NDI-091143 |
| رقم الكتالوجGC38932 |
NDI-091143 هو مثبط لياز سيترات ATP بشري قوي وعالي التقارب (ACLY) مع IC50 من 2.1 نانومتر (اختبار ADP-Glo) ، وكي من 7.0 نانومتر و Kd 2.2 نانومتريثبط NDI-091143 تحفيز ACLY بشكل خافت ، عن طريق تثبيت التغييرات التوافقية الكبيرة في مجال السترات التي تمنع بشكل غير مباشر ربط السترات والتعرف عليها
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2375840-87-0
Sample solution is provided at 25 µL, 10mM.
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NDI-091143 is a potent and high-affinity human ATP-citrate lyase (ACLY) inhibitor with an IC50 of 2.1 nM (ADP-Glo assay), a Ki of 7.0 nM and a Kd of 2.2 nM. NDI-091143 inhibits ACLY catalysis allosterically, by stabilizing large conformational changes in the citrate domain that indirectly block the binding and recognition of citrate[1].
Thermal shift assays shows that NDI-091143 gives rise to considerable stabilization of both full-length ACLY and the N-terminal segment. The thermal shift data are consistent with limited proteolysis experiments using full-length ACLY, in which NDI-091143 together with Mg-ATP provided the greatest protection against digestion by chymotrypsin[1].
[1]. Wei J, et al. An allosteric mechanism for potent inhibition of human ATP-citrate lyase. Nature. 2019 Apr;568(7753):566-570.
| Cas No. | 2375840-87-0 | SDF | |
| Canonical SMILES | O=C(OC)C1=CC(S(=O)(NC2=CC(C3=CC=CC=C3)=C(F)C=C2F)=O)=C(O)C(Cl)=C1 | ||
| Formula | C20H14ClF2NO5S | M.Wt | 453.84 |
| الذوبان | DMSO: 125 mg/mL (275.43 mM) | Storage | Store at -20°C |
| 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 | 2.2034 mL | 11.0171 mL | 22.0342 mL |
| 5 mM | 0.4407 mL | 2.2034 mL | 4.4068 mL |
| 10 mM | 0.2203 mL | 1.1017 mL | 2.2034 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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