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0.8μMのEC50による強力な、可逆的なAMPを起動するプロテインキナーゼ(AMPK)活性剤で、3.2μMでIC50で脂肪酸合成を禁止します。
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 MWHGeY5kfGmxbjDhd5NigQ>? NGjn[2YyKG2P M{Dn[mROW09? MmG3bY5pcWKrdIOg[oF1fHliYXPp[EB{gW62aHXzbZMhf2m2aDDJR|UxKG:oIEOuOkDPxE1? NFTWfpUyPjd3M{W3Oi=>
rat hepatocytes M1mzVWZ2dmO2aX;uJIF{e2G7 NIT1N3kyKG2P MX\EUXNQ MUTpcohq[mm2czDmZZR1gSCjY3nkJJN6dnSqZYPpd{B4cXSqIFnDOVAhd2ZiMz62JO69VQ>? NF;UN2EyPjd3M{W3Oi=>
HEK293 MonZT4lv[XOnIHHzd4F6 NVjRelhGOjByIN88US=> MYLEUXNQ NIGzV5Vi[3SrdnH0[ZMh\W6mb3flco92eyCDTWDL MXGxO|czQDJ2MR?=
CCL13 NF\KRphMcW6jc3WgZZN{[Xl? M1rtd|IxOCEQvF2= MlLxSG1UVw>? MVHhZ5RqfmG2ZYOg[Y5ld2enbn;1d{BCVVCN MVKxO|czQDJ2MR?=
MEFs NUL5Ump[TnWwY4Tpc44h[XO|YYm= NWi0SlNJOzByIN88US=> Moi3SG1UVw>? NGe1Z49qdmirYnn0d{Bxem:2ZXHzc41idCCodX7jeIlwdiCkeTDhckBCVVCNLXnu[IVx\W6mZX70JI1m[2ijbnnzcS=> NGn1VYkyQDV7M{W4OC=>
epididymal clear cells NHzl[W9HfW6ldHnvckBie3OjeR?= NE\NcoczODBizszN MkLiSG1UVw>? NETaNmpqdmirYnn0d{B1cGVicFitcYVlcWG2ZXSgWk1CXFCjc3WgZYNkfW23bHH0bY9vKGG2IITo[UBieGmlYXygcYVu[nKjbnW= M2DSNVE6OjFzOUG4
3T3-L1 MYPGeY5kfGmxbjDhd5NigQ>? NXvscZJOOS5{IH3N NUfJ[ldoTE2VTx?= MUjpcohq[mm2czCzWFMuVDFiQXTpdI9o\W6nc3nz NYLBPFRnOTl2OEOzNFQ>
3T3-L1 NUS0RoUzTnWwY4Tpc44h[XO|YYm= M3HZWFEvOiCvTR?= MWLEUXNQ MmLxbY5pcWKrdIOgeIhmKEW6cILld5Nqd25ib3[gRYRqeG:pZX7ld4l{WmWuYYTl[EBVemGwc3PybZB1cW:wIF\hZ5RwenNiYX7kJG1iemuncoO= Mn7HNVk1QDN|MES=
3T3-L1 NH7mSGZHfW6ldHnvckBie3OjeR?= Ml21NU4zKG2P MVjEUXNQ MUHpcohq[mm2czDNbZRwfGmlIFPsc45idCCHeIDhcpNqd25? NWn0SpBKOTl2OEOzNFQ>
3T3-L1 MlPYZ5l1d3SxeHnjbZR6KGG|c3H5 MnjrNU4zKG2P NUnxXFZXTE2VTx?= M1P2O4Rm[3KnYYPld{BE\WyuIG\pZYJqdGm2eR?= MWixPVQ5OzNyNB?=
3T3-L1 MX7LbY5ie2ViYYPzZZk> M2\wclEvOiCvTR?= NWjoZWlpTE2VTx?= M3XHW4FkfGm4YYTld{BCVVCN NIrFZlEyQTR6M{OwOC=>
L6 skeletal muscle cells MXzGeY5kfGmxbjDhd5NigQ>? M{K3bFI2OCEQvF2= MYnEUXNQ NU\HfWlR[WO2aY\heIV{KEGPUFugd4lodmGuaX7nJJBifGi5YYnz NYjPOGY2OTl6Mki4N|Y>
