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NF157
Catalog No. T16291Cas No. 104869-26-3
NF157 significantly decreases the expression of metalloproteinase (MMP)-3, MMP-13, which can be used in the treatment of osteoarthritis (OA). NF157 is a highly selective nanomolar P2Y11 antagonist (pKi: 7.35). The IC50s are 463 nM, 1811 μM, 170 μM for P2Y11 (Ki=44.3 nM), P2Y1 (Ki=187 μM), P2Y2 (Ki=28.9 μM), respectively.
NF157
Catalog No. T16291Cas No. 104869-26-3
NF157 significantly decreases the expression of metalloproteinase (MMP)-3, MMP-13, which can be used in the treatment of osteoarthritis (OA). NF157 is a highly selective nanomolar P2Y11 antagonist (pKi: 7.35). The IC50s are 463 nM, 1811 μM, 170 μM for P2Y11 (Ki=44.3 nM), P2Y1 (Ki=187 μM), P2Y2 (Ki=28.9 μM), respectively.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | $584 | Backorder |
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Product Introduction
Bioactivity
Chemical Properties
| Description | NF157 significantly decreases the expression of metalloproteinase (MMP)-3, MMP-13, which can be used in the treatment of osteoarthritis (OA). NF157 is a highly selective nanomolar P2Y11 antagonist (pKi: 7.35). The IC50s are 463 nM, 1811 µM, 170 µM for P2Y |
| Targets&IC50 | P2Y1:1811 μM, P2Y1:187 μM(ki), P2Y2:170 μM, P2Y2:28.9 μM(ki), P2Y11:(ki)44.3 nM, P2Y11:(pki)7.35 , P2Y11:463 nM |
| In vitro | NF157 (30 and 60 μM; 24 hours) induces a significant reduction in the degradation of type II collagen in a dose-dependent manner. NF157 (30 and 60 μM; 24 hours) almost fully restores nuclear translocation of p65 triggered by TNF-α (10 ng/mL) and significantly reduces the luciferase activity of NF-κB. NF157 (60 μM) nearly fully rescues type II collagen from degradation induced by TNF-α (10 ng/mL). NF157 shows selectivity for P2Y11 over P2Y1 (>650-fold), P2Y2 (>650-fold), P2X2 (3-fold), P2X3 (8-fold), P2X4 (>22-fold), and P2X7 (>67-fold) but no selectivity over P2X1[1][2]. |
| Molecular Weight | 1437.1 |
| Formula | C49H28F2N6Na6O23S6 |
| Cas No. | 104869-26-3 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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