OATD-01 |
Katalog-Nr.GC62127
One-Click Copy Product Info
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OATD-01 ist ein hochwirksamer, erster seiner Klasse, oral aktiver und selektiver Chitinase-Inhibitor mit niedriger nanomolarer AktivitÄt gegenÜber CHIT1 (hCHIT1, IC50=23 nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2088453-21-6
Sample solution is provided at 25 µL, 10mM.
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OATD-01 is a highly potent, first-in-class, orally active and selective chitinase inhibitor with low nanomolar activity toward CHIT1 (hCHIT1,IC50=23 nM). OATD-01 shows excellect PK profile in multiple species and is selectivity against a panel of other off-targets. OATD-01 exhibits significant antifibrotic efficacy in vivo and can be used for pulmonary fibrosis (IPF) research[1].
OATD-01 exhibits high affinity toward h/mCHIT1 and h/mAMCase, and the inhibitory constants (Ki) for all four enzymes are 17.3 nM, 26.05 nM, 4.8 nM and 5.7 nM, respectively[1]. These Ki values reveals good correlation with earlier established IC50 data, the IC50 values are 23 nM, 28 nM, 9 nM and 7.8 nM for hCHIT1,mCHIT1, hAMCase and mAMCase, respectively.[1].Off-target in vitro effects of compound OATD-01 have been evaluated at 10 μM in the Eurofins Panlabs panel of 98 in vitro binding and enzymatic assays, involving diverse molecular classes of proteins[1].
OATD-01 (oral gavage; 30 mg/kg, 100 mg/kg; once daily; 21 days) shows significant antifibrotic efficacy in an animal model of bleomycin-induced pulmonary fibrosis. It reduces the degree of lung fibrosis in a dose-dependent manner, ultimately achieving comparable therapeutic efficacy to reference treatment with Nintedanib in this animal model[1].
[1]. Robert Koralewski, et al. Discovery of OATD-01, a First-in-Class Chitinase Inhibitor as Potential New Therapeutics for Idiopathic Pulmonary Fibrosis. J Med Chem. 2020 Dec 24;63(24):15527-15540.
| Cas No. | 2088453-21-6 | SDF | |
| Formula | C19H27ClN6O | M.Wt | 390.91 |
| Löslichkeit | DMSO : 100 mg/mL (255.81 mM; Need ultrasonic) | Storage | Store at -20°C, protect from light, stored under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5581 mL | 12.7907 mL | 25.5813 mL |
| 5 mM | 511.6 μL | 2.5581 mL | 5.1163 mL |
| 10 mM | 255.8 μL | 1.2791 mL | 2.5581 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 5 reference(s) in Google Scholar.)