| Bioactivity | 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]. |
| Target | IC50: 29 nM (mCHIT1); 4200 nM (mAMCase)IC50: 67 nM (hCHIT1); 1300 nM (hAMCase) |
| Invitro | OAT-2068 is a potent inhibitor developed for mAMCase (IC50=4200 nM) and mCHIT1(IC50=29 nM), which also displays activity toward hAMCase (IC50=67 nM) and hCHIT1 (IC50=1300 nM), it exhibits off-target activity toward the human ether-a-go-go-related gene (hERG)(hERG IC50=2.4 μM)[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> OAT-2068 相关抗体: |
| 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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
| CAS | 2221950-65-6 |
| Formula | C23H36ClN7 |
| Molar Mass | 446.03 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. [2]. Gleb Andryianau, et al. Benzoxazepine-Derived Selective, Orally Bioavailable Inhibitor of Human Acidic Mammalian Chitinase. ACS Med Chem Lett |
OAT-2068
CAS: 2221950-65-6 F: C23H36ClN7 W: 446.03
OAT-2068 is a selective, high activity and orally active inhibitor of mouse chitotriosidase (mCHIT1) (IC50=29 nM) and di
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