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PF04191834 is a novel, potent and selective non-redox 5-lipoxygenase(5-LOX) inhibitor with an IC50 value of 229 +/- 20 nM. It inhibits 5-LOX in human blood cells with an IC80 value of 370 +/- 20 nM. It exhibits good potency in enzyme- and cell-based assays, as well as in a rat model of acute inflammation. It demonstrated approximately 300-fold selectivity for 5-LOX over 12-LOX and 15-LOX and shows no activity toward the cyclooxygenase enzymes. It is effective in inflammation and pain. Uses: Pf04191834 is effective in inflammation and pain. Synonyms: PF-04191834; PF04191834; PF 04191834; PF-4191834; PF4191834; PF 4191834. 4-(3-((4-(1-Methyl-1H-pyrazol-5-yl)phenyl)thio)phenyl)tetrahydro-2H-pyran-4-carboxamide. Grades: >98 %. CAS No. 1029317-21-2. Molecular formula: C22H23N3O2S. Mole weight: 393.51.
PF-04217903 is a potent ATP-competitive c-Met kinase inhibitor with K i of 4.8 nM for human c-Met. PF-04217903 shows more than 1,000-fold selectivity relative to 208 kinases. Antiangiogenic properties [1] [2]. Uses: Scientific research. Group: Signaling pathways. CAS No. 956905-27-4. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-12017.
PF-04217903
PF-04136309 is an orally available human chemokine receptor 2 (CCR2) antagonist with potential immunomodulating and antineoplastic activities. Upon oral administration, CCR2 antagonist PF-04136309 specifically binds to CCR2 and prevents binding of the endothelium-derived chemokine ligand CLL2 (monocyte chemoattractant protein-1 or MCP1) to its receptor CCR2, which may result in inhibition of CCR2 activation and signal transduction. This may inhibit inflammatory processes as well as angiogenesis, tumor cell migration, and tumor cell proliferation. The G-protein coupled receptor CCR2 is expressed on the surface of monocytes and macrophages, stimulates the migration and infiltration of these cell types, and plays an important role in inflammation, angiogenesis, and tumor cell migration and proliferation. Synonyms: PF-04217903; PF 04217903; PF04217903; PF-4217903; PF4217903; PF 4217903. Grades: >98%. CAS No. 956905-27-4. Molecular formula: C19H16N8O. Mole weight: 372.392.
PF-04217903 mesylate is a potent ATP-competitive c-Met kinase inhibitor with K i of 4.8 nM for human c-Met. PF-04217903 mesylate shows more than 1,000-fold selectivity relative to 208 kinases. Antiangiogenic properties [1] [2]. Uses: Scientific research. Group: Signaling pathways. CAS No. 956906-93-7. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-12017A.
PF-04217903 methanesulfonate
PF-04217903 methanesulfonate is a selective ATP-competitive c-Met inhibitor and is susceptible to oncogenic mutations (no activity to Y1230C mutant). It showed more than 1000-fold greater selectivity against c-Met kinase over 150 other kinases. It displays similar potency to inhibit the activity of c-Met-H1094R, c-Met-R988C, and c-Met-T1010I, but has no inhibitory activity against c-Met-Y1230C. It showed antitumor activity in tumor models where c-Met is activated by mechanisms including c-Met gene amplification, HGF/c-Met autocrine loop formation or c-Met overexpression. It suppressed proliferation of c-Met-amplified GTL-16 and H1993cells. It induced apoptosis in GTL-16 cells. It inhibited the phosphorylation of c-Met and suppressed tumor growth. Synonyms: PF-04217903 methanesulfonate; PF 04217903 methanesulfonate; PF04217903 methanesulfonate. Grades: >98%. CAS No. 956906-93-7. Molecular formula: C20H20N8O4S. Mole weight: 468.49.
PF 04418948 acts as a novel, potent and selective prostoglandin EP2 receptor antagonist. Group: Biochemicals. Alternative Names: (1-(-fluorbenzoyl)-3-{[(6-methoxy-2-napthyl)oxy]methyl} Azetidine-3-carboxylic Acid. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences.
Worldwide
PF-04418948
PF-04418948 is an orally active, potent and selective prostaglandin EP 2 receptor antagonist with an IC 50 of 16 nM [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1078166-57-0. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 50 mg. Product ID: HY-18966.
