PeptideDB

ML67-33 1443290-89-8

ML67-33 1443290-89-8

CAS No.: 1443290-89-8

ML67-33 is a selective activator of temperature- and mechanically-sensitive K2P channels. ML67-33 rapidly and reversibly
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ML67-33 is a selective activator of temperature- and mechanically-sensitive K2P channels. ML67-33 rapidly and reversibly activates K2P2.1 (TREK-1) with EC50s of 36.3 μM and 9.7 μM in cell-free systems and HEK293 cells, respectively.

Physicochemical Properties


Molecular Formula C18H17CL2N5
Molecular Weight 374.267081022263
Exact Mass 373.086
CAS # 1443290-89-8
PubChem CID 86272454
Appearance White to off-white solid powder
LogP 5.3
Hydrogen Bond Donor Count 1
Hydrogen Bond Acceptor Count 4
Rotatable Bond Count 3
Heavy Atom Count 25
Complexity 446
Defined Atom Stereocenter Count 0
SMILES

ClC1C=CC2=C(C=1)C(C)(C)C1C=C(C=CC=1N2CCC1N=NNN=1)Cl

InChi Key GQPMJOXQJUGJPG-UHFFFAOYSA-N
InChi Code

InChI=1S/C18H17Cl2N5/c1-18(2)13-9-11(19)3-5-15(13)25(8-7-17-21-23-24-22-17)16-6-4-12(20)10-14(16)18/h3-6,9-10H,7-8H2,1-2H3,(H,21,22,23,24)
Chemical Name

2,7-dichloro-9,9-dimethyl-10-[2-(2H-tetrazol-5-yl)ethyl]acridine
HS Tariff Code 2934.99.9001
Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


Targets EC50: 36.3 μM (K2P2.1 (TREK-1)), 9.7 μM (K2P2.1 (TREK-1), in HEK293 cells)[1].
ln Vitro K2P2.1 (TREK-1) W275S, K2P2.1 (TREK-1)-3G, K2P10.1 (TREK-2), and K2P4.1 (TRAAK) have EC50 values of 21.8±1.3 μM, 49.4±1.1 μM, 30.2±1.4 μM, and 27.3±1.2 μM, respectively. ML67-33 is known to activate K2P channels and variants.
References

[1]. A high-throughput functional screen identifies small molecule regulators of temperature- and mechano-sensitive K2P channels. ACS Chem Biol. 2013 Aug 16;8(8):1841-51.


Solubility Data


Solubility (In Vitro) DMSO: 100 mg/mL (267.19 mM)
Solubility (In Vivo) Solubility in Formulation 1: ≥ 1.25 mg/mL (3.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.6719 mL 13.3593 mL 26.7187 mL
5 mM 0.5344 mL 2.6719 mL 5.3437 mL
10 mM 0.2672 mL 1.3359 mL 2.6719 mL
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.