A-769662

Catalog No.S2697

A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM in cell-free assays, little effect on GPPase/FBPase activity.

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A-769662 Chemical Structure

A-769662 Chemical Structure
Molecular Weight: 360.39

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Product Description

Biological Activity

Description A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM in cell-free assays, little effect on GPPase/FBPase activity.
Targets AMPK [1]
(Cell-free assay)
Fatty acid synthesis [1]
(Cell-free assay)
IC50 0.8 μM(EC50) 3.2 μM
In vitro A-769662 stimulates partially purified rat liver AMPK with EC50 with 0.8 μM. A-769662 activates AMPK purified from multiple tissues and species in a dose-responsive manner with modest variations in observed EC50s. EC50s determined for A-769662 using partially purified AMPK extracts from rat heart, rat muscle, or human embryonic kidney cells (HEKs) are 2.2 mM, 1.9 mM, or 1.1 mM, respectively. A 4 hours treatment of primary rat hepatocytes with A-769662 dose-dependently increases ACC phosphorylation, which correlated inhibition of fatty acid synthesis with IC50 of 3.2 μM. A-769662 also inhibits fatty acid sythesis in mouse hepatocytes with IC50 with 3.6 μM [1] A-769662 activates AMPK both allosterically and by inhibiting dephosphorylation of AMPK on Thr-172, similar to the effects of AMP. [2] A-769662 inhibits proteasomal function by an AMPK-independent mechanism. A-769662 affects the in vitro activity of purified 26S proteasomes but not the in vitro activity of purified 20S proteasomes. A-769662 has toxic effects on MEF cells. [3] A recent research shows A-769662 inhibited cell proliferation and DNA synthesis. [4]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
mouse hepatocytesNXTVT3hQTnWwY4Tpc44h[XO|YYm=NXvt[FI5OSCvTR?=NXfDXppjTE2VTx?=M{LIV4lvcGmkaYTzJIZifHS7IHHjbYQhe3mwdHjld4l{KHerdHigTWM2OCCxZjCzMlYh|ryPMlL2NVY4PTN3N{[=
rat hepatocytesNVPMRYpNTnWwY4Tpc44h[XO|YYm=M3zvNVEhdU1?M1L6UGROW09?NXfHdWV{cW6qaXLpeJMh\mG2dImgZYNq\CC|eX70bIV{cXNid3n0bEBKSzVyIH;mJFMvPiEQvF2=Mn\rNVY4PTN3N{[=
HEK293MlzXT4lv[XOnIHHzd4F6NUXBR2xqOjByIN88US=>Mm\6SG1UVw>?NGDRUY1i[3SrdnH0[ZMh\W6mb3flco92eyCDTWDLMWGxO|czQDJ2MR?=
CCL13NWizXXM5U2mwYYPlJIF{e2G7M4PqcFIxOCEQvF2=NFfkNWhFVVORMUfhZ5RqfmG2ZYOg[Y5ld2enbn;1d{BCVVCNMV6xO|czQDJ2MR?=