PF-04418948
PF-04418948 is a potent and selective prostaglandin EP2 receptor antagonist with IC50 of 16 nM. Phase 1. PF-04418948 antagonizes the effects of butaprost and PGE2 on an EFS-induced contraction of the human myometrium, and antagonizes PGE2-induced relaxation of carbachol pre-contracted rings of mouse trachea. Synonyms: PF04418948; PF-04418948; PF 04418948; PF4418948; PF-4418948; PF 4418948. Grades: 98%. CAS No. 1078166-57-0. Molecular formula: C23H20FNO5. Mole weight: 409.41.
PF-04447943 is a potent, selective brain penetrant PDE9 inhibitor (Ki of 2.8, 4.5 and 18 nM) for human, rhesus and rat recombinant PDE9 respectively and high selectivity for PDE9 versus PDEs1-8 and 10-11. Synonyms: PF-04447943; PF 04447943; PF04447943; PF-4447943; PF 4447943; PF4447943. Grades: >98%. CAS No. 1082744-20-4. Molecular formula: C20H25N7O2. Mole weight: 395.46.
PF 04449613
PF 04449613 is a potent PDE9 inhibitor (IC50 = 22 nM), and also shows a high affinity for cGMP (Km ~170 nM). Some studies suggest that elevating the level of cGMP with the PDE9 inhibitor PF-04449613 increases synaptic calcium activity and learning-dependent synaptic plasticity. Synonyms: (R)-6-(1-(3-Phenoxyazetidin-1-yl)ethyl)-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one; 1,5-Dihydro-6-[(1R)-1-(3-phenoxy-1-azetidinyl)ethyl]-1-(tetrahydro-2H-pyran-4-yl)-4H-pyrazolo[3,4-d]pyrimidin-4-one, 6-[(1R)-1-(3-Phenoxyazetidin-1-yl)ethyl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one; PF 4449613; PF 9613; PF4449613; PF9613; PF-4449613; PF-9613. Grades: ≥98% by HPLC. CAS No. 1236858-52-8. Molecular formula: C21H25N5O3. Mole weight: 395.45.
PF-04449613
PF-04449613 is a selective PDE9A inhibitor with an IC50 of 22 nM[1]. PF-04449613 improved motor learning ability in a mouse model[2]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1236858-52-8. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-12788.
PF-04457845 is a potent and exquisitely selective inhibitor of FAAH, with an IC50 of 7.2 nM, and both analgesic and antiinflammatory effects in animal studies comparable to naproxen. Synonyms: PF-04457845; PF 04457845; PF04457845; PF-4457845; PF 4457845; PF4457845. Grades: >98%. CAS No. 1020315-31-4. Molecular formula: C23H20F3N5O2. Mole weight: 455.43.
PF 04628935 is a potent antagonist/inverse agonist of the ghrelin receptor, growth hormone secretagogue receptor 1a (GHS-R1a) with an IC50 of 4.6 nM. It is orally bioavailable and exhibits reasonable brain penetration. Synonyms: 1-[2-[[2-Chloro-4-(2H-1,2,3-triazol-2-yl)phenyl]methyl]-2,7-diazaspiro[3.5]non-7-yl]-2-(2-methylimidazo[2,1-b]thiazol-6-yl)ethanone; PF-04628935; PF04628935; PF 04628935; PF-4628935; PF4628935; PF 4628935. Grades: ≥98% by HPLC. CAS No. 1383719-97-8. Molecular formula: C24H26ClN7OS. Mole weight: 496.03.
PF-04634817
PF-04634817 is a dual CCR2/CCR5 antagonist, which can be used to treat diabetic nephropathy and diabetic macular edema. Synonyms: PF-04634817; 1228111-63-4; UNII-51M3FB9B9E51M3FB9B9E[(1S,3R)-3-[[(3S,4S)-3-methoxyoxan-4-yl]amino]-1-propan-2-ylcyclopentyl]-[(1S,4S)-5-[6-(trifluoromethyl)pyrimidin-4-yl]-2,5-diazabicyclo[2.2.1]heptan-2-yl]methanone. CAS No. 1228111-63-4. Molecular formula: C25H36F3N5O3. Mole weight: 511.6.
PF 04671536 is a highly potent and selective inhibitor of phosphodiesterase 8B (PDE8B) phosphodiesterase 8A (PDE8A) (IC50= 1.3 and 1.9 nM, respectively), with selectivity for PDE8A/B over other PDEs (IC50 values are >10 μM) and a range of other targets. Synonyms: PF-04671536 hydrochloride; PF04671536 hydrochloride; PF 04671536 hydrochloride; PF-04671536 HCL; PF04671536 HCL; PF 04671536 HCL; PF04671536HCL; 5-Methyl-3-[[(2R)-4-(2-thiazolylmethyl)-2-morpholinyl]methyl]-3H-1,2,3-triazolo[4,5-d]pyrimidin-7-amine hydrochloride. Grades: ≥98% by HPLC. CAS No. 1305116-67-9. Molecular formula: C14H18N8OS.HCl. Mole weight: 382.87.
