| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
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| Targets |
DDR1 29 nM (IC50) DDR2 1900 nM (IC50)
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|---|---|
| ln Vitro |
In HT1080 cells overexpressing DDR1, DDR1-IN-4 (Compound 2.45) exhibits a definite dose-dependent inhibition of DDR1 phosphorylation, with more than 70% of phosphorylation inhibition at a concentration of 1 μM and selectivity over inhibition of DDR2[1].
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| ln Vivo |
Using DDR1-IN-4 (Compound 2.45, ip, 90 mg/kg) at a therapeutic dose preserves renal function and minimizes tissue damage in Col4a3–/– mice (the preclinical animal model of Alport syndrome), demonstrating the true therapeutic benefit of specifically suppressing DDR1 phosphorylation in vivo[1].
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| Animal Protocol |
Animal/Disease Models: Col4a3–/– mice, a mouse model phenocopying Alport syndrome[1].
Doses: 90 mg/kg. Route of Administration: Injected intraperitoneally (ip) daily. Experimental Results: Resulted in a significant reduction of fibrosis evaluated by Picro Sirius Red, smooth muscle actin staining, and collagen I accumulation. Dramatically reduces the levels of pDDR1 in Col4a3 knockout mice compared to controls. |
| References |
[1]. Hans Richter, et al. DNA-Encoded Library-Derived DDR1 Inhibitor Prevents Fibrosis and Renal Function Loss in a Genetic Mouse Model of Alport Syndrome. ACS Chem Biol. 2019 Jan 18;14(1):37-49.
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| Molecular Formula |
C23H20BRF3N6O3
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|---|---|
| Molecular Weight |
565.34
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| CAS # |
2125676-13-1
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| SMILES |
BrC1=CC=CC2=C1C1(C(N2CC(NCC(F)(F)F)=O)=O)CCN(C(C2C=CC3=C(C=NN3)N=2)=O)CC1
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 250 mg/mL (442.21 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.68 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.68 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7688 mL | 8.8442 mL | 17.6885 mL | |
| 5 mM | 0.3538 mL | 1.7688 mL | 3.5377 mL | |
| 10 mM | 0.1769 mL | 0.8844 mL | 1.7688 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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