Pk11195

Manufactured by Merck Group

Sourced in United States, France, United Kingdom

PK11195 is a chemical compound used in laboratory research. It functions as a selective ligand for the translocator protein (TSPO), which is involved in various cellular processes. The core function of PK11195 is to serve as a research tool for the study of TSPO and its associated biological mechanisms.

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Lab products found in correlation

Ro5 4864, by Merck Group (4 mentions) L carnosine, by Merck Group (3 mentions) Amersham hyperfilm mp, by GE Healthcare (2 mentions) Rifampicin rif, by Merck Group (2 mentions) Papaverine, by Merck Group (2 mentions) Dimethyl sulfoxide (dmso), by Merck Group (2 mentions) Lipopolysaccharides (lps), by Solarbio (2 mentions) Microbeta2 2450 microplate counter, by PerkinElmer (2 mentions) Tnf α, by R&D Systems (2 mentions) Penicillin streptomycin, by Thermo Fisher Scientific (2 mentions) Culture media, by Thermo Fisher Scientific (1 mentions) 4 hne, by Merck Group (1 mentions) Streptozotocin (stz), by Merck Group (1 mentions) Metformin, by Merck Group (1 mentions) Fluoxetine, by Merck Group (1 mentions) Dimethyl sulfoxide (dmso), by Thermo Fisher Scientific (1 mentions) Citco, by Bio-Techne (1 mentions) Hek293, by American Type Culture Collection (1 mentions) Hepg2 c3a, by American Type Culture Collection (1 mentions) Midazolam, by Merck Group (1 mentions)

38 protocols using pk11195

TSPO Modulation in Activated Microglia

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Murine microglial BV2 cells were cultured with Dulbecco’s Modified Eagle Medium (Gibco/Thermo Fisher Scientific, MA, USA) supplemented with fetal bovine serum (10%, Gibco) and penicillin-streptomycin (1%, Thermo Fisher Scientific) in a humidified, 5% CO₂ incubator at 37°C.
BV-2 cells were exposed to 100 ng/mL lipopolysaccharide (LPS; Sigma-Aldrich) and interferon (IFN)-γ (20 ng/mL; Peprotech) for 24 h. Subsequently, BV2 cells were transfected with TSPO siRNA and siRNA-NC (100 nM; Genechem) for 6 h using Lipofectamine 2000 (Invitrogen) according to the manufacturer’s instructions and harvested 12 h after transfection. Cells were divided into two groups: LPS+IFN-γ+ si-NC and LPS+IFN-γ+ si-TSPO groups. The cells were then treated with PK11195 (0.5 Μm; Sigma-Aldrich) for 6 h (LPS+IFN-γ+ PK11195 and LPS+IFN-γ+ si-TSPO+PK11195 groups, respectively).

Xue X., Duan R., Zheng G., Chen H., Zhang W, & Shi L. (2022). Translocator protein (18 kDa) regulates the microglial phenotype in Parkinson’s disease through P47. Bioengineered, 13(4), 11061-11071.

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Detailed TSPO Ligand Characterization

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Otherwise indicated, all chemicals and solvents used were purchased from Sigma–Aldrich (Marne la Coquette, France). Culture media were purchased from Life Technology (Saint-Aubin, France). TSPO ligands (Supplementary Figure 9) were purchased from Sigma-Aldrich (PK 11195 and Ro5-4864) or synthesized following the procedure previously described (SSR-180,575)44 .

Marginedas-Freixa I., Hattab C., Bouyer G., Halle F., Chene A., Lefevre S.D., Cambot M., Cueff A., Schmitt M., Gamain B., Lacapere J.J., Egee S., Bihel F., Le Van Kim C, & Ostuni M.A. (2016). TSPO ligands stimulate ZnPPIX transport and ROS accumulation leading to the inhibition of P. falciparum growth in human blood. Scientific Reports, 6, 33516.