MEFsNGD0[HRHfW6ldHnvckBie3OjeR?=NHK3SlY{ODBizszNM3\PfGROW09?NU\lcXlRcW6qaXLpeJMheHKxdHXhd49u[WxiZoXuZ5Rqd25iYomgZY4hSU2SSz3pcoRmeGWwZHXueEBu\WOqYX7pd40>MnPzNVg2QTN3OES=
epididymal clear cellsNHrBOYlHfW6ldHnvckBie3OjeR?=MonDNlAxKM7:TR?=NXjBOIpjTE2VTx?=NU\ZSHNPcW6qaXLpeJMhfGinIIDIMY1m\GmjdHXkJHYuSVSSYYPlJIFk[3WvdXzheIlwdiCjdDD0bIUh[XCrY3HsJI1mdWK{YX7lNWnHPIVXOTl{MUG5NVg>
3T3-L1NVHN[nlqTnWwY4Tpc44h[XO|YYm=MY[xMlIhdU1?M{HTV2ROW09?MljGbY5pcWKrdIOgN3Q{NUxzIFHkbZBw\2WwZYPpdy=>NFnRc4MyQTR6M{OwOC=>
3T3-L1NYPJTJJQTnWwY4Tpc44h[XO|YYm=M4rwZlEvOiCvTR?=NVf0fJJoTE2VTx?=NYPyXHRocW6qaXLpeJMhfGinIFX4dJJme3Orb36gc4YhSWSrcH;n[Y5me2m|UnXsZZRm\CCWcnHud4NzcXC2aX;uJGZi[3SxcoOgZY5lKE2jcnvldpM>MYGxPVQ5OzNyNB?=
3T3-L1MnfWSpVv[3Srb36gZZN{[Xl?MVqxMlIhdU1?MVLEUXNQNIDKdGFqdmirYnn0d{BOcXSxdHnjJGNtd26jbDDFfJBidnOrb36=NWC1PZI4OTl2OEOzNFQ>
3T3-L1NVLaSnA2[3m2b4TvfIlkcXS7IHHzd4F6NFGy[GMyNjJibV2=NX6zNXQ1TE2VTx?=MmXt[IVkemWjc3XzJGNmdGxiVnnhZoltcXS7M1GyVFE6PDh|M{C0
3T3-L1NEfO[VhMcW6jc3WgZZN{[Xl?MlT3NU4zKG2PMlnSSG1UVw>?NETvdJpi[3SrdnH0[ZMhSU2SSx?=M{np[lE6PDh|M{C0
L6 skeletal muscle cellsNWH0eXNLTnWwY4Tpc44h[XO|YYm=NHfLRnEzPTBizszNNGTKXFdFVVORMn3WZYN1cX[jdHXzJGFOWEtic3nncoFtcW6pIIDheIh4[Xm|NX\KWYNyOTl6Mki4N|Y>
L6 skeletal muscle cellsM{KwbWZ2dmO2aX;uJIF{e2G7MnrINlUxKM7:TR?=MULEUXNQMXPpcohq[mm2czD0bIUhVmFtLVurMWFVWGG|ZTD0doFve3CxcoSgZYN1cX[rdImgZY5lKGOnbHygd5Vz\mGlZTDhZpVv\GGwY3W=M2CwWlE6QDJ6OEO2
MDA-MB231NWXjOYwzSXCxcITvd4l{KGG|c3H5MWC0NFAh|ryPMVnEUXNQMnTPd4Vve2m2aYrld{BpfW2jbjDidoVie3RiY3HuZ4VzKGOnbHygcIlv\XNidH:gWHJCUUxvaX7keYNm\CCjcH;weI9{cXN?NFvOS3MyQTh7NkS2PS=>
BT474M1\oW2Fxd3C2b4Ppd{Bie3OjeR?=MlTzOFAxKM7:TR?=NE\ROpBFVVORNV7pb21Se2Wwc3n0bZpmeyCqdX3hckBjemWjc4SgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hXFKDSVytbY5lfWOnZDDhdI9xfG:|aYO=NWPZTI1sOTl6OU[0Olk>
MCF7Mnz3RZBweHSxc3nzJIF{e2G7MonmOFAxKM7:TR?=NVXFcpRvTE2VTx?=M{iye5NmdnOrdHn6[ZMhcHWvYX6gZpJm[XO2IHPhcoNmeiClZXzsJIxqdmW|IITvJHRTSUmOLXnu[JVk\WRiYYDvdJRwe2m|NYjFfFFzOTl6OU[0Olk>
Mesenchymal stem cellsMYHLbY5ie2ViYYPzZZk>M2T5Z|ExKML3TR?=MVTEUXNQNUXxXIpzcW6mdXPld{BiKHKxYoXzeEBidmRic4XzeIFqdmWmIFHNVGsh[WO2aY\heIlwdg>?NWrYV2pPOjRzMES4O|k>
Mesenchymal stem cellsM2rNWYN6fG:2b4jpZ4l1gSCjc4PhfS=>NXn3WoF3OTByINM1US=>MkHZSG1UVw>?MXPk[YNz\WG|ZYOgeIhmKE2VQzDwdo9tcW[ncnH0bY9vMV6yOFExPDh5OR?=
MG-63M1\sToN6fG:2b4jpZ4l1gSCjc4PhfS=>MWixNEDDvU1?NEXuUWtFVVORMmLLbY5pcWKrdIOgTFJQOi2LbnT1Z4VlKE:|dHXvZoxie3RiQ3XscEBF\WG2aB?=NELlWJEzPDl4MEO2Ni=>
