IMR-1A |
رقم الكتالوجGC36304
One-Click Copy Product Info
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IMR-1A ، مستقلب الحمض لـ IMR-1 ، هو مثبط Notch مع IC 50 بمقدار 0.5 ميكرومترIMR-1A لديه زيادة في الفاعلية بمقدار 50 ضعفًا فيما يتعلق بـ IMR-1يمكن استقلاب IMR-1 في الجسم الحي إلى IMR-1A
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 331862-41-0
Sample solution is provided at 25 µL, 10mM.
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IMR-1A, a acid metabolite of IMR-1, is a Notch inhibitors with an IC50 of 0.5 μM. IMR-1A has a 50-fold increase in potency with respect to IMR-1. IMR-1 can metabolize in vivo to IMR-1A[1]. IC50: 0.5 μM (Notch)[1]
IMR-1A (2 mg/kg (i.v.) and 100 mg/kg (i.p)) exhibits low systematic plasma clearance (CL = 7 mL/min/kg) with terminal elimination half-life (T1/2) of 2.22 h following a single i.v. administration. The normal liver blood flow in mice is 90 mL/min/kg and the Vss (volume of distribution) is ~4-fold. Plasma concentrations is quantifiable up to 24 h with Tmax of 0.50 h after i.p. administration[1]. Animal Model: Male C57 BL/6 mice[1]
[1]. Astudillo L et al. The Small Molecule IMR-1 Inhibits the Notch Transcriptional Activation Complex to Suppress Tumorigenesis. Cancer Res. 2016 Jun 15;76(12):3593-603.
| Cas No. | 331862-41-0 | SDF | |
| Canonical SMILES | O=C(O)COC1=CC=C(/C=C(SC(N2)=S)\C2=O)C=C1OC | ||
| Formula | C13H11NO5S2 | M.Wt | 325.36 |
| الذوبان | DMSO: 2 mg/mL (6.15 mM); Water: < 0.1 mg/mL (insoluble) | 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. |
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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 | 3.0735 mL | 15.3676 mL | 30.7352 mL |
| 5 mM | 614.7 μL | 3.0735 mL | 6.147 mL |
| 10 mM | 307.4 μL | 1.5368 mL | 3.0735 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: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 8 reference(s) in Google Scholar.)