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Zebrafish Embryo 4-HNE Intervention

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Fertilized zebrafish embryos were transferred into 6-well plate, around 30 embryos per well with 5 ml eggwater. At 24 hpf the chorion of zebrafish embryos was removed using sharp forceps and 0,003% PTU was added to the eggwater. For 4-HNE intervention and rescue experiments, 10 μM 4-HNE (393,204; Sigma-Aldrich), 10 μM PK11195 (C0424; Sigma-Aldrich), 1 mM, 5 mM or 10 mM l-Carnosine (C9625; Sigma-Aldrich) treatments were started at 3 hpf and continued until the end. For ALDH inhibition, 0.25 μM or 1 μM Gossypol (G8761-100MG; Sigma-Aldrich) and DEAB (D86256-100G; Sigma-Aldrich) treatments were started at 3 hpf and continued until the end; Medium was changed every day.

Lou B., Boger M., Bennewitz K., Sticht C., Kopf S., Morgenstern J., Fleming T., Hell R., Yuan Z., Nawroth P.P, & Kroll J. (2020). Elevated 4-hydroxynonenal induces hyperglycaemia via Aldh3a1 loss in zebrafish and associates with diabetes progression in humans. Redox Biology, 37, 101723.

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Synthesis of TSPO Ligands for Pharmaceutical Research

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Otherwise indicated, all chemicals and solvents used were purchased from Sigma–Aldrich (Marne la Coquette, France). TSPO ligands (Figure 7) N,N-Diethyl-2-(2-(furan-2-yl)-5-oxomidazo[1-c]quinazolin-6(5H)-yl)acetamide (NCS1018), N,N-dipropyl-2-(5-oxo-2-phenylimidazo[1-c]quinazolin-6(5H)-yl)acetamide (NCS1026), and N,N-diethyl-2-(2-(furan-2-yl)-5-oxoimidazo[1-c]quinazolin-6(5H)-yl)acetamide (NCS1016), which belonged to the imidazo[1-c]quinazolin-5-one family, were synthesized following the previously-described protocol [28 (link)]. SSR-180,575 was synthetized as previously described [49 ]. PK 11195 and Ro5-4864 were purchased from Sigma–Aldrich.

Marginedas-Freixa I., Alvarez C.L., Moras M., Hattab C., Bouyer G., Chene A., Lefevre S.D., Le Van Kim C., Bihel F., Schwarzbaum P.J, & Ostuni M.A. (2018). Induction of ATP Release, PPIX Transport, and Cholesterol Uptake by Human Red Blood Cells Using a New Family of TSPO Ligands. International Journal of Molecular Sciences, 19(10), 3098.

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Pharmacological Interventions for Diabetes and Depression

Cited 2 times

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AC-5216 was purchased from Medchem Express (USA). PK11195, STZ, metformin (Met) and fluoxetine (Flu) were purchased from Sigma-Aldrich (USA). AC-5216 was prepared as a suspension in 0.5% tragacanth gum solution and administered to rats by gavage (i.g)27 (link). The dose range of AC-5216 (0.1, 0.3, and 1 mg/kg, i.g.) was based on its antidepressant- and anxiolytic- like activities as described previously with minor adjustments24 (link). PK11195, injected intraperitoneally (i.p.), was suspended in saline containing 2% DMSO and 0.8% Tween 8024 (link). The dosage of PK11195 (1 and 3 mg/kg, i.p.) was based on published studies showing the inhibitory effect of PK11195 against AC-5216 and other TSPO ligands24 (link)28 (link)29 (link). STZ dissolved freshly in citrate buffer (pH 4.5)30 (link). With the control effects of blood glucose, Met is the mainstay treatment in the prevention of T2DM and associated comorbidities31 (link). The lowered blood glucose induced by Met in HFD-STZ model mimics the situation of type 2 diabetes relevant to human condition. Consequently, Met (1.8 mg/kg, i.p), Flu (10.8 mg/kg, i.p) and the combination (Met+Flu, MF) were administered as positive control drugs in all behavioral tests respectively based on their antidepressant-like effects on the T2DM rodent model30 (link).

