0.00

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.

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

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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.

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