A-769662

A-769662は一種の有効的で、可逆なAMPK活性剤で、無細胞試験でEC50値が0.8 μMになって、GPPase/FBPaseの活性にほとんど役立ちません。

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A-769662 化学構造
分子量: 360.39

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製品説明

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製品の説明

生物活性

製品説明 A-769662は一種の有効的で、可逆なAMPK活性剤で、無細胞試験でEC50値が0.8 μMになって、GPPase/FBPaseの活性にほとんど役立ちません。
ターゲット

AMPK

Fatty acid synthesis

IC50

0.8 μM

3.2 μM [1]

In vitro試験 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 hepatocytes M1PVfmZ2dmO2aX;uJIF{e2G7 NHn5[WEyKG2P MkDUSG1UVw>? MYXpcohq[mm2czDmZZR1gSCjY3nkJJN6dnSqZYPpd{B4cXSqIFnDOVAhd2ZiMz62JO69VQ>? M3TYZ|E3PzV|NUe2
rat hepatocytes MV;GeY5kfGmxbjDhd5NigQ>? NGKyfJYyKG2P MWjEUXNQ NG\IUlNqdmirYnn0d{Bn[XS2eTDhZ4llKHO7boTo[ZNqeyC5aYToJGlEPTBib3[gN{43KM7:TR?= MVWxOlc2OzV5Nh?=
HEK293 NF3LeFZMcW6jc3WgZZN{[Xl? Ml7kNlAxKM7:TR?= MUnEUXNQ Ml23ZYN1cX[jdHXzJIVv\G:pZX7veZMhSU2SSx?= NGHrUlEyPzd{OEK0NS=>
CCL13 Mn;qT4lv[XOnIHHzd4F6 Mo\PNlAxKM7:TR?= MVLEUXNQ NYq2epV3[WO2aY\heIV{KGWwZH;n[Y5wfXNiQV3QTy=> NV7tTnBqOTd5MkiyOFE>
MEFs MXXGeY5kfGmxbjDhd5NigQ>? Mn;GN|AxKM7:TR?= NFO4T4RFVVOR M2n2NYlvcGmkaYTzJJBzd3SnYYPvcYFtKG[3bnP0bY9vKGK7IHHuJGFOWEtvaX7k[ZBmdmSnboSgcYVkcGGwaYPt NH;GdYsyQDV7M{W4OC=>
epididymal clear cells NFHUW3VHfW6ldHnvckBie3OjeR?= NUj3RYxTOjByIN88US=> NW\tc4pTTE2VTx?= MkPubY5pcWKrdIOgeIhmKHCKLX3l[IlifGWmIG[tRXRR[XOnIHHjZ5VufWyjdHnvckBifCC2aHWgZZBq[2GuIH3lcYJz[W6n M4mxUFE6OjFzOUG4
3T3-L1 NX3IWWJlTnWwY4Tpc44h[XO|YYm= MVKxMlIhdU1? M3PsNGROW09? M{jTfYlvcGmkaYTzJFNVOy2OMTDB[Ilxd2enbnXzbZM> MV:xPVQ5OzNyNB?=
3T3-L1 MVHGeY5kfGmxbjDhd5NigQ>? MYWxMlIhdU1? NHfESWZFVVOR NUfNZlA5cW6qaXLpeJMhfGinIFX4dJJme3Orb36gc4YhSWSrcH;n[Y5me2m|UnXsZZRm\CCWcnHud4NzcXC2aX;uJGZi[3SxcoOgZY5lKE2jcnvldpM> MVmxPVQ5OzNyNB?=
3T3-L1 NILIeIFHfW6ldHnvckBie3OjeR?= NHK3[|UyNjJibV2= NUmwW4RQTE2VTx?= NFnLRnlqdmirYnn0d{BOcXSxdHnjJGNtd26jbDDFfJBidnOrb36= M1;lTlE6PDh|M{C0
3T3-L1 MV3jfZRwfG:6aXPpeJkh[XO|YYm= NYC5TVZUOS5{IH3N NIPydIZFVVOR NV;Yb2U6\GWlcnXhd4V{KEOnbHygWoli[mmuaYT5 NGPYfXoyQTR6M{OwOC=>
3T3-L1 MX7LbY5ie2ViYYPzZZk> MXKxMlIhdU1? NHixOlNFVVOR NIjGPVhi[3SrdnH0[ZMhSU2SSx?= M{fESVE6PDh|M{C0
L6 skeletal muscle cells NF\TVGZHfW6ldHnvckBie3OjeR?= NIXoU40zPTBizszN MVrEUXNQ MYnhZ5RqfmG2ZYOgRW1RUyC|aXfuZYxqdmdicHH0bJdigXN? NFTwRYQyQTh{OEizOi=>
