Amiloride (MK-870) HCl

Catalog No.S1811

For research use only.

Amiloride (MK-870) is a selective T-type calcium channel blocker, an epithelial sodium channel blocker and a selective inhibitor of urokinase plasminogen activator (uPA)(Ki=7 μM).

Amiloride (MK-870) HCl Chemical Structure

CAS No. 2016-88-8

Selleck's Amiloride (MK-870) HCl has been cited by 14 publications

Purity & Quality Control

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Biological Activity

Description Amiloride (MK-870) is a selective T-type calcium channel blocker, an epithelial sodium channel blocker and a selective inhibitor of urokinase plasminogen activator (uPA)(Ki=7 μM).
Targets
Sodium channel [1] T-type calcium channel [2] uPA [3]
7 μM(Ki)
In vitro

Amiloride is a relatively selective inhibitor of the epithelial sodium channel (ENaC) with an IC50 (the concentration required to reach 50% inhibition of an ion channel) in the concentration range of 0.1 to 0.5 μM. Amiloride is a relatively poor inhibitor of the the Na+/H+ exchanger (NHE) with an IC50 as low as 3 μM in the presence of a low external [Na+] but as high as 1 mM in the presence of a high [Na+]. Amiloride is an even weaker inhibitor of the Na+/Ca2+ exchanger (NCX), with an IC50 of 1 mM. Amiloride (1 μM) and submicromolar doses of Benzamil (30 nM), doses known to inhibit the ENaC, inhibit the myogenic vasoconstriction response to increasing perfusion pressure by blocking the activity of ENaC proteins. Amiloride completely inhibits Na+ influx in doses known to be relatively specific for ENaC (1.5 μM) in vascular smooth muscle cells (VSMC). [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
D17 MYTD[YxtKH[rYXLpcIl1gSCjc4PhfS=> MXy3NkBp MUTJR|UxRTFzMD62OkDPxE1? NYDsd4w2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C1OVYyPzhpPkOwOVU3OTd6PD;hQi=>
Abrams MofHR4VtdCC4aXHibYxqfHliYYPzZZk> M4O5fVczKGh? MnfFTWM2OD1zMkGuOlEh|ryP Mne1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB3NU[xO|goRjNyNUW2NVc5RC:jPh?=
Dharma MWrD[YxtKH[rYXLpcIl1gSCjc4PhfS=> NXr0[FI1PzJiaB?= MlOzTWM2OD1zNEiuN|ch|ryP NG[0Om89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEW1OlE4QCd-M{C1OVYyPzh:L3G+
YD-10B M{WzW2Z2dmO2aX;uJIF{e2G7 NH;seo41KG2P MmPyOEBp NF60[41idWmub4Lp[IUhe3S{b37ncJkh[myxY3vl[EB1cGVibXXybYRq[W6rbjDD5qCRcW6mdXPl[EBi[2O3bYXsZZRqd25ib3[geoFkfW:uZYOgbY4hYURvMUDCJINmdGy| Mni4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{NE[0PFQoRjNyMkS2OFg1RC:jPh?=
NS20Y MXzGeY5kfGmxbjDhd5NigQ>? NUP4XGs5SW2rbH;ybYRmKGSxc3Wg[IVx\W6mZX70cJkhcW6qaXLpeJMhfGinIFHTTWMh[3W{cnXueEBqdiCQU{KwXUBk\WyuczD3bZRpKGGwIFnDOVAhd2ZiMUGuNFQh|ryP NG\sRpc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{O0NlA4Pid-MkezOFIxPzZ:L3G+
COS-7 MVLGeY5kfGmxbjDhd5NigQ>? M{O5eGJqdmSrbnegZYZncW6rdImg[o9zKEiDLYTh[4dm\CCvdYThcpQhcHWvYX6gRYRmdm:|aX7lJGEzSSC{ZXPldJRweiBqSEK1NG4qKHW|aX7nJHs{UF1vQ1fTMVIyNDZ6MDDhd{Bz[WSrb3zp[4Fv\CCneIDy[ZN{\WRiaX6gR29UNTdiY3XscJMtKEurPUOuNljPxE1? MkH6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwQTJ3OEO2Okc,QTJ3OEO2Olww[T5?
COS-7 NEjm[INHfW6ldHnvckBie3OjeR?= MkXYRolv\GmwZzDh[oZqdmm2eTDmc5IhUEFvdHHn[4VlKG23dHHueEBpfW2jbjDB[IVvd3OrbnWgRVJCKHKnY3XweI9zKCiYOETMLUwhfXOrbnegX|NJZUOJUz2yNVY5OCCjczDyZYRqd2yrZ3Hu[EBmgHC{ZYPz[YQhcW5iQ1;TMVch[2WubIOsJGtqRTFzLkdOwG0> Mon5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwQTJ3OEO2Okc,QTJ3OEO2Olww[T5?
