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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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B137236-50mg | 50mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $286.90 | |
B137236-200mg | 200mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,033.90 | |
B137236-250mg | 250mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $1,162.90 | |
B137236-1g | 1g | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $4,184.90 |
Selective PDE7 inhibitor
Specifications & Purity | Moligand™, ≥98% |
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Biochemical and Physiological Mechanisms | BRL 50481 is a potent and selective PDE7 inhibitor (IC50 = 260 nM).Selective, competitive PDE7 inhibitor (IC 50 values are 0.15 and 12.1 μm for PDE7A and PDE7B respectively). Active in vivo and in vitro . Potentiates the anti-inflammatory effect of PDE4 i |
Storage Temp | Store at 2-8°C |
Shipped In | Wet ice |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of phosphodiesterase 7A;Inhibitor of phosphodiesterase 7B |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | BRL-50481 is a selective inhibitor of phosphodiesterase 7 (PDE 7) that has acceptable selectivity for in vitro studies. Studies suggest that BRL-50481 is used to inhibit the activity of hrPDE7A1 which is usually expressed in baculovirus-infected Spodoptera frugiperda in a competitive manner. In osteoblasts, BRL-50481increases mineralization and bALP as a result of PDE7 silencing which upregulates several osteogenic genes. Further studies show that BRL-50481increases apoptosis in CLL cells via a mitochondrial-dependent process, and is associated with increased cAMP accumulation and down-regulation of the antiapoptotic protein survivin. BRL-50481 is a inhibitor of PDE7A. |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | N,N,2-trimethyl-5-nitrobenzenesulfonamide |
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INCHI | InChI=1S/C9H12N2O4S/c1-7-4-5-8(11(12)13)6-9(7)16(14,15)10(2)3/h4-6H,1-3H3 |
InChi Key | IFIUFCJFLGCQPH-UHFFFAOYSA-N |
Canonical SMILES | CC1=C(C=C(C=C1)[N+](=O)[O-])S(=O)(=O)N(C)C |
Isomeric SMILES | CC1=C(C=C(C=C1)[N+](=O)[O-])S(=O)(=O)N(C)C |
WGK Germany | 3 |
PubChem CID | 2921148 |
Molecular Weight | 244.27 |
CAS Registry No. | 433695-36-4 |
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Wikipedia | BRL-50481 |
ChEMBL Ligand | CHEMBL484928 |
PubChem CID | 2921148 |
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Sensitivity | Heat Sensitive |
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Melt Point(°C) | 73 °C |
WGK Germany | 3 |
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