Qiu Z.K., He J.L., Liu X., Zhang G.H., Zeng J., Nie H., Shen Y.G, & Chen J.S. (2016). The antidepressant-like activity of AC-5216, a ligand for 18KDa translocator protein (TSPO), in an animal model of diabetes mellitus. Scientific Reports, 6, 37345.

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Cell Line Authentication and Maintenance

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Human embryonic kidney cell line HEK293 (ATCC CRL-1573) and liver hepatocellular cell line HepG2/C3A (ATCC CRL-10741) were obtained from American Type Culture Collection (ATCC, Manassas, VA). The cell lines, which have been authenticated by ATCC by using short tandem repeat DNA profiling, were expanded immediately upon receipt within three passages and frozen for future use. The cells were tested routinely for mycoplasma contamination and always tested negative. Fetal bovine serum (FBS) was obtained from HyClone (Logan, UT). HepG2/C3A and HEK293 cell lines were maintained in Eagle’s minimum essential medium (EMEM) supplemented with 10% FBS, 100 U/mL penicillin, and 100 μg/mL streptomycin in a humidified incubator at 37 °C with 5% CO₂. Dimethylsulfoxide (DMSO) was purchased from Fisher Scientific (Pittsburgh, PA). CITCO was obtained from Tocris Bioscience (Bristol, UK). CINPA1 was obtained from ChemDiv (San Diego, CA) and PK11195 was purchased from Sigma-Aldrich (St. Louis, MO).

Cherian M.T., Chai S.C., Wright W.C., Singh A., Casal M.A., Zheng J., Wu J., Lee R.E., Griffin P.R, & Chen T. (2018). CINPA1 binds directly to constitutive androstane receptor and inhibits its activity. Biochemical pharmacology, 152, 211-223.

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Radiolabeling and Quantification of TSPO in Cardiac Tissue

Cited 1 time

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[¹²⁵I]-IodoDPA-713, used to assess TSPO levels in the heart, was synthesized using a two-step reaction process, as previously [29 (link)]. Desmethyl DPA-713 was first iodinated with [¹²⁵I]NaI in the presence of iodogen. The ¹²⁵I radiolabeled intermediate was methylated by MeI/K₂CO₃/DMF and HPLC purified. The overall radioactive yield was 35-50% with >99% radiochemical purity. Fresh-frozen hearts were sectioned (20μm) on a cryostat in the sagittal plane and thaw-mounted onto poly-L-lysine-coated slides and stored at −20°C. Slides were dried for 30min and prewashed with 50mM Tris-HCl buffer (pH 7.4). To determine total binding, slides were incubated for 1h at RT in buffer containing 0.8nM [¹²⁵I]-IodoDPA-713 (specific activity 2200 Ci/mmol). To measure non-specific binding, adjacent slides were incubated in the presence of 50μM cold racemic PK11195 (Sigma, St. Louis, MO). After incubation, slides were washed and exposed to film at RT for 20min. Images were captured and analyzed using MCID (InterFocus Imaging Ltd., Cambridge, England) calibrating for density using [¹²⁵I]-microscales. The mean value for all sections/heart was used for statistical analyses.

Fairweather D., Coronado M.J., Garton A.E., Dziedzic J.L., Bucek A., Cooper LT J.r., Brandt J.E., Alikhan F.S., Wang H., Endres C.J., Choi J., Pomper M.G, & Guilarte T.R. (2014). Sex differences in translocator protein 18 kDa (TSPO) in the heart: implications for imaging myocardial inflammation. Journal of cardiovascular translational research, 7(2), 192-202.

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Benzodiazepine and TSPO Ligand Effects

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Alprazolam, midazolam, clonazepam, PK11195, and bicuculline were purchased from Sigma-Aldrich. AP-3 was provided by Algiax Pharmaceuticals GmbH. Stock solutions of Alprazolam (10 mM in DMSO), midazolam (6.25 mM in water), clonazepam (50 mM in ETOH), or AP-3 (50 mM in DMSO) were diluted into media to the indicated concentration.

