1609583-14-3
Chemical Structure
PF-06256142
- CAS No.: 1609583-14-3
- Formula:C21H16N4O2
- Molecular Weight:356.38
IUPAC Name: 4-(3-methyl-4-(6-methylimidazo[1,2-a]pyrazin-5-yl)phenoxy)furo[3,2-c]pyridine
InChIKey: HWAIAGZSWHOLLK-UHFFFAOYSA-N
SMILES: CC1=[C@]([C@]2=C(C)N=CC3=NC=CN32)C=CC(OC4=C(C=CO5)C5=CC=N4)=C1
Biological Activity: PF-06256142 is a potent, selective, CNS-penetrant and orally active agonist of the D1 receptor, with an EC50 and Ki of 33 nM and 12 nM, respectively. PF-06256142 has the potential for the research of schizophrenia and Parkinson's disease[1].
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PF-06256142 | 99.90% | PF-06256142 is a potent, selective, CNS-penetrant and orally active agonist of the D1 receptor, with an EC50 and Ki of 33 nM and 12 nM, respectively. PF-06256142 has the potential for the research of schizophrenia and Parkinson's disease. | ||||||||||||||||||||
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TWS119 (Standard) | ≥98% | TWS119 (Standard) is the analytical standard of TWS119. This product is intended for research and analytical applications. TWS119 is a specific inhibitor of GSK-3β, with an IC50 of 30 nM, and activates the wnt/β-catenin pathway. | ||||||||||||||||||||
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BI-9321 | BI-9321, a chemical probe, is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells. | |||||||||||||||||||||
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Tavapadon | 99.94% | Tavapadon (PF-06649751) is an orally active and highly selective dopamine D1/D5 receptor partial agonist. Tavapadon is effective in enabling movement and reducing disability and has the potential for Parkinson's disease. | ||||||||||||||||||||
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(Rac)-Tavapadon | 99.49% | (Rac)-Tavapadon ((Rac)-PF-06649751) is a potent and selective noncatechol dopamine D1 receptor agonist. (Rac)-Tavapadon displays potent full agonism in the GS activation assay as well as partial agonism in the β-arrestin2 recruitment assay (GS-cAMP, EC50=0.8 nM; β-arrestin2, EC50=68 nM). (Rac)-Tavapadon has antiparkinsonian activity. | ||||||||||||||||||||
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(Rac)-PF-06256142 | 99.59% | (Rac)-PF-06256142 is the less effective enantiomer of PF-06256142 (HY-119943). (Rac)-PF-06256142 is an agonist of D1 receptor, with an EC50 of 107 nM. (Rac)-PF-06256142 can be used for the research of schizophrenia and Parkinson's disease. | ||||||||||||||||||||
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(R)-PF-06256142 | 99.59% | (R)-PF-06256142 is the R enantiomer of PF-06256142 with low active. PF-06256142 is a potent and selective orthosteric D1 receptor agonist that can reduce receptor desensitization relative to dopamine and other catechol-containing agonists. | ||||||||||||||||||||
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PF2562 | PF2562 (Example 6), a dopamine D1 ligand, ascts as a dopamine D1 agonist or partial agonist. PF2562 binds to human D1 receptor with a Ki of 113 nM. PF2562 exhibits activity against human D1 cAMP with an EC50 of 568 nM in HTRF assay. | |||||||||||||||||||||
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PF-4211 | PF-4211 is a selective non-catechol D1R agonist with a Ki value of 2.2 μM.. PF-4211 activates adenylate cyclase by binding to D1R, thereby increasing intracellular cAMP levels. PF-4211 can be used in research related to Parkinson's disease and schizophrenia. | |||||||||||||||||||||
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Tubulin polymerization-IN-48 | Tubulin polymerization-IN-48 (Compound 4k) is a tubulin polymerization inhibitor. Tubulin polymerization-IN-48 has a moderate effect on disruption of the microtubule network. Tubulin polymerization-IN-48 inhibits neuroblastoma cancer cell proliferation, with IC50s of 79 and 165 nM for Chp-134 and Kelly cell line. | |||||||||||||||||||||
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Noncatechol agonist-1 | Noncatechol agonist-1 (19) is a Noncatechol agonist with full efficacy at both D1R-G protein and D1R-β-arrestin2 pathways, with pEC50 values of 8.41 for D1R-mediated cAMP production and 7.7 for β-arrestin2 recruitment, respectively. | |||||||||||||||||||||
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