L6 skeletal muscle cells NF3UbVRHfW6ldHnvckBie3OjeR?= NFe1PJkzPTBizszN NFjuZnBFVVOR NIX5ZWxqdmirYnn0d{B1cGViTnGrMWssNUGWUHHz[UB1emGwc4DvdpQh[WO2aY\peJkh[W6mIHPlcIwhe3W{ZnHj[UBi[nWwZHHuZ4U> MmX6NVk5Ojh6M{[=
MDA-MB231 NIi5PVZCeG:ydH;zbZMh[XO|YYm= NWj1RZp{PDByIN88US=> M4LEUmROW09? M{jueZNmdnOrdHn6[ZMhcHWvYX6gZpJm[XO2IHPhcoNmeiClZXzsJIxqdmW|IITvJHRTSUmOLXnu[JVk\WRiYYDvdJRwe2m| NHnKOHQyQTh7NkS2PS=>
BT474 Ml3GRZBweHSxc3nzJIF{e2G7 MmXmOFAxKM7:TR?= MVTEUXNQ NWLsTlNTe2Wwc3n0bZpmeyCqdX3hckBjemWjc4SgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hXFKDSVytbY5lfWOnZDDhdI9xfG:|aYO= MVyxPVg6PjR4OR?=
MCF7 NXLaTHU2SXCxcITvd4l{KGG|c3H5 NHLIS2E1ODBizszN MmXXSG1UVw>? MUTz[Y5{cXSrenXzJIh2dWGwIHLy[YF{fCClYX7j[ZIh[2WubDDsbY5meyC2bzDUVmFKVC2rbnT1Z4VlKGGyb4D0c5Nqew>? M1nwWFE6QDl4NE[5
Mesenchymal stem cells NFXWWVBMcW6jc3WgZZN{[Xl? Mo\ONVAhyrWP NX7nZWhZTE2VTx?= M37nZYlv\HWlZYOgZUBzd2K3c4SgZY5lKHO3c4ThbY5m\CCDTWDLJIFkfGm4YYTpc44> NVPiUGZ[OjRzMES4O|k>
Mesenchymal stem cells NITBdI1kgXSxdH;4bYNqfHliYYPzZZk> MWCxNFAhyrWP NFXzSHJFVVOR NVjkUGlJ\GWlcnXhd4V{KHSqZTDNV2MheHKxbHnm[ZJifGmxbh?= MV:yOFExPDh5OR?=
MG-63 NUDmS|g2[3m2b4TvfIlkcXS7IHHzd4F6 M2OwbFExKML3TR?= MWnEUXNQ NXe1Z3JlcW6qaXLpeJMhUDKRMj3JcoR2[2WmIF;zeIVw[myjc4SgR4VtdCCGZXH0bC=> MXyyOFk3ODN4Mh?=
MC3T3-E1 NVjKTY9l[3m2b4TvfIlkcXS7IHHzd4F6 M1TyUFExKML3TR?= MWDEUXNQ MYDpcohq[mm2czDINm8zNUmwZIXj[YQhV3O2ZX;icIF{fCCFZXzsJGRm[XSq NEKyWG0zPDl4MEO2Ni=>
MG-63 M2i2ZmFxd3C2b4Ppd{Bie3OjeR?= MkLHNVAhyrWP M1LGe2ROW09? NVXLfZhte3WycILld5NmeyCKMl:yMWlv\HWlZXSgU5N1\W:kbHHzeEBE\WyuIFHwc5B1d3Orcx?= M{PaUlI1QTZyM{[y
MC3T3-E1 M4W5fmFxd3C2b4Ppd{Bie3OjeR?= NEHpTmQyOCEEtV2= NUToNWRNTE2VTx?= MUTzeZBxemW|c3XzJGgzVzJvSX7keYNm\CCRc4Tlc4Jt[XO2IFPlcIwhSXCxcITvd4l{ NUPtNmpZOjR7NkCzOlI>
MG-63 M170XmZ2dmO2aX;uJIF{e2G7 NH31cmsyOCEEtV2= MVvEUXNQ NVzhXFhU[WyuZY\pZZRmeyCUT2OgZYNkfW23bHH0bY9vKGGwZDDBWHAh\GWybHX0bY9vKGOjdYPl[EBjgSCKMl:y M3rMS|I1QTZyM{[y
MC3T3-E1 MmHDSpVv[3Srb36gZZN{[Xl? M2PBXFExKML3TR?= MYXEUXNQ MULhcIxmfmmjdHXzJHJQWyCjY3P1cZVt[XSrb36gZY5lKEGWUDDk[ZBt\XSrb36gZ4F2e2WmIHL5JGgzVzJ? M3nxRlI1QTZyM{[y
MG-63 NVfKRZBsTnWwY4Tpc44h[XO|YYm= M{T0fFExKML3TR?= NY[wSJdSTE2VTx?= NHXzdZdn[WOrbHn0ZZRmeyCKMl:yMYlv\HWlZXSgZZV1d3CqYXf5JIFkfGm4YYTpc44> M1z2SVI1QTZyM{[y
MC3T3-E1 M{f4fGZ2dmO2aX;uJIF{e2G7 NYjzZWxFOTBiwsXN M1vwNGROW09? MoHK[oFkcWyrdHH0[ZMhUDKRMj3pcoR2[2WmIHH1eI9xcGGpeTDhZ5RqfmG2aX;u NXmyZYVEOjR7NkCzOlI>