PF-04691502
PF-04691502 is an agent targeting the phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) in the PI3K/mTOR signaling pathway, with potential antineoplastic activity. It inhibits both PI3K and mTOR kinases, which may result in apoptosis and growth inhibition of cancer cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to chemotherapy and radiotherapy. mTOR, a serine/threonine kinase downstream of PI3K, may also be activated independent of PI3K. Synonyms: PF04691502; PF 04691502; PF-04691502; PF4691502; PF 4691502; PF-4691502; 2-amino-8-((1R,4R)-4-(2-hydroxyethoxy)cyclohexyl)-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3-d]pyrimidin-7(8H)-one. Grades: > 98%. CAS No. 1013101-36-4. Molecular formula: C22H27N5O4. Mole weight: 425.489.
PF-04691502 is a potent and selective inhibitor of PI3K and mTOR. PF-04691502 binds to human PI3Kα, β, δ, γ and mTOR with K i s of 1.8, 2.1, 1.6, 1.9 and 16 nM, respectively. Uses: Scientific research. Group: Signaling pathways. CAS No. 1013101-36-4. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-15177.
Potent and selective dual ATP-competitive PI 3-K/mTOR inhibitor (Ki values are 1.6, 1.8, 1.9, 2.1 and 16nm for human PI 3-K delta, alpha, gamma, beta, and mTOR, respectively). Displays no significant inhibitory activity at more than 80 protein kinases (concentration ≥ 10um) including hVps34, PI 3-K downstream kinases, and MAPK family members. Orally available. Induces robust cell cycle arrest at the G1 phase in U87MG cancer cells and antitumor activity in SKOV3 ovarian cancer xenograft models. Group: Biochemicals. Grades: Highly Purified. CAS No. 1013101-36-4. Pack Sizes: 5mg, 25mg. US Biological Life Sciences.
This active molecular is a human Nav1.7 voltage gated sodium channel inhibitor with the IC50 value of 28 nM. PF-04856264 inhibits the Nav channel by interacting with the S1-S4 voltage sensor segment of homologous domain 4 which is unlike other known NaV inhibitors. PF-04856264 interaction with the region of the channel which controls voltage sensitivity enables subtype selective modulation and may be applicated as an efficient tool for drug development. Synonyms: PF-04856264; PF04856264; PF 04856264; PF-4856264; PF4856264; PF 4856264. 3-cyano-4-(2-(1-methyl-1H-pyrazol-5-yl)phenoxy)-N-(thiazol-2-yl)benzenesulfonamide. Grades: 98%. CAS No. 1235397-05-3. Molecular formula: C20H15N5O3S2. Mole weight: 437.49.
PF-04859989 hydrochloride is a brain-penetrant, irreversible kynurenine aminotransferase (KAT) II inhibitor with IC 50 s of 23 and 263 nM for hKAT II and rKAT II. PF-04859989 hydrochloride is selective for KAT II over human KAT I, KAT III, and KAT IV (IC50s of 22, 11, and >50 μM, respectively) [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 177943-33-8. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-116451.
PF-04880594 is a RAF inhibitor, which induces ERK phosphorylation and RAF dimerization in those epithelial tissues that undergo hyperplasia. PF-04880594 stimulates production of the inflammatory cytokine interleukin 8 in HL-60 cells. Synonyms: PF04880594; PF 04880594; 3-((4-(1-(2,2-difluoroethyl)-3-(1H-pyrrolo[2,3-b]pyridin-5-yl)-1H-pyrazol-4-yl)pyrimidin-2-yl)amino)propanenitrile. CAS No. 1111636-35-1. Molecular formula: C19H16F2N8. Mole weight: 394.39.
PF 04885614
PF 04885614 is a potent and selective Nav1.8 inhibitor (IC50 = 53 nM for human NaV1.8 channel), with selectivity for hNaV1.8 over hNaV1.6, hNaV1.7, hNaV1.1, hNaV1.2 and hNaV1.5 (IC50= 4.2, 7.0, 11, 16 and 27 μM respectively). Synonyms: PF 04885614; PF04885614; PF-04885614; 1-Methyl-[1-[4-(4-trifluoromethoxy)phenyl]-imidazol-2-yl]-ethanamine. Grades: ≥98% by HPLC. Molecular formula: C13H14F3N3O. Mole weight: 285.26.
