Pioglitazone HCl

For research use only.

Catalog No.S2046 Synonyms: AD-4833, U-72107E

5 publications

Pioglitazone HCl Chemical Structure

CAS No. 112529-15-4

Pioglitazone HCl (AD-4833, U-72107E) is an inhibitor of cytochrome P450 (CYP)2C8 and CYP3A4 enzymes. Pioglitazone HCl inhibits CYP2C8, CYP3A4 and CYP2C9 with Ki of 1.7 μM, 11.8 μM and 32.1 μM, respectively. Pioglitazone HCl is also a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist with EC50 of 0.93 μM and 0.99 μM for human PPARγ and mouse PPARγ, respectively. Pioglitazone HCl inhibits mitochondrial iron uptake, lipid peroxidation, and subsequent ferroptosis.

Selleck's Pioglitazone HCl has been cited by 5 publications

2 Customer Reviews

  • Primary hepatocytes were treated with or without 20μM Wy14643/Pioglitazone/Rosiglitazone for 24h followed by stimulation with or without 1μg/ml recombinant human FGF21 for 15min. FGF21 signaling was analyzed by phosphorylation of ERK1/2 and FRS2 examination.

    Mol Nutr Food Res, 2017, 61(9). Pioglitazone HCl purchased from Selleck.

    Accumulated 7-day BrdU labeling in representative sections of pancreatic islets from mice fed (A) normal chow, (B) HFD, (C) HFD+clodronate, and (D) HFD+pioglitazone. β-Cells were immunostained with anti-insulin Ab (green) and for replication with anti-BrdU Ab (red). Nuclei were stained in blue. Scale bar, 100 μm. The percentage of BrdU-positive β-cells was calculated. Values are means±SE with 5 pancreas samples in each experimental group analyzed and are shown in E. *P<0.05 where significant difference was detected between the HFD mice and other treatment groups. No significant difference was detected between the results of other groups.

    Endocrinology and Metabolism, 2016, 311(4): E763-E771.. Pioglitazone HCl purchased from Selleck.

Purity & Quality Control

Choose Selective P450 (e.g. CYP17) Inhibitors

Biological Activity

Description Pioglitazone HCl (AD-4833, U-72107E) is an inhibitor of cytochrome P450 (CYP)2C8 and CYP3A4 enzymes. Pioglitazone HCl inhibits CYP2C8, CYP3A4 and CYP2C9 with Ki of 1.7 μM, 11.8 μM and 32.1 μM, respectively. Pioglitazone HCl is also a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist with EC50 of 0.93 μM and 0.99 μM for human PPARγ and mouse PPARγ, respectively. Pioglitazone HCl inhibits mitochondrial iron uptake, lipid peroxidation, and subsequent ferroptosis.
Targets
Ferroptosis [8]
()
hPPARγ [1]
(Cell-free assay)
rPPARγ [6]
(Cell-free assay)
CYP2C8 [7]
(Cell-free assay)
CYP3A4 [7]
(Cell-free assay)
0.93 μM(EC50) 0.99 μM(EC50) 1.7 μM(Ki) 11.8 μM(Ki)
In vitro