Tian J., Dang H., Middleton B, & Kaufman D.L. (2017). Clinically applicable GABA receptor positive allosteric modulators promote ß-cell replication. Scientific Reports, 7, 374.

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In Vitro Autoradiography of TSPO

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Mice were terminally anaesthetized with an overdose of sodium pentobarbital and transcardially perfused with 0.9% saline. Brains were harvested, frozen in isopentane at a temperature of −40°C and stored at −80°C. NBH (n = 7), ME7 (n = 8) and ME7 + JNJ-527 (n = 8) mouse brains were coronally cryosectioned at 20 μm and directly mounted onto glass slides. Slides were incubated at room temperature for 30 min in 100 mM Tris-HCl containing 1 nM [3H]PK11195 (specific activity 82.7 Ci per mmol; Perkin Elmer), washed twice for 6 min in 100 mM Tris-HCl, rinsed dipping into dH₂O and air dried. Non-specific binding was carried out in the presence of 20 µM PK11195 (Sigma-Aldrich) and 1 nM ³H-PK11195. The slides were exposed to tritium-sensitive film (Amersham Hyperfilm MP, GE Healthcare) in autoradiography cassettes together with a set of tritium standards ([3H]Microscale, American Radiolabeled Chemicals) for 6 weeks. Sections for specific and non-specific binding were processed together in a paired protocol. Films were developed using ECOMAX X-ray film processor (PROTEC). Quantitative analysis was performed using a MCID image analyser (Image Research), and brain structures were identified using the mouse brain atlas of Franklin and Paxinos (1997). All regions of interest (hippocampus, cortex and thalamus) were analysed by freehand drawing tools in three consecutive sections per brain.

Mancuso R., Fryatt G., Cleal M., Obst J., Pipi E., Monzón-Sandoval J., Ribe E., Winchester L., Webber C., Nevado A., Jacobs T., Austin N., Theunis C., Grauwen K., Daniela Ruiz E., Mudher A., Vicente-Rodriguez M., Parker C.A., Simmons C., Cash D., Richardson J., Jones D.N., Lovestone S., Gómez-Nicola D, & Perry V.H. (2019). CSF1R inhibitor JNJ-40346527 attenuates microglial proliferation and neurodegeneration in P301S mice. Brain, 142(10), 3243-3264.

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Ligand Screening for Nuclear Receptors

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Compound 1 (CITCO, (6-(4-chlorophenyl)imidazo [2,1-b][1,3]thiazole-5-carbaldehyde-O-(3,4-dichloro-benzyl)oxime)),
rifampicin (rif), TCPOBOP, and PK11195 were obtained from Sigma-Aldrich
(St. Louis, Missouri, United States, now Merck), which is now known
as Merck (Darmstadt, Germany). Phenobarbital (Luminal 200 mg/mL injection)
was manufactured by Desitin Pharma spol. s.r.o. (Prague, Czech Republic).
Ligands for nuclear receptors (GW3965, thyroxin, obeticholic acid,
dexamethasone, fenofibrate, GW501516, rosiglitazone, 3-methylcholanthrene,
calcitriol, testosterone, and estradiol) were purchased from Sigma-Aldrich
(now Merck). The prototype ligands were used at 100 nM (dexamethasone,
calcitriol), 1 μM (thyroxin), or 10 μM concentrations.
The compounds were dissolved in DMSO, and the final concentration
of DMSO in the entire reaction mixture or cultivation media was 0.1%.

Mejdrová I., Dušek J., Škach K., Stefela A., Skoda J., Chalupský K., Dohnalová K., Pavkova I., Kronenberger T., Rashidian A., Smutná L., Duchoslav V., Smutny T., Pávek P, & Nencka R. (2023). Discovery of Novel Human Constitutive Androstane Receptor Agonists with the Imidazo[1,2-a]pyridine Structure. Journal of Medicinal Chemistry, 66(4), 2422-2456.

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