PF-04929113, also known as SNX-5422, is a synthetic prodrug targeting the human heat-shock protein 90 (Hsp90) with potential antineoplastic activity. Although the mechanism of action remains to be fully elucidated, Hsp90 inhibitor SNX-5542 is rapidly converted to SNX-2112, which accumulates in tumors relative to normal tissues. SNX-2112 inhibits Hsp90, which may result in the proteasomal degradation of oncogenic client proteins, including HER2/ERBB2, and the inhibition of tumor cell proliferation. Hsp90 is a molecular chaperone that plays a key role in the conformational maturation of oncogenic signaling proteins, such as HER2/ERBB2, AKT, RAF1, BCR-ABL, and mutated p53, as well as many other molecules that are important in cell cycle regulation or immune responses. Synonyms: (1r,4r)-4-((2-carbamoyl-5-(6,6-dimethyl-4-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl)phenyl)amino)cyclohexyl glycinate; SNX5422; SNX-5422; SNX 5422; PF4929113; PF-4929113; PF 4929113; PF04929113; PF 04929113; PF-04929113. Grades: >97%. CAS No. 908115-27-5. Molecular formula: C25H30F3N5O4. Mole weight: 521.53.
PF-04929113 mesylate
The methlate salt form of PF-04929113 that has potential antineoplastic activity targeting Hsp90. It could probably result in the proteasomal degradation of oncogenic client proteins and the restrain of tumor cell proliferation. Uses: The methlate salt form of pf-04929113 that has potential antineoplastic activity targeting hsp90. Synonyms: PF-04929113 mesylate; PF 04929113 mesylate; PF04929113 mesylate; (1r,4r)-4-((2-carbamoyl-5-(6,6-dimethyl-4-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl)phenyl)amino)cyclohexyl glycinate mesylate; PF-04929113 mesylate; SNX5422; SNX-5422; SNX 5422; PF4929113; PF-4929113; PF 4929113; PF04929113; PF 04929113; PF-04929113. Grades: 98%. CAS No. 1173111-67-5. Molecular formula: C26H34F3N5O7S. Mole weight: 617.64.
PF-04937319
This active molecular is a glucokinase activator originated by Pfizer and EC50 value is 174 nM. PF-04937319 can improve glycemic control in adults with type 2 diabetes when applicated in conjunction with metformin and it can also maintain lower-glucose levels without it resulting in hypoglycemia. However,clinical trials were discontinued for Type 2 diabetes mellitus in 2016. Uses: Type 2 diabetes mellitus. Synonyms: PF-04937319; PF04937319; PF 04937319; PF-4937319; PF 4937319; PF4937319; N,N-dimethyl-5-((2-methyl-6-((5-methylpyrazin-2-yl)carbamoyl)benzofuran-4-yl)oxy)pyrimidine-2-carboxamide. Grades: 98%. CAS No. 1245603-92-2. Molecular formula: C22H20N6O4. Mole weight: 432.44.
PF-04942487
PF-4942847 is a novel oral Hsp90 inhibitor, which is a candidate for clinical development in TNBC by collaboratively targeting multiple signaling pathways. In addition, AKT degradation in PBLs may serve as a biomarker in clinical development. Synonyms: PF4942847; PF 4942847; PF-04942847. Grades: >98%. CAS No. 1046859-34-0. Molecular formula: C20H18Cl2F3N7O2. Mole weight: 516.31.
This active molecular is a hepatoselective glucokinase activator that reduces MDG (mean daily glucose), FPG (fasting plasma glucose) and glucose excursion in humans. PF-04991532 may offer glycemic control without inducing hepatic steatosis. PF-04991532 was developed by Pfizer but was discontinued in Phase-II for Type-2 diabetes mellitus in USA in 2012. Uses: Type 2 diabetes mellitus. Synonyms: PF-04991532; PF 04991532; PF04991532; PF-4991532; PF4991532; PF 4991532; UNII-AJ212MS2O2; CHEMBL2165620; AJ212MS2O2; SCHEMBL1711504; BDBM50394681; 6-[[(2S)-3-cyclopentyl-2-[4-(trifluoromethyl)imidazol-1-yl]propanoyl]amino]pyridine-3-carboxylic acid. Grades: 98%. CAS No. 1215197-37-7. Molecular formula: C18H19F3N4O3. Mole weight: 396.37.