COS-7 M3Xn[2Z2dmO2aX;uJIF{e2G7 NYD6c5pvSmmwZHnu[{Bi\m[rbnn0fUBnd3JiSFGteIFo\2WmIIfpcIQhfHmyZTDoeY1idiCDZHXuc5NqdmViQULBJJJm[2WydH;yJEhYXClidYPpcochYzOKXVPHV{0zOTZ6MDDhd{Bz[WSrb3zp[4Fv\CCneIDy[ZN{\WRiaX6gR29UNTdiY3XscJMtKEurPUGy{txO NYTnVXBmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxOUK1PFM3Pid-OUK1PFM3PjxxYU6=
MDCK MYXGeY5kfGmxbjDhd5NigQ>? MlvRWHBgXFKDTmPQU3JVTVJ8IHnubIljcXSrb36gc4YhXEWDIIXweIFs\SCrbjDPR3QzNWW6cILld5NqdmdiTVTDT{Bk\WyuczygT4k:PC55zszN M3XxUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFzN{W4O|U6Lz5zMUe1PFc2QTxxYU6=
MDCK MXfGeY5kfGmxbjDhd5NigQ>? Mk\0WHBgXFKDTmPQU3JVTVJ8IHnubIljcXSrb36gc4YhXEWDIIXweIFs\SCrbjDPR3QyNWW6cILld5NqdmdiTVTDT{Bk\WyuczygT4k:Pi57zszN MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOTd3OEe1PUc,OTF5NUi3OVk9N2F-
AP1 M3nncWZ2dmO2aX;uJIF{e2G7 NWPXVHh2UW6qaXLpeIlwdiCxZjDBcZBpcXWvYTD0doll[WO2eXz1cUBPUEVzIH31eIFvfCClb370ZYlvcW6pIGTNNVAuOTJiZH;tZYlvKG:oIGDs[ZVzd26nY4Tld{BidWW{aXPhcpV{KGW6cILld5Nm\CCrbjDjbIlv\XOnIHjhcZN1\XJiQWCxJINmdGy|IHHzd4V{e2WmIHHzJIlvfHKjY3XscJVt[XJicFjpJJJm[2:4ZYL5JIJ6KGGvbX;ubZVuKGOqbH;ybYRmKHC{ZYD1cJNmKHC{b4TvZ49tNCCLQ{WwQVM5|ryP M3foV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NEmzPVM4Lz5zN{S5N|k{PzxxYU6=
AP1 MlHwSpVv[3Srb36gZZN{[Xl? NH;QWmtKdmirYnn0bY9vKG:oIGDs[ZVzd26nY4Tld{BidWW{aXPhcpV{KE6KRUGgR{11\XKvaX7hcEBufXSjboSgZ49vfGGrbnnu[{BVVTdiZH;tZYlvKG:oIFHtdIhqfW2jIITybYRi[3S7bIXtJIV5eHKnc4Pl[EBqdiClaHnu[ZNmKGijbYP0[ZIhSVBzIHPlcIx{KGG|c3Xzd4VlKGG|IHnueJJi[2WubIXsZZIheEirIILlZ493\XK7IHL5JIFudW:waYXtJINpdG:{aXTlJJBz\XC3bIPlJJBzd3SxY3;s NEPofYs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{S5N|k{Pyd-MUe0PVM6Ozd:L3G+
AP1 MoLqSpVv[3Srb36gZZN{[Xl? M1rn[WlvcGmkaYTpc44hd2ZiUHzleZJwdmWldHXzJIFu\XKrY3HueZMhVkiHMTDUUVQhdXW2YX70JINwdnSjaX7pcochXE[ITF[gd4VyfWWwY3Wgc4YhSW2yaHn1cYEhfHKrZHHjeJltfW1iZYjwdoV{e2WmIHnuJINpcW6nc3WgbIFue3SncjDBVFEh[2WubIOgZZN{\XO|ZXSgZZMhcW62cnHj[YxtfWyjcjDwTIkhemWlb4\ldpkh[nliYX3tc45qfW1iY3jsc5Jq\GVicILldJVte2VicILveI9kd2x? Ml;FQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd2OUO5N|coRjF5NEmzPVM4RC:jPh?=
HBE NIfsenhHfW6ldHnvckBie3OjeR?= NXj3OZA5UW6qaXLpeIlwdiCxZjDoeY1idiCHTnHDJIlvKEiERTDj[YxteyCkeTDzbI9zfC2laYLjeYl1KGO3coLlcpQhfGWlaH7pdZVmNCCLQ{WwQVAvOjMQvF2= M4T4clxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MUm3NVQ1Lz5{MkG5O|E1PDxxYU6=
FRT NETYNoVHfW6ldHnvckBie3OjeR?= MnG2TY5pcWKrdHnvckBw\iCpdXnu[YEheGmpIFXOZWNj\XSjMT;nZY1u[TFiZYjwdoV{e2WmIHnuJGZTXCClZXzsd{BjgSC|aH;yeE1kcXKldXn0JIN2enKnboSgeIVkcG6rcYXlMEBKSzVyPUCuOVTPxE1? MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjF7N{G0OEc,OjJzOUexOFQ9N2F-
HBE MkG0SpVv[3Srb36gZZN{[Xl? NEPrTm9DdG:la3Hk[UBw\iCqdX3hckBGVmGFIHX4dJJme3OnZDDpckBJSkViY3XscJMh[nlic3jvdpQu[2m{Y4XpeEBkfXK{ZX70JIF{e2G7LDDJR|UxRTBwMkNOwG0> NIDTOlA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkSyOVQ2Oid-MkK0NlU1PTJ:L3G+
FRT MXTGeY5kfGmxbjDhd5NigQ>? NWmzZodDSmyxY3vh[IUhd2ZiZ4XpcoViKHCrZzDFUoFEKGW6cILld5Nm\CCrbjDGVnQh[2WubIOgZpkhe2ixcoStZ4lz[3WrdDDjeZJz\W62IHHzd4F6NCCLQ{WwQVAvPTUQvF2= M4rzOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NEK1OFUzLz5{MkSyOVQ2OjxxYU6=
DAOY NWXZfoNKeUiWUzDhd5NigQ>? M4DiTpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCGQV;ZJINmdGy| MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
A673 MXLxTHRUKGG|c3H5 NV7teI1qeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFG2O|Mh[2WubIO= NG\Yfpk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-MC NHHwSIFyUFSVIHHzd4F6 NXjCc41ieUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> NXLucJl3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-SH NH\Fe49yUFSVIHHzd4F6 MlHCdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tV2gh[2WubIO= NXewfmxZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643 MkP1dWhVWyCjc4PhfS=> MnLKdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6EMU[0N{Bk\Wyucx?= MkHmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
A673 NVfPdJlyeUiWUzDhd5NigQ>? MVHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDBOlc{KGOnbHzzLS=> MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
U-2 OS NXzZUFNGeUiWUzDhd5NigQ>? MmrLdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgWU0zKE:VIHPlcIx{ NV;SZnpQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
AP1 MXjGeY5kfGmxbjDhd5NigQ>? MmfoTY5pcWKrdHnvckBw\iC{YYSgUmhGOSCneIDy[ZN{\WRiaX6gZ4hqdmW|ZTDoZY1{fGW{IFHQNUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHHjbYQucW6mdXPl[EAzOk6jKzDpcoZtfXhiYomgcIlyfWmmIIPjbY51cWyuYYTpc44he3CnY4Tyc5Nkd3C7LDDLbV0y|ryP M3LGd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk1PS9pPlPoSW1DVDxxYU6=
AP1 MV;GeY5kfGmxbjDhd5NigQ>? NG\PeYVKdmirYnn0bY9vKG:oIH\1cIwhdGWwZ4ToJIh2dWGwIFOteIVzdWmwYXygTGEufGGpZ3XkJIh2dWGwIF7ISVUh\XiycnXzd4VlKGmwIHPobY5me2ViaHHtd5RmeiCDUEGgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCjY3nkMYlv\HWlZXSgNlJPSStiaX7mcJV5KGK7IHzpdZVq\CC|Y3nueIltdGG2aX;uJJNx\WO2cn;zZ49xgSxiS3m9NlHPxE1? Mn;sQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVQ2Nyd-Q3jFUWJNRC:jPh?=
Assay
Methods Test Index PMID
Western blot p-AKT / AKT / p-PP1 / PP1 21694768
Immunofluorescence p53 30556178
In vivo Amiloride at 1 mg/kg/day subcutaneously is found to reverse the initial increases in collagen deposition and prevent any further increases in the DOCA-salt hypertensive rat. Amiloride delays the onset of proteinuria and improved brain and kidney histologic scores in the saline-drinking, stroke-prone spontaneously hypertensive rats (SHRSP). compared with controls. Amiloride antagonizes or prevents actions of aldosterone in these cells and in cardiovascular and renal tissues in animals with salt-dependent forms of hypertension. [1]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 53 mg/mL
(199.18 mM)
Water 6 mg/mL
(22.54 mM)
Ethanol '''5 mg/mL

* 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 266.09
Formula

C6H8ClN7O.HCl

CAS No. 2016-88-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1(=C(N=C(C(=N1)Cl)N)N)C(=O)N=C(N)N.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 (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05044611 Not yet recruiting Drug: Anhydrous Amiloride Hydrochloride|Drug: Placebo Bipolar Disorder Assistance Publique - Hôpitaux de Paris April 1 2022 Phase 4
NCT04181008 Recruiting Drug: Amiloride Pharmacokinetics University of Utah|Center for Addiction and Mental Health September 28 2020 Early Phase 1
NCT02323100 Recruiting Drug: Ravicti low dose|Drug: Ravicti high dose|Drug: Placebo Cystic Fibrosis National Jewish Health|University of Alabama at Birmingham|Children''s Hospital of Philadelphia|Johns Hopkins University|Horizon Pharma Ireland Ltd. Dublin Ireland December 2 2018 Phase 1|Phase 2
NCT02586883 Completed Other: bronchial ddp test Idiopathic Dilation of the Bronchi Assistance Publique - Hôpitaux de Paris March 29 2016 Not Applicable

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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