MC3T3-E1NYOzRY8{[3m2b4TvfIlkcXS7IHHzd4F6MljqNVAhyrWPNUTlS4VOTE2VTx?=M4GxcYlvcGmkaYTzJGgzVzJvSX7keYNm\CCRc4Tlc4Jt[XO2IFPlcIwhTGWjdHi=MWiyOFk3ODN4Mh?=
MG-63NYnRcYFpSXCxcITvd4l{KGG|c3H5MnjYNVAhyrWPMnrvSG1UVw>?M1zMNJN2eHC{ZYPz[ZMhUDKRMj3JcoR2[2WmIF;zeIVw[myjc4SgR4VtdCCDcH;weI9{cXN?MkPpNlQ6PjB|NkK=
MC3T3-E1MnrrRZBweHSxc3nzJIF{e2G7MUmxNEDDvU1?MXnEUXNQM4C3[5N2eHC{ZYPz[ZMhUDKRMj3JcoR2[2WmIF;zeIVw[myjc4SgR4VtdCCDcH;weI9{cXN?NY\hR2o2OjR7NkCzOlI>
MG-63M4XYdWZ2dmO2aX;uJIF{e2G7MYKxNEDDvU1?NVLUN4dyTE2VTx?=NUD2fpY2[WyuZY\pZZRmeyCUT2OgZYNkfW23bHH0bY9vKGGwZDDBWHAh\GWybHX0bY9vKGOjdYPl[EBjgSCKMl:yM1fDN|I1QTZyM{[y
MC3T3-E1NG\YRpJHfW6ldHnvckBie3OjeR?=NUjYU25oOTBiwsXNNEPYeXVFVVORMkT1ZYxt\X[rYYTld{BTV1NiYXPjeY12dGG2aX;uJIFv\CCDVGCg[IVxdGW2aX;uJINifXOnZDDifUBJOk9{MXSyOFk3ODN4Mh?=
MG-63M{\DWWZ2dmO2aX;uJIF{e2G7NVftT4RuOTBiwsXNNHviOWJFVVORMYnmZYNqdGm2YYTld{BJOk9{LXnu[JVk\WRiYYX0c5Bp[We7IHHjeIl3[XSrb36=MnPONlQ6PjB|NkK=
MC3T3-E1NWXRcnF[TnWwY4Tpc44h[XO|YYm=MknRNVAhyrWPNEnGNI5FVVORMWnmZYNqdGm2YYTld{BJOk9{LXnu[JVk\WRiYYX0c5Bp[We7IHHjeIl3[XSrb36=M4rzTlI1QTZyM{[y
PC3MV7LbY5ie2ViYYPzZZk>NVHXbW1QOTByINM1US=>NH:yfJlFVVORM2XrbJVxemWpdXzheIV{KHSqZTDs[ZZmdHNib3[gRW1RUyCjbnSgRWNEKHCqb4PwbI9zgWyjdHnvci=>Mlv6NlU2QTRyNEO=
PC3MMkfvT4lv[XOnIHHzd4F6NGfyNXUyODBiwsXNNV;kSllGTE2VTx?=MUX1dJJm\3WuYYTld{B1cGVibHX2[Yx{KG:oIFHNVGsh[W6mIFHDR{BxcG:|cHjvdplt[XSrb36=NXTEUGQ3OjV3OUSwOFM>
PC3Ml\GSpVv[3Srb36gZZN{[Xl?M1P4c|ExOCEEtV2=M1TVbmROW09?MVjpcoR2[2W|IGDJN2swdVSRUjDwZZRpf2G7cx?=NHn3Z4wzPTV7NEC0Ny=>
PC3MM1\wbGZ2dmO2aX;uJIF{e2G7M{OzfFExOCEEtV2=MorQSG1UVw>?MYDpcoR2[2W|IGDJN2swdVSRUjDwZZRpf2G7cx?=NHLxfpYzPTV7NEC0Ny=>
PC3Mn;iS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?M3Xjc|ExOCEEtV2=MlThSG1UVw>?Mli4d5VxeHKnc4Pld{Bxem:uaX\ldoF1cW:wMUSyOVU6PDB2Mx?=
PC3MM2fkZ2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7Ml:xNVAxKML3TR?=MVvEUXNQMmjnd5VxeHKnc4Pld{Bxem:uaX\ldoF1cW:wMnrrNlU2QTRyNEO=
MC3T3-E1NUDT[WFKU2mwYYPlJIF{e2G7M1PqblExKM7:TR?=NFPHbGFFVVORNWnqNmF4cW6mdXPld{B{cWewaX\pZ4FvfCCDTWDLJIFkfGm4YYTpc44>MmjBNlY5QTF6Nk[=
MC3T3-E1NXyzSnpqT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm=MVGxNEDPxE1?MUfEUXNQNEfWOXhqdmirYnn0d{BF\XhvaX7keYNm\CCxc4Tlc4Jt[XO2IHPlcIwh\GWjdHi=M3nud|I3QDlzOE[2
MC3T3-E1MUjGeY5kfGmxbjDhd5NigQ>?MkXnNVAh|ryPMYrEUXNQNVPrRXQzcW6qaXLpeJMhTGW6LXnu[JVk\WRib4jp[IF1cX[nIIP0doV{ew>?MUCyOlg6OTh4Nh?=