L6 skeletal muscle cells NVG0ZphXTnWwY4Tpc44h[XO|YYm= MkDoNlUxKM7:TR?= NGPxSFVFVVOR MWLpcohq[mm2czD0bIUhVmFtLVurMWFVWGG|ZTD0doFve3CxcoSgZYN1cX[rdImgZY5lKGOnbHygd5Vz\mGlZTDhZpVv\GGwY3W= M3Lv[lE6QDJ6OEO2
MDA-MB231 NGTLSYVCeG:ydH;zbZMh[XO|YYm= M37pTVQxOCEQvF2= MXrEUXNQ MlPNd4Vve2m2aYrld{BpfW2jbjDidoVie3RiY3HuZ4VzKGOnbHygcIlv\XNidH:gWHJCUUxvaX7keYNm\CCjcH;weI9{cXN? MYmxPVg6PjR4OR?=
BT474 MX;BdI9xfG:|aYOgZZN{[Xl? M{TidVQxOCEQvF2= M2rBWWROW09? M1PTW5NmdnOrdHn6[ZMhcHWvYX6gZpJm[XO2IHPhcoNmeiClZXzsJIxqdmW|IITvJHRTSUmOLXnu[JVk\WRiYYDvdJRwe2m| Ml;SNVk5QTZ2Nkm=
MCF7 M2e1fGFxd3C2b4Ppd{Bie3OjeR?= NFjV[Iw1ODBizszN M4LUS2ROW09? M{L2d5NmdnOrdHn6[ZMhcHWvYX6gZpJm[XO2IHPhcoNmeiClZXzsJIxqdmW|IITvJHRTSUmOLXnu[JVk\WRiYYDvdJRwe2m| MUWxPVg6PjR4OR?=
Mesenchymal stem cells NGq0W|lMcW6jc3WgZZN{[Xl? MXKxNEDDvU1? NWXCPGMxTE2VTx?= NInTcWVqdmS3Y3XzJIEhem:kdYP0JIFv\CC|dYP0ZYlv\WRiQV3QT{Bi[3SrdnH0bY9v NHjRcFEzPDFyNEi3PS=>
Mesenchymal stem cells NUXPUHc2[3m2b4TvfIlkcXS7IHHzd4F6 M4LXXVExOCEEtV2= NVO1N|V1TE2VTx?= NYnaemlv\GWlcnXhd4V{KHSqZTDNV2MheHKxbHnm[ZJifGmxbh?= M1\mSlI1OTB2OEe5
MG-63 MojvZ5l1d3SxeHnjbZR6KGG|c3H5 NEPjPJAyOCEEtV2= NEWxOIlFVVOR MXLpcohq[mm2czDINm8zNUmwZIXj[YQhV3O2ZX;icIF{fCCFZXzsJGRm[XSq Mn7tNlQ6PjB|NkK=
MC3T3-E1 Ml\4Z5l1d3SxeHnjbZR6KGG|c3H5 MkfFNVAhyrWP NVzsU2g3TE2VTx?= M1HJU4lvcGmkaYTzJGgzVzJvSX7keYNm\CCRc4Tlc4Jt[XO2IFPlcIwhTGWjdHi= MXuyOFk3ODN4Mh?=
MG-63 MYHBdI9xfG:|aYOgZZN{[Xl? MoHiNVAhyrWP MXLEUXNQ NULMRYJwe3WycILld5NmeyCKMl:yMWlv\HWlZXSgU5N1\W:kbHHzeEBE\WyuIFHwc5B1d3Orcx?= MViyOFk3ODN4Mh?=
MC3T3-E1 NHvWZldCeG:ydH;zbZMh[XO|YYm= MmHpNVAhyrWP M4HCSWROW09? MlfCd5VxeHKnc4Pld{BJOk9{LVnu[JVk\WRiT4P0[Y9jdGG|dDDD[YxtKEGyb4D0c5Nqew>? MlOwNlQ6PjB|NkK=
MG-63 NHjYNnZHfW6ldHnvckBie3OjeR?= NF\Jb|EyOCEEtV2= NETHWo1FVVOR NGCz[HNidGyndnnheIV{KFKRUzDhZ4N2dXWuYYTpc44h[W6mIFHUVEBl\XCuZYTpc44h[2G3c3XkJIJ6KEh{T{K= NXXaNWs4OjR7NkCzOlI>
MC3T3-E1 MVvGeY5kfGmxbjDhd5NigQ>? MlzWNVAhyrWP M3i4ZmROW09? M1vje4FtdGW4aXH0[ZMhWk:VIHHjZ5VufWyjdHnvckBidmRiQWTQJIRmeGyndHnvckBk[XW|ZXSgZpkhUDKRMh?= MV[yOFk3ODN4Mh?=