PF-04995274 is a 5-HT4 receptor partial agonist with Ki = 0.15 - 0.46 nM for 5-HT4 isoforms a, b, d and e, developed for the treatment of Alzheimer's disease (AD). Synonyms: (R)-4-((4-(((4-(Tetrahydrofuran-3-yloxy)-1,2-benzisoxazol-3-yl)oxy)methyl)piperidin-1-yl)methyl)tetrahydro-2H-pyran-4-ol; PF-04995274; PF 04995274; PF04995274; PF-4995274; PF 4995274; PF4995274. CAS No. 1331782-27-4. Molecular formula: C23H32N2O6. Mole weight: 432.52.
PF-05020182
PF05020182 is novel potent and selective Kv7.2/4 potassium channel opener originated by Pfizer. It can inhibit convulsions in the MES assay at doses tested, consistent with in vitro activity measure. PF-05020182 may be applicated for adjunctive treatment of refractory epilepsy. Uses: Refractory epilepsy. Synonyms: PF05020182; PF-05020182; PF 05020182; PF5020182; PF-5020182; PF 5020182. N-[4,6-Dimethoxy-2-(4-methoxy-1-piperidinyl)-5-pyrimidinyl]-3,3-dimethyl-butanamide. Grades: 98%. CAS No. 1354712-92-7. Molecular formula: C18H30N4O4. Mole weight: 366.46.
A fully humanized monoclonal antibody (mAb) that stimulates signaling through 4-1BB (CD-137), a protein expressed in many immune cells. Synonyms: Utomilumab; PF-2566; PF-5082566; PF 2566; PF 5082566; PF2566; PF5082566. CAS No. 1417318-27-4.
PF 05089771 is a potent, orally active and selective arylsulfonamide Na v 1.7 inhibitor, with IC 50 values of 11 nM, 12 nM, 13 nM, 171 nM and 8 nM for hNa v 1.7, cynNa v 1.7, dogNa v 1.7, ratNa v 1.7, and musNa v 1.7, respectively. PF 05089771 is under the study for pain and diabetic neuropathy [1] [2]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1235403-62-9. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-12883.
PF-05089771, a Nav1.7 channel blocker, has been studied to have potential effect in the treatment of chronic neuropathic pain. It is still under Phase II clinical trial. IC50: 8.6 nM. Uses: Pf-05089771 is a nav1.7 channel blocker that has been studied to have potential effect in the treatment of chronic neuropathic pain. Synonyms: PF 05089771; PF05089771; PF-05089771; 4-(2-(3-amino-1H-pyrazol-4-yl)-4-chlorophenoxy)-5-chloro-2-fluoro-N-(thiazol-4-yl)benzenesulfonamide; SCHEMBL1095065; CHEMBL2325014; ZYSCOUXLBXGGIM-UHFFFAOYSA-N. Grades: 98%. CAS No. 1235403-62-9. Molecular formula: C18H12Cl2FN5O3S2. Mole weight: 500.35.
PF 05089771 tosylate
PF 05089771 is a selective and potent inhibitor of the human voltage-gated sodium ion channel Nav1.7 with an IC50 value of 11 nM. It exhibits selectivity for Nav1.7 over other Nav1 channels (IC50 values are 0.11, 0.16, 0.85, 10, 11 and 25 μM for Nav1.2, Nav1.6, Nav1.1, Nav1.4, Nav1.3 and Nav1.5, respectively). Synonyms: 4-[2-(3-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-4-thiazolylbenzenesulfonamide tosylate; PF-05089771; PF05089771; PF 05089771 Tosylate. Grades: ≥98% by HPLC. CAS No. 1430806-04-4. Molecular formula: C18H12Cl2FN5O3S2.C7H8O3S. Mole weight: 672.56.
PF 05105679
PF-05105679 is a selective TRPM8 Antagonist with clinical efficacy in cold-related pain. IC50 value is 103 nM. It shows >100-fold selectivity for TRPM8 over a panel of receptors, ion channels and enzymes, including TRPV1 and TRPA1 ion channels. In Sep 2011, Pfizer completed a phase I trial for the treatment of neuropathic pain in Healthy volunteers in Belgium. Uses: Neuropathic pain;cold-related pain. Synonyms: PF-05105679; PF 05105679; PF05105679; PF-5105679; PF 5105679; PF5105679. 3-[[[(1R)-1-(4-Fluorophenyl)ethyl](3-quinolinylcarbonyl)amino]methyl]-benzoic acid, PF05105679, [(R)-3-[(1-(4-fluorophenyl)ethyl)(quinolin-3-ylcarbonyl)amino]methylbenzoic acid. Grades: 98%. CAS No. 1398583-31-7. Molecular formula: C26H21FN2O3. Mole weight: 428.45.