PC3 M1G4OmtqdmG|ZTDhd5NigQ>? NHuweHMyODBiwsXN NFfCcHJFVVOR MYX1dJJm\3WuYYTld{B1cGVibHX2[Yx{KG:oIFHNVGsh[W6mIFHDR{BxcG:|cHjvdplt[XSrb36= NWHtTGxUOjV3OUSwOFM>
PC3M NYT4[mNRU2mwYYPlJIF{e2G7 MXSxNFAhyrWP NFfPWmFFVVOR NVLiOYgyfXC{ZXf1cIF1\XNidHjlJIxmfmWuczDv[kBCVVCNIHHu[EBCS0NicHjvd5Bpd3K7bHH0bY9v M2S1b|I2PTl2MESz
PC3 MnHvSpVv[3Srb36gZZN{[Xl? M1j4[VExOCEEtV2= MW\EUXNQ NGHmS2FqdmS3Y3XzJHBKO0txbWTPVkBx[XSqd3H5dy=> NXz4OW5{OjV3OUSwOFM>
PC3M NVvlWGRoTnWwY4Tpc44h[XO|YYm= M2HsS|ExOCEEtV2= Mn\RSG1UVw>? MoPjbY5lfWOnczDQTVNMN22WT2KgdIF1cHejeYO= MY[yOVU6PDB2Mx?=
PC3 NGC0fpVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXSxNFAhyrWP M3rsVGROW09? NUTMWoY4e3WycILld5NmeyCycn;sbYZmemG2aX;u M{\HSVI2PTl2MESz
PC3M M{G5Tmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGn3VGwyODBiwsXN MoLJSG1UVw>? NEXmSpJ{fXCycnXzd4V{KHC{b3zp[oVz[XSrb36= NWLB[ZhQOjV3OUSwOFM>
MC3T3-E1 M1vUeGtqdmG|ZTDhd5NigQ>? M1j3[|ExKM7:TR?= MV3EUXNQ MYLpcoR2[2W|IIPp[45q\mmlYX70JGFOWEtiYXP0bZZifGmxbh?= NWXESJU3OjZ6OUG4OlY>
MC3T3-E1 MkLFS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NX;tc4o6OTBizszN MXTEUXNQ NFXEWoNqdmirYnn0d{BF\XhvaX7keYNm\CCxc4Tlc4Jt[XO2IHPlcIwh\GWjdHi= MUWyOlg6OTh4Nh?=
MC3T3-E1 NYXEVFc5TnWwY4Tpc44h[XO|YYm= MofPNVAh|ryP NV:5Rm9YTE2VTx?= MnHNbY5pcWKrdIOgSIV5NWmwZIXj[YQhd3irZHH0bZZmKHO2cnXzdy=> NHHuPWYzPjh7MUi2Oi=>

... Click to View More Cell Line Experimental Data

In vivo試験 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]
臨床試験
特集

プロトコル (参考用のみ)

キナーゼアッセイ:

[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.

細胞アッセイ:

[3]

細胞株 MEF cells
濃度 300 μM
反応時間 24 hours
実験の流れ

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.

動物実験:

[1]

動物モデル Sprague Dawley rats
製剤 A-769662 is dissolved in DMSO.
投薬量 30 mg/kg
投与方法 Administered via i.p.

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

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
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

参考

化学情報

Download A-769662 SDF
分子量 360.39
化学式

C20H12N2O3S

CAS No. 844499-71-4
保管 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 72 mg/mL (199.78 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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.
化学名 Thieno[2,3-b]pyridine-5-carbonitrile, 6,7-dihydro-4-hydroxy-3-(2'-hydroxy[1,1'-biphenyl]-4-yl)-6-oxo-

文献中の引用 (6)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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