MG-63 NFuyPHhHfW6ldHnvckBie3OjeR?= NFrkOXAyOCEEtV2= MUDEUXNQ NI\BUodn[WOrbHn0ZZRmeyCKMl:yMYlv\HWlZXSgZZV1d3CqYXf5JIFkfGm4YYTpc44> NYnkdHI2OjR7NkCzOlI>
MC3T3-E1 MkW4SpVv[3Srb36gZZN{[Xl? M4\UO|ExKML3TR?= NGnlUVdFVVOR MX7mZYNqdGm2YYTld{BJOk9{LXnu[JVk\WRiYYX0c5Bp[We7IHHjeIl3[XSrb36= NXrQS4IxOjR7NkCzOlI>
PC3 MUTLbY5ie2ViYYPzZZk> NX\zcGpTOTByINM1US=> MWTEUXNQ NV;tcVV3fXC{ZXf1cIF1\XNidHjlJIxmfmWuczDv[kBCVVCNIHHu[EBCS0NicHjvd5Bpd3K7bHH0bY9v MX6yOVU6PDB2Mx?=
PC3M MkLNT4lv[XOnIHHzd4F6 NFXuS|MyODBiwsXN M3L5WmROW09? NGf5d|l2eHKnZ4XsZZRmeyC2aHWgcIV3\Wy|IH;mJGFOWEtiYX7kJGFESyCyaH;zdIhwenmuYYTpc44> NV[5fWlyOjV3OUSwOFM>
PC3 M{LGSmZ2dmO2aX;uJIF{e2G7 M2L0NlExOCEEtV2= M{n6N2ROW09? MXPpcoR2[2W|IGDJN2swdVSRUjDwZZRpf2G7cx?= NHPhdpMzPTV7NEC0Ny=>
PC3M NEXhSnNHfW6ldHnvckBie3OjeR?= NXTO[ZQ{OTByINM1US=> M{LoSWROW09? Mn7vbY5lfWOnczDQTVNMN22WT2KgdIF1cHejeYO= MmXhNlU2QTRyNEO=
PC3 MljjS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFznWlQyODBiwsXN MXPEUXNQ MlnPd5VxeHKnc4Pld{Bxem:uaX\ldoF1cW:w NGW1T4QzPTV7NEC0Ny=>
PC3M MonBS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MonQNVAxKML3TR?= Mli3SG1UVw>? MXfzeZBxemW|c3XzJJBzd2yrZnXyZZRqd25? MWqyOVU6PDB2Mx?=
MC3T3-E1 NHv6O4hMcW6jc3WgZZN{[Xl? MWmxNEDPxE1? MoPmSG1UVw>? MYXpcoR2[2W|IIPp[45q\mmlYX70JGFOWEtiYXP0bZZifGmxbh?= M4XrdVI3QDlzOE[2
MC3T3-E1 M1rqVmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1\ROlExKM7:TR?= NW\Fb5BuTE2VTx?= M1TqUYlvcGmkaYTzJGRmgC2rbnT1Z4VlKG:|dHXvZoxie3RiY3XscEBl\WG2aB?= NV\YWGRTOjZ6OUG4OlY>
MC3T3-E1 Mn[xSpVv[3Srb36gZZN{[Xl? MUKxNEDPxE1? NGP0[3NFVVOR M1;VZYlvcGmkaYTzJGRmgC2rbnT1Z4VlKG:6aXTheIl3\SC|dILld5M> MVKyOlg6OTh4Nh?=

... 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 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 72 mg/mL (199.78 mM)
<1 mg/mL (<1 mM)
エタノール <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.
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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