Pioglitazone inhibits LPS-induced iNOS expression and NO generation, and inhibition of iNOS is sufficient to protect dopaminergic neurons against LPS insult. Pioglitazone protects dopaminergic neurons against LPS insult at least via inhibiting iNOS expression and NO generation, which is potentially mediated via inhibition of p38 MAPK activity. Pioglitazone inhibits LPS-induced phosphorylation of p38 MAPK. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
COS cells MYLGeY5kfGmxbjDhd5NigQ>? NV\PZ2t7XHKjboPjdolxfGmxbnHsJIFkfGm4YYTpc44hcW5iQ1;TJINmdGy|IHX4dJJme3OrbnegVHBCWiCpYX3tZUBidmRiUmjSJIFteGijOzD2ZYx2\XNiaX6geIhmKHCjcnXueIhme2W|IHnu[Ilk[XSnczC5OUUh[2:wZnnk[Y5k\SCrboTldpZidCxiRVO1NF0xNjR7IN88US=> NX7rSJBtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUG5NFYzQTNpPkGxPVA3Ojl|PD;hQi=>
HepG2 cells MVzGeY5kfGmxbjDhd5NigQ>? MYfQ[ZJwgGm|b33lJJBzd2yrZnXyZZRweiCjY4TpeoF1\WRicnXj[ZB1d3JiZ3HtcYEh[WexbnnzeIlkKGGldHn2bZR6KGmwIFjldGczKGOnbHzzMEBGSzVyPUeuOkDPxE1? M{TqWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFyN{G0OVA{Lz5zMEexOFUxOzxxYU6=
CV-1 NE\JXFVHfW6ldHnvckBie3OjeR?= MoTTTY4hfmm2cn:geJJidnOlcnnweIlwdmGuIHHjeIl3[XSrb36gc4YhWGW{b4jpd49u\SCycn;sbYZmemG2b4KgZYN1cX[jdHXkJJJm[2WydH;yJIdidW2jIDjQVGFTMSCneIDy[ZN{\WRiaX6gR3YuOSClZXzsd{whTUN3ME2wMlY6|ryPLh?= MlLvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwQDV5NkmwO{c,QDV5NkmwO|ww[T5?
3T3-L1 NV;SU2R[TnWwY4Tpc44h[XO|YYm= MorGSYZn\WO2aY\lJINwdmOnboTyZZRqd25iZn;yJFUxLSCnbnjhcoNmdWWwdDDv[kBqdnO3bHnuMYlv\HWlZXSgeJJq\2y7Y3XybYRmKGGlY4XteYxifGmxbjDpckA{XDNvTEGgZ4VtdHNuIFXDOVA:OC5zNt88UU4> NIftNmQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi97NUm5NlQyLz57NUm5NlQyRC:jPh?=
CV-1 NIjyU49HfW6ldHnvckBie3OjeR?= NYq4cFhjSWO2aY\heIlwdiCxZjDw[ZJwgGm|b33lJJBzd2yrZnXyZZRweiCjY4TpeoF1\WRicnXj[ZB1d3JiZ3HtcYEhdWWjc4Xy[YQh[nliaX7keYN1cW:wIH;mJFUxLSCxZjDtZZhqdXWvIHHsb4FtcW6nIIDoc5NxcGG2YYPlJIFkfGm4aYT5MEB1emGwc3\lZ5Rqd25iYYPzZZkhcW5iQ2[tNUBk\WyuczygSWM2OD1yLkW4PFg1|ryPLh?= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek86QDN4NkKwK|46QDN4NkKwQE9iRg>?
CV-1 Ml7ESpVv[3Srb36gZZN{[Xl? NGHSRXRO[XirbXHsJJJmeG:{dHXyJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUHXyc5hqe2:vZTDwdo9tcW[ncnH0c5Ih[WO2aY\heIVlKHKnY3XweI9zKGejbX3hJGdidDRiY3jpcYVzcWNiaX6geJJidnOrZX70cJkhfHKjboPm[YN1\WRiQ2[tNUBk\WyuczDifUBnfW6ldHnvcoFtKGG|c3H5MEBGSzVyPUCuOVjPxE1w MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOTd{MEi1OEc,OTF5MkC4OVQ9N2F-
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CV1 MnnNSpVv[3Srb36gZZN{[Xl? NYOzSZI4XHKjboPhZ5RqfmG2aX;uJI9nKFCSQWLnZY1u[SCrbjDDWlEh[2WubIOsJGVEPTB;MD61Oe69VS5? MonGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZ6MkG3OlkoRjF4OEKxO|Y6RC:jPh?=
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CHO NUfncHhDTnWwY4Tpc44h[XO|YYm= MVPBZ5RqfmG2aX;uJI9nKEejbESteIFo\2WmIHj1cYFvKFCSQWLnZY1u[SCneIDy[ZN{\WRiaX6gR2hQKGOnbHzzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygSWM2OD1yLkG0{txONg>? Mo\XQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB4NU[0PVQoRjJyNkW2OFk1RC:jPh?=
HEK293T M3\aS2Z2dmO2aX;uJIF{e2G7 M17CXFEhfU1? MW[yOEBpenN? M4\XU3BienSrYXygZYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDQVGFT\2GvbXGtUGJFKGW6cILld5Nm\CCrbjDISWszQTOWIHPlcIx{KGG|c3Xzd4VlKGG|IHnu[JVkfGmxbjDv[kBz\WOncITvdkB1emGwc3HjeIl3[XSrb36gZZQhOSC3TTDh[pRmeiB{NDDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5 MmfKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjFyM{CyOlMoRjJzMEOwNlY{RC:jPh?=
