Synonym
ML335; ML-335; ML 335; TREK-1/2 Activator;
IUPAC/Chemical Name
N-[(2,4-Dichlorophenyl)methyl]-4-(methanesulfonamido)benzamide
InChi Key
RDFIQTZRJRVFHK-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H14Cl2N2O3S/c1-23(21,22)19-13-6-3-10(4-7-13)15(20)18-9-11-2-5-12(16)8-14(11)17/h2-8,19H,9H2,1H3,(H,18,20)
SMILES Code
O=C(NCC1=CC=C(Cl)C=C1Cl)C2=CC=C(NS(=O)(C)=O)C=C2
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
ML335 is a selective activator of both TREK-1 and TREK-2.
In vitro activity:
TREK-1 activation also decreased IL-6, IP-10, and CCL-2 secretion from primary AECs. Mechanistically, ML335 and BL1249 induced TREK-1 currents in AECs, counteracted HO-induced cell depolarization, and lowered iCa2+ concentrations. In addition, CCL-2 secretion was decreased after L-type CaV inhibition.
Reference: Sci Rep. 2020 Dec 15;10(1):22011. https://pubmed.ncbi.nlm.nih.gov/33319831/
In vivo activity:
Once-daily, intra-tracheal injections of HO-exposed mice with ML335 or BL1249 improved lung compliance, histological lung injury scores, broncho-alveolar lavage protein levels and cell counts, and IL-6 and IP-10 concentrations.
Reference: Sci Rep. 2020 Dec 15;10(1):22011. https://pubmed.ncbi.nlm.nih.gov/33319831/
|
Solvent |
mg/mL |
mM |
comments |
| Solubility |
| DMF |
30.0 |
80.38 |
|
| DMSO |
74.3 |
199.15 |
|
| DMSO:PBS (pH 7.2) (1:20) |
0.0 |
0.11 |
|
| Ethanol |
5.8 |
15.59 |
|
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
373.25
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
Zyrianova T, Lopez B, Olcese R, Belperio J, Waters CM, Wong L, Nguyen V, Talapaneni S, Schwingshackl A. K2P2.1 (TREK-1) potassium channel activation protects against hyperoxia-induced lung injury. Sci Rep. 2020 Dec 15;10(1):22011. doi: 10.1038/s41598-020-78886-y. PMID: 33319831; PMCID: PMC7738539.
In vitro protocol:
Zyrianova T, Lopez B, Olcese R, Belperio J, Waters CM, Wong L, Nguyen V, Talapaneni S, Schwingshackl A. K2P2.1 (TREK-1) potassium channel activation protects against hyperoxia-induced lung injury. Sci Rep. 2020 Dec 15;10(1):22011. doi: 10.1038/s41598-020-78886-y. PMID: 33319831; PMCID: PMC7738539.
In vivo protocol:
Zyrianova T, Lopez B, Olcese R, Belperio J, Waters CM, Wong L, Nguyen V, Talapaneni S, Schwingshackl A. K2P2.1 (TREK-1) potassium channel activation protects against hyperoxia-induced lung injury. Sci Rep. 2020 Dec 15;10(1):22011. doi: 10.1038/s41598-020-78886-y. PMID: 33319831; PMCID: PMC7738539.
1: Lolicato M, Arrigoni C, Mori T, Sekioka Y, Bryant C, Clark KA, Minor DL Jr.
K(2P)2.1 (TREK-1)-activator complexes reveal a cryptic selectivity filter binding
site. Nature. 2017 Jul 20;547(7663):364-368. doi: 10.1038/nature22988. Epub 2017
Jul 10. PubMed PMID: 28693035; PubMed Central PMCID: PMC5778891.
2: Pinello C, Guerrero M, Eberhart C, Volmar CH, Saldanha SA, Cayanan C, Urbano
M, Brown SJ, Ferguson J, Gomes I, Devi LA, Roberts E, Hodder P, Rosen H.
Characterization of an agonist probe for opioid receptor mu 1 (OPRM1)-opioid
receptor delta 1 (OPRD1) heterodimerization. 2012 Dec 17 [updated 2013 Apr 5].
Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD):
National Center for Biotechnology Information (US); 2010-. Available from
http://www.ncbi.nlm.nih.gov/books/NBK148496/
PubMed PMID: 23833799.
