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RO5166017

目录号: PL12399 纯度: ≥99%

RO5166017 是具有口服活性的、跨物种的 TAAR1 的激动剂，其对小鼠、大鼠、人和食蟹猴的 Ki 值分别为1.9 nM、2.7 nM、31 nM 和 24 nM。

CAS No. :1048346-74-2

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中文名称	RO5166017
中文别名	(4S)-4-[(N-Ethylanilino)methyl]-4,5-dihydro-1,3-oxazol-2-amine
英文名称	RO5166017
英文别名	(4S)-4-[(N-Ethylanilino)methyl]-4,5-dihydro-1,3-oxazol-2-amine;RO5166017;(S)-4-[(ethyl-phenyl-amino)-methyl]-4,5-dihydro-oxazol-2-ylamine;(S)-4-((Ethyl(phenyl)amino)methyl)-4,5-dihydrooxazol-2-amine;PPONHQQJLWPUPH-JTQLQIEISA-N;RO 5166017;GTPL5862;BDBM50158431;Q7277303
Cas No.	1048346-74-2
分子式	C₁₂H₁₇N₃O
分子量	219.28
包装储存	-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
详情描述	RO5166017 是具有口服活性的、跨物种的 TAAR1 的激动剂，其对小鼠、大鼠、人和食蟹猴的 Ki 值分别为1.9 nM、2.7 nM、31 nM 和 24 nM。

产品详情	RO5166017 是具有口服活性的、跨物种的 TAAR1 的激动剂，其对小鼠、大鼠、人和食蟹猴的 K_i 值分别为1.9 nM、2.7 nM、31 nM 和 24 nM。
生物活性	RO5166017 is an orally active and species-crosses TAAR1 agonist, with K i values of 1.9 nM, 2.7 nM, 31 nM and 24 nM for mouse, rat, human and cynomolgus monkey, respectively.
性状	Solid
体外研究(In Vitro)	RO5166017 showed high affinity and potent functional activity at mouse, rat, cynomolgus monkey, and human TAAR1 stably expressed in HEK293 cells as well as high selectivity vs. other targets. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	RO5166017 prevents stress-induced hyperthermia and blocked dopamine-dependent hyperlocomotion in cocaine-treated and dopamine transporter knockout mice as well as hyperactivity induced by an NMDA antagonist. RO5166017 (0.01-1 mg/kg, orally) dose-dependently prevents the SIH in NMRI mice. RO5166017 exhibits TAAR1-mediated anxiolytic-like properties at doses 0.1-0.3 mg/kg.. RO5166017 prevents the cocaine-induced hyperlocomotion. RO5166017 also inhibits stereotypies induced by cocaine in WT mice similar to olanzapine, and this effect is lost in Taar1 mice. TAAR1 activation by RO5166017 increases glucose-dependent insulin secretion in INS1E cells and human islets and elevated plasma and peptide YY (PYY) and glucagon like peptide 1 (GLP-1) levels in mice. Subchronic treatment of diet-induced obese (DIO) mice with RO5166017 results in reduced food intake and body weight.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[1]. Florent G Revel, et al. TAAR1 activation modulates monoaminergic neurotransmission, preventing hyperdopaminergic and hypoglutamatergic activity. Proc Natl Acad Sci U S A [2]. Justin N Siemian, et al. Trace amine-associated receptor 1 agonists RO5263397 and RO5166017 attenuate quinpirole-induced yawning but not hypothermia in rats. Behav Pharmacol. 2017 Oct;28(7):590-593.

溶解度数据	In Vitro: DMSO : 25 mg/mL (114.01 mM; Need ultrasonic)配制储备液

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[1]. Florent G Revel, et al. TAAR1 activation modulates monoaminergic neurotransmission, preventing hyperdopaminergic and hypoglutamatergic activity. Proc Natl Acad Sci U S A
[2]. Justin N Siemian, et al. Trace amine-associated receptor 1 agonists RO5263397 and RO5166017 attenuate quinpirole-induced yawning but not hypothermia in rats. Behav Pharmacol. 2017 Oct;28(7):590-593.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

RO5166017

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