PAT-1251 (Synonyms: PAT-1251; GB2064) |
| Katalog-Nr.GC30112 |
PAT-1251 ist ein potenter, selektiver und oral wirksamer Lysyl-Oxidase-ähnlicher 2 (LOXL2)-Inhibitor mit IC50-Werten von 0,71 bzw. 1,17 μM für hLOXL2 und hLOXL3. Es hemmt auch stark Maus-, Ratten- und Hund LOXL2 (IC50s: 0,10; 0,12 bzw. 0,16 μM). PAT-1251 wird in der Forschung zu fibrotischen Erkrankungen eingesetzt.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2007885-39-2
Sample solution is provided at 25 µL, 10mM.
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PAT-1251 is a potent, selective and oral Lysyl Oxidase-Like 2 (LOXL2) inhibitor, with IC50s of 0.71 and 1.17 μM for hLOXL2 and hLOXL3, respectively, and also potently inhibits mouse, rat, and dog LOXL2 (IC50s, 0.10, 0.12, and 0.16 μM, respectively); PAT-1251 has entered clinical development with the potential to treat a number of fibrotic diseases.
PAT-1251 is a Lysyl Oxidase-Like 2 (LOXL2) inhibitor, with IC50s of 0.71 and 1.17 μM for hLOXL2 and hLOXL3, respectively, and also potently inhibits mouse, rat, and dog LOXL2 (IC50s, 0.10, 0.12, and 0.16 μM, respectively). PAT-1251 shows highly selective for LOXL2 over other key members of the amine oxidase family, such as the copper-dependent amine oxidases semicarbazide-sensitive amine oxidase (SSAO) and diamine oxidase (DAO), in addition to the flavin-dependent monoamine oxidases A (MAO-A) and B (MAO-B), with <10% inhibition at 10 μM[1].
[1]. Rowbottom MW, et al. Identification of 4-(Aminomethyl)-6-(trifluoromethyl)-2-(phenoxy)pyridine Derivatives as Potent, Selective, and Orally Efficacious Inhibitors of the Copper-Dependent Amine Oxidase, Lysyl Oxidase-Like 2 (LOXL2). J Med Chem. 2017 May 25;60(10):4403-4423.
| Cas No. | 2007885-39-2 | SDF | |
| Überlieferungen | PAT-1251; GB2064 | ||
| Canonical SMILES | FC(F)(F)C1=NC(OC2=CC(C(N3C[C@@H](F)[C@H](O)C3)=O)=CC=C2)=CC(CN)=C1 | ||
| Formula | C18H17F4N3O3 | M.Wt | 399.34 |
| Löslichkeit | DMSO : ≥ 130 mg/mL (325.54 mM) | Storage | 4°C, 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. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5041 mL | 12.5207 mL | 25.0413 mL |
| 5 mM | 500.8 μL | 2.5041 mL | 5.0083 mL |
| 10 mM | 250.4 μL | 1.2521 mL | 2.5041 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 ddH2O, 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)
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