MRK-016
- CAS No.
- 342652-67-9
- Chemical Name:
- MRK-016
- Synonyms
- MRK016;MRK 016;3-[3-tert-butyl-2-[(2-methyl-1,2,4-triazol-3-yl)methoxy]pyrazolo[1,5-d][1,2,4]triazin-7-yl]-5-methyl-1,2-oxazole;3-(9-(tert-Butyl)-8-((1-methyl-1H-1,2,4-triazol-5-yl)methoxy)pyrazolo[1,5-d][1,2,4]triazin-2-yl)-5-methylisoxazole;Pyrazolo[1,5-d][1,2,4]triazine, 3-(1,1-dimethylethyl)-7-(5-methyl-3-isoxazolyl)-2-[(1-methyl-1H-1,2,4-triazol-5-yl)methoxy]-;7-(5-Methyl-1,2-oxazol-3-yl)-3-(2-methyl-2-propanyl)-2-[(1-methyl-1H-1,2,4-triazol-5-yl)methoxy]pyrazolo[1,5-d][1,2,4]triazine
- CBNumber:
- CB63133349
- Molecular Formula:
- C17H20N8O2
- Molecular Weight:
- 368.39
- MDL Number:
- MFCD18086893
- MOL File:
- 342652-67-9.mol
- MSDS File:
- SDS
- TDS File:
- TDS
| Melting point | 175-176 °C(Solv: ethyl ether (60-29-7); methanol (67-56-1)) |
|---|---|
| Density | 1.43±0.1 g/cm3(Predicted) |
| storage temp. | under inert gas (nitrogen or Argon) at 2-8°C |
| solubility | DMF: 2 mg/ml; DMSO: Slightly soluble; Ethanol: Slightly soluble; PBS (pH 7.2): 0.2 mg/ml |
| form | A solid |
| pka | 2.28±0.10(Predicted) |
| color | White to off-white |
| InChI | 1S/C17H20N8O2/c1-10-6-11(23-27-10)15-21-19-7-12-14(17(2,3)4)16(22-25(12)15)26-8-13-18-9-20-24(13)5/h6-7,9H,8H2,1-5H3 |
| InChIKey | QYSYOGCIDRANAR-UHFFFAOYSA-N |
| SMILES | CC(C)(C1=C2C=NN=C(N2N=C1OCC3=NC=NN3C)C4=NOC(C)=C4)C |
| FDA UNII | TXZ4DVJ9MF |
| UNSPSC Code | 12352200 |
| NACRES | NA.77 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P280-P301+P312-P302+P352-P305+P351+P338 |
| WGK Germany | WGK 3 |
| Storage Class | 11 - Combustible Solids |
MRK-016 price More Price(40)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | SML3088 | MRK-016 ≥98% (HPLC) | 342652-67-9 | 5MG | $161 | 2026-04-30 | Buy |
| Sigma-Aldrich | SML3088 | MRK-016 ≥98% (HPLC) | 342652-67-9 | 25MG | $515 | 2026-04-30 | Buy |
| Cayman Chemical | 36656 | MRK-016 ≥98% | 342652-67-9 | 1mg | $44 | 2026-04-30 | Buy |
| Cayman Chemical | 36656 | MRK-016 ≥98% | 342652-67-9 | 5mg | $174 | 2026-04-30 | Buy |
| Cayman Chemical | 36656 | MRK-016 ≥98% | 342652-67-9 | 10mg | $304 | 2026-04-30 | Buy |
MRK-016 Chemical Properties, Uses, Production
Uses
MRK 016 is an inverse benzodiazepine antagonist which may assist in mitigating inflammation-induced decrements in cognitive function.
Biological Activity
MRK-016 is an orally active, benzodiazepine site-targeting, alpha5-selective GABAA inverse agonist (Emax = -55%/α5, -16%/α1, -9%/α3, +6%/α2 of a EC20 GABA response using respective recombinant human αβ3γ2) with in vivo cognition-enhancing properties (0.3-3 mg/kg p.o. in r at Morris water maze test).
in vivo
MRK-016 does not enhance pentylenetetrazole-induced convulsions at 10 mg/kg via ip, or cause seizures at 30 mg/kg, via po for 20 days in mice. MRK-016 shows no obvious anxiogenic-like effects in rats at doses that occupy >95% of benzodiazepine (BZ) binding sites. MRK-016 (0.3, 1, and 3 mg/kg, p.o.) dose-dependently improves performance of rats hippocampal-dependent memory task[1]. MRK-016 (0.3-30 mg/kg, p.o.) causes good receptor occupancy in rats. MRK-016 (0.3, 1, or 3 mg/kg p.o.) shows cognition-enhancing activity in the delayed matching-to-position version of the Morris water maze. MRK-016 (1, 3, or 10 mg/kg i.p.) does not produce kindling in mice[2]. MRK-016 (3 mg/kg, i.p.) protects against LPS-induced learning/memory decrements in mice[3].
storage
Store at +4°C
MRK-016 Preparation Products And Raw materials
Raw materials
Preparation Products
MRK-016 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9799 | 58 |
| Shanghai Chaolan Chemical Technology Center | QQ：65489617 13301690235 | Sales@ATKchemical.com | China | 9711 | 58 |
| Musechem | +1-800-259-7612 | info@musechem.com | United States | 4648 | 60 |
| Fan De(Beijing) Biotechnology Co., Ltd. | 15911056312 | liming@bio-fount.com | China | 9718 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +1-00000000000 | marketing@targetmol.com | United States | 32431 | 58 |
| Xi'an Minze Pharmaceutical Technology Co., Ltd | 13981836672 | 2560370848@qq.com | China | 2807 | 58 |
| ChemeGen(Shanghai) Biotechnology Co.,Ltd. | 18818260767 | sales@chemegen.com | China | 11123 | 58 |
| Shanghai hongqu biomedical technology co. LTD | 88888888888 | hongquchem@qq.com | China | 5123 | 58 |
| Bide Pharmatech Ltd. | 400-1647117 13681763483 | product02@bidepharm.com | China | 59929 | 58 |
| Kaifeng Mingren Pharmaceutical Co.,LTD | 0371-65741762 | sales@hasunny.com | China | 2377 | 58 |