... Click to View More Cell Line Experimental Data

In vivo Short-term treatment of normal Sprague Dawley rats with A-769662 decreases liver malonyl CoA levels and the respiratory exchange ratio, VCO2/VO2, indicating an increased rate of whole-body fatty acid oxidation. Treatment of ob/ob mice with 30 mg/kg b.i.d. A-769662 decreases hepatic expression of PEPCK, G6Pase, and FAS, lowers plasma glucose by 40%, reduced body weight gain and significantly decreases both plasma and liver triglyceride levels. [1]
Features

Protocol(Only for Reference)

Kinase Assay:

[1]

96-well AMPK assay AMPK activity is measured by monitoring phosphorylation of the SAMS peptide substrate (20 mM in standard assays and 100 mM in additivity assays) following a previously described protocol (Anderson et al., 2004). To determine whether A-769662-induced AMPK activation occurs in a reversible manner, AMP or A-769662 are preincubated with rat liver AMPK for 10 minutes at 20 times standard assay concentrations prior to dilution and measurement of AMPK activity.
Fatty Acid Synthesis Assay Primary rat hepatocytes are isolated and plated at 5 × 104 cells per well on BioCoat, collagen-coated, black-walled 96-well plates in DMEM supplemented with 10% FBS, 5 mM glucose, 1 mM sodium pyruvate, 2 mM L-glutamine, 25 mM HEPES, 0.1 m M nonessential amino acids, 5 μg/ml transferrin, 100 nM dexamethasone, 100 nM insulin and 25 μg/ml gentamycin. After 4 hr medium is replaced with medium as described above but without FBS and containing 100 nM triiodothyronine (T3). Following a 16 hr, 37°C incubation, the incubation medium is removed and replaced with medium containing 14C acetate (2 μCi/ml) and AICAR or test compounds at the indicated concentrations. Cells are incubated 4 hr at 37°C then the plates are rinsed with PBS. The final wash is replaced with Microscint20 and radioactivity incorporated into fatty acid monitors on a Wallac Microbeta plate reader.

Cell Assay:

[3]

Cell lines MEF cells
Concentrations 300 μM
Incubation Time 24 hours
Method

Cell viability of MEF cells treated or not with A-769662 is performed as follows: cells are harvested by trypsinization and incubated with 0.5 mg/mL RNase and 50 μg/mL propidium iodine at room temperature in the dark; cell viability is analyzed by flow cytometry using a FACScanto flow cytometer, using an excitation laser at 488 nm and a propidium iodine fluorescence detection at 600 nm. To determine the proportion of cells in each phase of the cell cycle, cells are harvested by trypsinization, collected by centrifugation, washed in PBS and fixed overnight in 80% ethanol at -20 °C. Subsequently, these fixed cells are centrifuged to remove the fixative and incubated for 20 minutes in the dark at room temperature in PBS containing 0.5 mg/mL RNase and 50 μg/mL propidium iodine. Flow cytometry analysis is performed as above. The proportion of cells in G1, S, and G2 is determined using the MODFIT program. Cell culture pictures are taken at the indicated times using a camera coupled to an inverted microscope with a 20 × objective.

Animal Study:

[1]

Animal Models Sprague Dawley rats
Formulation A-769662 is dissolved in DMSO.
Dosages 30 mg/kg
Administration Administered via i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Cool B, et al, Cell Metab, 2006, 3(6), 403-416.

[2] Sanders MJ, J Biol Chem, 2007, 282(45), 32539-32548.

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Chemical Information

Download A-769662 SDF
Molecular Weight (MW) 360.39
Formula

C20H12N2O3S

CAS No. 844499-71-4
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 72 mg/mL (199.78 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 30 mg/mL
* <1 mg/ml means slightly soluble or 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 Name Thieno[2,3-b]pyridine-5-carbonitrile, 6,7-dihydro-4-hydroxy-3-(2'-hydroxy[1,1'-biphenyl]-4-yl)-6-oxo-

Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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