MRK-016
- Product Name
- 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
- Formula Weight
- 368.39
- MOL File
- 342652-67-9.mol
MRK-016 Property
- 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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- SML3088
- Product name
- MRK-016
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $142.5
- Updated
- 2025/07/31
- Product number
- SML3088
- Product name
- MRK-016
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $481
- Updated
- 2025/07/31
- Product number
- M750235
- Product name
- MRK016
- Packaging
- 5mg
- Price
- $440
- Updated
- 2021/12/16
- Product number
- CS-5698
- Product name
- MRK-016
- Purity
- 98.29%
- Packaging
- 50mg
- Price
- $750
- Updated
- 2021/12/16
- Product number
- CS-5698
- Product name
- MRK-016
- Purity
- 98.29%
- Packaging
- 10mg
- Price
- $190
- Updated
- 2021/12/16
MRK-016 Chemical Properties,Usage,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
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