| Identification | Back Directory | [Name]
3-(3-(pyridin-3-yl)-1,2,4-oxadiazol-5-yl)benzonitrile | [CAS]
913830-15-6 | [Synonyms]
NS 9283 NS-9283;NS9283 NS 9283;NS-9283;NS9283 3-[3-(3-Pyridinyl)-1,2,4-oxadiazol-5-yl]benzonitrile 3-(3-(pyridin-3-yl)-1,2,4-oxadiazol-5-yl)benzonitrile Benzonitrile, 3-[3-(3-pyridinyl)-1,2,4-oxadiazol-5-yl]- | [Molecular Formula]
C14H8N4O | [MDL Number]
MFCD26390306 | [MOL File]
913830-15-6.mol | [Molecular Weight]
248.24 |
| Chemical Properties | Back Directory | [Boiling point ]
469.9±55.0 °C(Predicted) | [density ]
1.37±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 10 mg/ml; DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml; DMSO: 3 mg/ml; Ethanol: Partially soluble | [form ]
A crystalline solid | [pka]
1.40±0.12(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
NS 9283 is a positive allosteric modulator of α4β2 subunit-containing nicotinic acetylcholine receptors (nAChRs) that potentiates ACh-induced currents in HEK293 cells expressing human α4β2 subunit-containing nAChRs (EC50 = 4 μM). In vivo, NS 9283 potentiates ABT-594 analgesic efficacy in rat models of carrageenan-induced thermal hyperalgesia, paw skin incision post-operative pain, and monoiodoacetate-induced osteoarthritis. It reduces nicotine, but not sucrose, self-administration and reinstatement in rats when administered at a dose of 3.5 mg/kg. | [Uses]
NS 9283 is a positive allosteric modulator of α4β2 receptor affecting the potency of acetylcholine (Ach) related events. This has been linked to affect on everyday brain function including cognitive function and pain alleviation. | [storage]
Store at -20°C | [References]
[1] M GRUPE. Unravelling the mechanism of action of NS9283, a positive allosteric modulator of (α4)3(β2)2 nicotinic ACh receptors[J]. British Journal of Pharmacology, 2012, 168 8: 2000-2010. DOI: 10.1111/bph.12095 [2] CHANG Z. ZHU. Potentiation of analgesic efficacy but not side effects: Co-administration of an α4β2 neuronal nicotinic acetylcholine receptor agonist and its positive allosteric modulator in experimental models of pain in rats[J]. Biochemical pharmacology, 2011, 82 8: Pages 967-976. DOI: 10.1016/j.bcp.2011.05.007 [3] J. MAURER H S K Sandager‐Nielsen. Attenuation of nicotine taking and seeking in rats by the stoichiometry-selective alpha4beta2 nicotinic acetylcholine receptor positive allosteric modulator NS9283[J]. Psychopharmacology, 2016, 234 1: 475-484. DOI: 10.1007/s00213-016-4475-7 |
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