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DDR1-IN-4 (Compound 2.45) is a highly potent inhibitor that selectively targets Discoidin Domain Receptor 1 (DDR1) autophosphorylation, demonstrating exceptional efficacy with IC50 values of 29 nM for DDR1 and 1.9 μM for DDR2.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $215 | In Stock | |
5 mg | $538 | In Stock | |
10 mg | $868 | In Stock | |
25 mg | $1,730 | In Stock | |
50 mg | $2,820 | In Stock | |
100 mg | $4,560 | In Stock |
Description | DDR1-IN-4 (Compound 2.45) is a highly potent inhibitor that selectively targets Discoidin Domain Receptor 1 (DDR1) autophosphorylation, demonstrating exceptional efficacy with IC50 values of 29 nM for DDR1 and 1.9 μM for DDR2. |
Targets&IC50 | DDR1:29 nM, DDR2:1900 nM |
In vitro | DDR1-IN-4 (Compound 2.45) exhibits dose-dependent inhibition of DDR1 phosphorylation in DDR1-overexpressing HT1080 cells, achieving over 70% inhibition at a 1 μM concentration, while maintaining selectivity against DDR2 [1]. |
In vivo | DDR1-IN-4 (Compound 2.45, ip, 90 mg/kg) maintains renal function and mitigates tissue damage in Col4a3 –/– mice, a preclinical model for Alport syndrome, through DDR1 phosphorylation inhibition. In this model, daily 90 mg/kg intraperitoneal injections reduced fibrosis, indicated by Picro Sirius Red, smooth muscle actin staining, collagen I levels, and decreased pDDR1 levels, demonstrating efficacy. |
Molecular Weight | 565.34 |
Formula | C23H20BrF3N6O3 |
Cas No. | 2125676-13-1 |
Smiles | O=C(NCC(F)(F)F)CN1C(=O)C2(C=3C(Br)=CC=CC31)CCN(C(=O)C4=NC=5C=NNC5C=C4)CC2 |
Relative Density. | no data available |
Storage | store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 200 mg/mL (353.77 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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