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| 25mg |
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Purity: ≥98%
ML335 (ML-335) is a potent and selective activator of TREK-1/-2 and an agonist for OPRM1-OPRD1 (OPRM1: opioid receptor mu 1; OPRD1: delta opioid receptor) heterdimerization. ML335 selectively activates OPRM1-OPRD1 heterodimerization which may have potential use in the treatment of pain and alleviate unwanted effects associated with opiate use. The Scripps Research Institute Molecular Screening Center (SRIMSC) discovered ML335 as an agonist for OPRM1-OPRD1 heterdimerization with an EC50 of 403 nM, and selectivities vs. OPRM1, OPRD1, and HTR5A of 37, 2.7, and >99, respectively. Heteromerization of OPRM1 with OPRD1 leads to the modulation of receptor binding and signaling properties. It has further been shown that the selective activation of the OPRM1-OPRD1 heteromer by a combination of OPRM1 agonist with OPRD1 antagonist can be blocked by antibodies that selectively recognize the heteromer.
| ln Vitro |
Xenopus laevis oocytes were used for two-electrode voltage-clamp measurements. The results indicated that ML335 and ML402 activated K2P2.1 and K2P10.1, but not K2P4.1 (14.3±2.7 μM, K2P2.1-ML335; 13.7±7.0 μM, K2P2.1-ML402; 13.7±7.0 μM, K2P2.1-ML402; 13.7±7.0 μM, K2P2.1-ML402; 13.7±7.0 μM, K2P2.1-ML402; 13.7±7.0 μM, K2P2.1-ML402). 5.9±1.6μM, K2P10.1-ML402; and 5.2±0.5μM, K2P10.1-ML335). A substantial phenotypic reversal of ML335 and M402 activation is caused by the exchange of Lys271 equivalents between K2P2.1 and K2P4.1. Similar to their actions in Xenopus laevis oocytes (ML335 and ML402, 5.2±0.8 μM and 5.9±1.6 μM, respectively (n≥3)), ML335 and ML402 activate K2P2.1 in HEK293 cells [1].
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| References |
| Molecular Formula |
C15H14CL2N2O3S
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| Molecular Weight |
373.25
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| Exact Mass |
372.01
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| CAS # |
825658-06-8
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| Related CAS # |
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| PubChem CID |
1243054
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.635
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| LogP |
3.31
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
23
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| Complexity |
501
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RDFIQTZRJRVFHK-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.70 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 25.0 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 | 2.6792 mL | 13.3958 mL | 26.7917 mL | |
| 5 mM | 0.5358 mL | 2.6792 mL | 5.3583 mL | |
| 10 mM | 0.2679 mL | 1.3396 mL | 2.6792 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
K2P2.1(TREK-1) structures.Nature.2017 Jul 20;547(7663):364-368 |
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K2P2.1(TREK-1) activator interactions.Nature.2017 Jul 20;547(7663):364-368 |
K2P2.1(TREK-1) C-tail and lipid binding sites.Nature.2017 Jul 20;547(7663):364-368 |
K2P2.1(TREK-1) activator function.Nature.2017 Jul 20;547(7663):364-368 |
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K2Pactivator responses.Nature.2017 Jul 20;547(7663):364-368 |
K2Pchannel patch clamp recordings.Nature.2017 Jul 20;547(7663):364-368 |
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