COS-1 M3u4e2Z2dmO2aX;uJIF{e2G7 NGP2dlZC\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJHBRSVKpYX3tZUBtcWejbnSgZolv\GmwZzDkc41icW5iZYjwdoV{e2WmIHnuJGNQWy1zIHPlcIx{KGOxLYTyZY5{\mWldHXkJJdqfGhiR3HsOEBjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGVEPTB;MD6zPe69VS5? NFrMUHM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUGzNFY1QSd-MkGxN|A3PDl:L3G+
CHO M3;sUmZ2dmO2aX;uJIF{e2G7 MYiyOEBpenN? NIHIfphR[XK2aXHsJIFod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gVHBCWmejbX3hJIV5eHKnc4Pl[EBqdiCFSF:gZ4VtdHNiY3:teJJidnOoZXP0[YQhf2m2aDDHZYw1NXKnc4DvcpNqfmVibIXjbYZmemG|ZTDy[ZBwenSncjDwcIF{dWmmIHHmeIVzKDJ2IHjyd{BjgSC2cnHud4FkfGm4YYTpc44h[XO|YYmsJGVEPTB;MD6zPe69VS5? MlHSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|N{e4O|UoRjJzM{e3PFc2RC:jPh?=
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stem cells M{LyeGZ2dmO2aX;uJIF{e2G7 M2HPUlUh\GG7cx?= MVjJcoR2[3Srb36gc4Yh[WSrcH;n[Y5me2m|IHnuJIh2dWGwIHLvcoUhdWG{cn;3MYRmemm4ZXSgcYV{\W6laIntZYwhe3SnbTDj[YxteyCjc4Pld5Nm\CCjczDpcoNz\WG|ZTDpckBi\Gmyb37lZ5RqdiCycn;keYN1cW:wIH3lZZN2emWmIH;uJIRigSB3IHnuJJBz\XOnbnPlJI9nKEmGWDDifUBGVEmVQTygSWM2OD1yLkO1{txONg>? MmX0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB4N{K2PVgoRjNyNkeyOlk5RC:jPh?=
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HEK293T NYLscWw5TnWwY4Tpc44h[XO|YYm= M4rLZVE5KGi{cx?= NUPRfmVQXHKjboPhZ5RqfmG2aX;uJI9nKGOqaX3ldolkKEejbESgfYVie3RiRFLEJIZ2e2WmLWDQRXJo[W2vYTDMRmQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iSFXLNlk{XCClZXzsd{Bkdy2neIDy[ZN{cW6pIGDQVmUh[W[2ZYKgNVghcHK|IHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiRVO1NF0xNjN3zszNMi=> NUfoV5RjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C2O|Y4PDFpPkOwOlc3PzRzPD;hQi=>
HepG2 MWHGeY5kfGmxbjDhd5NigQ>? MYKzNEB2VQ>? NIDKenZDcW6maX7nJIFn\mmwaYT5JJRwKE6DRkGgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hcHWvYX6gTIVxTzJiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBucXSxY3jvcoRzcWGuIILld5BqemG2aX;uJIF1KDNyIIXN NIm2T209[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEe3NFE2PCd-M{C3O|AyPTR:L3G+
HepG2 NWXZUlkzTnWwY4Tpc44h[XO|YYm= M3vSUVMxKHWP MVHCbY5lcW6pIHHm[olvcXS7IITvJG5CTjFiaX6gbJVu[W5iSHXwS|Ih[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDtbZRw[2ixbnTybYFtKHKnc4DpdoF1cW:wIHH0JFMxKHWP MnfVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB5N{CxOVQoRjNyN{ewNVU1RC:jPh?=
COS7 NXfPVIsyTnWwY4Tpc44h[XO|YYm= M4\0O|M6KGi{cx?= NI\MdZBVemGwc3HjeIl3[XSrb36gc4YhT2GuND3meZNm\CCqdX3hckBRWEGUZ3HtcYEhfHKjboPm[YN1\WRiaX6gR29UPyClZXzsd{Bkdy22cnHud4Zm[3SnZDD3bZRpKHCJQVy1MXRMNXCJTEOgZY5lKHCUZX7ubYxt[S2FTW[gbY5kfWKjdHXkJIZweiB|OTDodpMh[nliZIXhcEBtfWOrZnXyZZNmKHKncH;yeIVzKGG|c3H5MEBGSzVyPUGuOO69VS5? MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTZ2OEGyOUc,OzF4NEixNlU9N2F-
K562 Ml\TSpVv[3Srb36gZZN{[Xl? NXvHTnF[OTBidV2= M{LW[|czKGi{cx?= MnXJTY5lfWO2aX;uJI9nKHOnboPpeIl7[XSrb36geI8hcW2jdHnubYIucW6mdXPl[EBkgXSxdH;4bYNqfHliaX6gbY1ifGmwaXKtdoV{cXO2YX70JIh2dWGwIFu1OlIuUU2DW4LdJINmdGy|IHHzd4V{e2WmIHHzJIlv\HWldHnvckBw\iClZXzsJIRm[XSqIHH0JFExKHWPIHHmeIVzKDd{IHjyd{BqdiCycnXz[Y5k\SCxZjCxJJVOKGmvYYTpcoljKGK7IIDyc5Bq\Gm3bTDpc4Rq\GVxVILpeI9vNVhzMECg[JlmKGKjc3XkJGZCS1NiYX7hcJl{cXN? NXPwcJZ7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{G2OFgyOjVpPkOxOlQ5OTJ3PD;hQi=>

