| Identification | Back Directory | [Name]
1H-1,2,4-Triazol-3-amine, 5-[4-[(2S,5S)-2-[(4-chlorophenyl)methyl]-5-methyl-4-(2-methylpropyl)-1-piperazinyl]-1-piperidinyl]- | [CAS]
2221950-65-6 | [Synonyms]
OAT-2068
1H-1,2,4-Triazol-3-amine, 5-[4-[(2S,5S)-2-[(4-chlorophenyl)methyl]-5-methyl-4-(2-methylpropyl)-1-piperazinyl]-1-piperidinyl]- | [Molecular Formula]
C23H36ClN7 | [MOL File]
2221950-65-6.mol | [Molecular Weight]
446.03 |
| Hazard Information | Back Directory | [Description]
OAT-2068 is a potent, selective, and orally bioavailable inhibitor of mouse chitotriosidase (mCHIT1). OAT-2068 displays a remarkable 143-fold mCHIT1 vs. mAMCase selectivity. OAT-2068 was found to have an excellent pharmacokinetic profile. OAT-2068 represents a highly potent and the most selective inhibitor of mCHIT1 described to date. | [Uses]
OAT-2068 is a selective, high activity and orally active inhibitor of mouse chitotriosidase (mCHIT1) (IC50=29 nM) and displays 143-fold selectivity over m AMCase (IC50=4170 nM). OAT-2068 displays a good pharmacokinetic profile and is an ideal tool to study the role of CHIT1 in biological systems, including animal models of human diseases[1]. | [in vivo]
OAT-2068 (intravenous injection; 3 mg/kg; single dose) displays a favorable pharmacokinetic profile, showing moderate plasma clearance (1.71 mg*kg/L),good volume of distribution (4.6 L/h/kg), and T1/2 (2.87 h) in female BALB/c mice[1].OAT-2068 (oral administartion; 10 mg/kg; single dose) displays a favorable pharmacokinetic profile,it is rapidly absorbed with Tmax 0.5 h and exhibited a high bioavailability of 61%, the T1/2 and the plasma clearance are 2.83 hours and 3.57 mg*kg/L, respectively[1]. | [References]
[1] Marzena Mazur, et al. Discovery of selective, orally bioavailable inhibitor of mouse chitotriosidase. Bioorg Med Chem Lett. 2018 Feb 1;28(3):310-314. DOI:10.1016/j.bmcl.2017.12.047
[2] Gleb Andryianau, et al. Benzoxazepine-Derived Selective, Orally Bioavailable Inhibitor of Human Acidic Mammalian Chitinase. ACS Med Chem Lett DOI:10.1021/acsmedchemlett.0c00092 |
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| Company Name: |
cjbscvictory
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| Tel: |
13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
| Company Name: |
InvivoChem
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| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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