MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報，我們不為任何個人用途提供產(chǎn)品和服務(wù)。

PF-4136309

CAS No. : 1341224-83-6

MCE 國際站：PF-4136309

產(chǎn)品活性：PF-4136309 是一種高效，選擇性，可口服的 CCR2 拮抗劑，能夠抑制人，小鼠和大鼠 CCR2，IC₅₀ 值分別為 5.2 nM，17 nM 和 13 nM。

研究領(lǐng)域：GPCR/G Protein  |  Immunology/Inflammation

作用靶點：CCR

In Vitro: PF-4136309 is potent in human chemotaxis activity (IC₅₀=3.9 nM) and in the whole blood assay (IC₅₀=19 nM), with IC₅₀ of 16 and 2.8 nM in mouse and rat chemotaxis assays. PF-4136309 is potent in inhibiting CCR2 mediated signaling events such as intracellular calcium mobilization and ERK (extracellular signal-regulated kinase) phosphorylation with IC₅₀ values of 3.3 and 0.5 nM, respectively. In hERG patch clamp assay, PF-4136309 inhibits hERG potassium current with an IC₅₀ of 20 μM. PF-4136309 is not a cytochrome P450 (CYP) inhibitor, with IC₅₀ values of >30 μM against five major CYP isozymes CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4. Moreover, PF-4136309 is not a CYP inducer at concentrations up to 30 μM.

In Vivo: PF-4136309 (2 mg/kg) exhibits a moderate half-life in both species after iv administration (2.5 and 2.4 h). When administered orally, PF-4136309 (10 mg/kg) is absorbed rapidly, with peak concentration time (T_max) at 1.2 h for rats and 0.25 h for dogs. A similar half-life is observed in both species between iv dosing and po dosing. PF-4136309 is well absorbed, with an oral bioavailability of 78% in both species.

相關(guān)產(chǎn)品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  GPCR/G Protein Compound Library  |  Immunology/Inflammation Compound Library  |  Clinical Compound Library  |  Small Molecule Immuno-Oncology Compound Library  |  Drug Repurposing Compound Library  |  Endocrinology Compound Library  |  Orally Active Compound Library  |  Anti-Pulmonary Fibrosis Compound Library  |  Chemokine Compound Library  |  Heterocyclic Compound Library  |  Membrane Protein-targeted Compound Library  |  Membrane Receptor-targeted Compound Library  |  Highly Selective Inhibitors Library  |  Cytokine Inhibitors Library  |  Pirfenidone  |  Maraviroc  |  RS 504393  |  Bindarit  |  INCB3344  |  BX471  |  RS102895 hydrochloride  |  Cenicriviroc  |  TAK-779  |  CCR6 inhibitor 1  |  Zelnecirnon  |  CCR6 antagonist 1  |  AZ084  |  ZK756326 dihydrochloride  |  AZD2098  |  GW 766994  |  R243  |  7,4'-Dihydroxyflavone  |  BMS-813160  |  CCR7 Ligand 1  |  MK-0812 Succinate  |  K777  |  Vercirnon  |  DAPTA  |  Tivumecirnon  |  C-021  |  CCR2 antagonist 4 hydrochloride  |  INCB 3284

熱門產(chǎn)品線：重組蛋白  |  化合物庫  |  天然產(chǎn)物  |  熒光染料  |  PROTAC  |  同位素標記物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds