There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
ML133 hydrochloride is a selective Kir2 family channels inhibitor, with an IC50 of 1.8 μM at pH 7.4 and 290 nM at pH 8.5, but exhibits little selectivity against other members of Kir2.x family channels. ML133 has no effect on Kir1.1 (IC50 > 300 μM), and displays weak activity for Kir4.1 (76 μM) and Kir7.1 (33 μM), making ML133 the most selective small molecule inhibitor of the Kir family reported to date[3]. Transplantation of ML133-treated or Kir2.1 knockdown EPCs (Endothelial progenitor cells) facilitated re-endothelialization in the rat injured arterial segment and inhibited neointima formation in vivo. In parallel, ML133 significantly enhanced autophagy and autophagic flux. After suppression of autophagy by 3-methyladenine (3-MA), the effects of ML133 on in vitro function and in vivo endothelialization capacity of EPCs were significantly inhibited[4].
ML133 significantly increased the frequency of glycinergic spontaneous inhibitory postsynaptic currents (gly-sIPSCs) but did not affect their amplitude.
Neurosci Bull. 2019 Apr;35(2):301-314.
Human pulmonary artery smooth muscle cells (HPASMCs)
20 µM
24 hours
ML133 reversed PDGF-BB-induced proliferation and migration of HPASMCs, inhibited the expression of OPN and PCNA, and suppressed the TGF-β1/SMAD2/3 signaling pathway.
Int J Mol Med. 2022 Sep;50(3):119.
Murine colonic smooth muscle cells (SMC)
10 μM
To investigate the effect of ML133 on inward currents in SMC, results showed that ML133 did not significantly inhibit the inward currents
J Physiol. 2018 Feb 1;596(3):379-391.
Murine colonic ICC
10 μM
To investigate the inhibitory effect of ML133 on inward rectifier K+ currents in ICC, results showed that ML133 significantly inhibited the inward current activated by elevated [K+]o
J Physiol. 2018 Feb 1;596(3):379-391.
Layer III pyramidal neurons
30 μM
ML133 is a specific antagonist for the Kir2 subfamily, used to study the hyperpolarization induced by NOP via Kir channels. Results showed that ML133 significantly inhibited Kir channel currents at negative potentials but had no significant effect on NOP-induced hyperpolarization at resting membrane potentials.
Neuropharmacology. 2019 Jun;151:144-158.
BV-2 microglial cells
20 μM
24 hours
To investigate the effect of ML133 on IFNγ-induced priming of microglial ROS production. Results showed that ML133 significantly inhibited the IFNγ-induced enhancement of ROS production.
PLoS One. 2016 Sep 6;11(9):e0162497.
Spino-PB neurons
100 µM
ML133 inhibits Kir2 channels, increases spontaneous activity, depolarizes RMP, reduces rheobase and AP amplitude
Neuroscience. 2016 Dec 17;339:502-510.
HEK293 cells
10 μM
To identify modulators of K ir2.1 function, ML133 was found as a potent inhibitor
ACS Chem Biol. 2011 Aug 19;6(8):845-56.
ML133 HCl 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6J mice
Spared nerve injury (SNI) model
Intrathecal administration
3 nmol, 10 nmol, 30 nmol
Pretreatment 30 min before SNI surgery or once daily from days 5 to 7 post-surgery
ML133 pretreatment dose-dependently inhibited SNI-induced dynamic mechanical allodynia but had no effect on punctate allodynia. Acute ML133 perfusion enhanced glycinergic transmission in spinal dorsal horn lamina IIi neurons.
Neurosci Bull. 2019 Apr;35(2):301-314.
Mice
Murine colonic muscle strips
10 μM and 30 μM
To investigate the effect of ML133 on resting membrane potential in intact colonic muscles, results showed that ML133 caused depolarization of cells
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