ABT-384 是 11β-羟基类固醇脱氢酶 1 (HSD-1) 的有效选择性抑制剂,该酶可在多种组织中再生皮质醇。
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Name | ABT-384 |
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Iupac Chemical Name | 4-[[2-methyl-2-[4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl]propanoyl]amino]adamantane-1-carboxamide |
Synonyms | ABT-384 ; ABT 384 ; ABT384 ; |
Molecular Formula | C25H34F3N5O2 |
Molecular Weight | 493.56 |
Smile | 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 |
InChiKey | CLHMYBJIOZXCEX-UHFFFAOYSA-N |
InChi | 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) |
CAS Number | 868623-40-9 |
Related CAS |
Packaging | Price | Availability | Purity | Shipping Time |
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Bulk | Enquiry | Enquiry | Enquiry |
Formulation | 类白色固体 |
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Purity | ≧98.0% |
Storage | 0-4 ℃ 可短期保存(两周);- 20 ℃ 可长期保存。 |
Solubility | 溶于DMSO |
Handling | Refer to MSDS operation |
Shipping Condition | 可在室温下运输。 |
HS Code | 2934200090 |
Targets | selective 11-β-hydroxysteroid dehydrogenase type 1 (HSD-1) inhibitor |
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Mechanism | |
Cell study | |
Animal study | |
Clinical study |
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.