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 11β-hydroxysteroid dehydrogenase type 1 inhibitor.
MedKoo Cat#: 531380
Name: ABT-384
CAS#: 868623-40-9
Chemical Formula: C25H34F3N5O2
Exact Mass: 493.2665
Molecular Weight: 493.5752
Elemental Analysis: C, 60.84; H, 6.94; F, 11.55; N, 14.19; O, 6.48
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
| 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 | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 0.0 | 0.0 |
The following data is based on the product molecular weight 493.5752 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 |
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. Review. PubMed PMID: 25931139.
2: 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. PubMed PMID: 25041811.
3: 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. PubMed PMID: 24418055.
4: 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:e295. doi: 10.1038/tp.2013.67. PubMed PMID: 23982627; PubMed Central PMCID: PMC3756293.
5: 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. PubMed PMID: 27121668.
6: 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. PubMed PMID: 23431112.