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In vivo

Pioglitazone administered orally (0.3-3 mg/kg/d for 7 days) dose dependently reduces hyperglycemia, hyperlipidemia, and hyperinsulinemia in male fatty rats. Pioglitazone improves glucose tolerance and augmentes the glycemic response to exogenous insulin and clearance of plasma triglyceride in rats. [2] Pioglitazone-treated transgenic mice reveals improved muscle strength and body weight, exhibits a delayed disease onset, and survives significantly longer than nontreated SOD1-G93A mice. [3] Pioglitazone markedly decreases hyperglycemia, hyperlipidemia, hyperinsulinemia, and glucoseintolerance characterized as insulin resistant states in these rats and mice. Pioglitazone potentiates insulin-mediated glucose metabolism in the diaphragm and adipose tissues of yellow KK mice and enhanced the glycemic response to exogenous insulin in Zucker fatty rats. [4] Pioglitazone results in a reduction in the number of activated microglia and reactive astrocytes in the hippocampus and cortex of APPV717I transgenic mice. Pioglitazone decreases beta-secretase-1 (BACE1) mRNA and protein levels in APPV717I transgenic mice. [5]

Protocol

Solubility (25°C)

In vitro DMSO 79 mg/mL (201.06 mM)
Ethanol 4 mg/mL (10.18 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 392.9
Formula

C19H20N2O3S.HCl

CAS No. 112529-15-4
Storage powder
in solvent
Synonyms AD-4833, U-72107E
Smiles CCC1=CN=C(C=C1)CCOC2=CC=C(C=C2)CC3C(=O)NC(=O)S3.Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Step 2: Enter the in vivo formulation ()
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04501406 Recruiting Drug: Pioglitazone|Other: Placebo Type 2 Diabetes Mellitus (T2DM)|Nonalcoholic Steatohepatitis University of Florida|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) December 15 2020 Phase 2
NCT04535700 Recruiting Drug: Pioglitazone 30 mg|Other: standard of care Type 2 Diabetes Fundacion para la Investigacion Biomedica del Hospital Universitario Ramon y Cajal September 18 2020 Phase 4
NCT00904046 Recruiting Drug: Pioglitazone|Drug: Placebo Uric Acid Kidney Stone Disease University of Texas Southwestern Medical Center|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|Takeda Pharmaceuticals North America Inc. September 5 2019 Not Applicable
NCT04671056 Completed Drug: MGL-3196|Drug: Pioglitazone 15mg Healthy Madrigal Pharmaceuticals Inc. November 9 2018 Phase 1
NCT03501277 Completed Drug: Alogliptin|Drug: Pioglitazone|Drug: SYR-322-4833 BL Healthy Volunteers Takeda May 26 2018 Phase 1
NCT03471117 Recruiting Drug: Pioglitazone|Other: Placebo Chronic Kidney Diseases The University of Texas at Arlington|University of Texas Southwestern Medical Center at Dallas April 1 2018 Phase 4

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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P450 (e.g. CYP17) Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID