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VU0810464

目录号: PL09963 纯度: ≥99%

VU0810464 是有效的，选择性的非尿素蛋白门控的内向整流钾通道 (GIRK, Kir3) 激活剂。 VU0810464 对神经元 GIRK1/2 (EC50=165 nM) 和 GIRK1/4 (EC50=720 nM) 神经通道具有纳摩尔效价，并且具有脑部渗透性。

CAS No. :2126040-21-7

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PL09963-5mg	5mg	¥968.00	请登录
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PL09963-100mg	100mg	¥4125.00	请登录
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PL09963-10mM*1mLinDMSO	10mM*1mLinDMSO	¥6188.00	请登录
PL09963-1 mL x 10 mM (in DMSO)		¥751.00	请登录

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中文名称	VU0810464
英文名称	VU0810464
英文别名	VU0810464;2-(3-chloro-4-fluorophenyl)-N-(1-cyclohexyl-3-methyl-1H-pyrazol-5-yl)acetamide;2-(3-chloro-4-fluorophenyl)-N-(2-cyclohexyl-5-methylpyrazol-3-yl)acetamide;GTPL10260;compound 8a [PMID: 28697302];E74987
Cas No.	2126040-21-7
分子式	C₁₈H₂₁ClFN₃O
分子量	349.83
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	VU0810464 是有效的，选择性的非尿素蛋白门控的内向整流钾通道 (GIRK, Kir3) 激活剂。 VU0810464 对神经元 GIRK1/2 (EC50=165 nM) 和 GIRK1/4 (EC50=720 nM) 神经通道具有纳摩尔效价，并且具有脑部渗透性。

产品详情	VU0810464 是有效的，选择性的非尿素蛋白门控的内向整流钾通道 (GIRK, Kir3) 激活剂。 VU0810464 对神经元 GIRK1/2 (EC₅₀=165 nM) 和 GIRK1/4 (EC₅₀=720 nM) 神经通道具有纳摩尔效价，并且具有脑部渗透性。
生物活性	VU0810464 is a potent and selective non-ureaG protein-gated inwardly-rectifying potassium channels (GIRK, Kir3) activator. VU0810464 displays nanomolar potency for neuronal (EC 50 =165 nM) and GIRK1/4 (EC 50 =720 nM) channels with improved brain penetration.
性状	Solid
IC50 & Target[1][2]	EC50: 165 nM (GIRK 1/2); 720 nM (GIRK1/4 )
体外研究(In Vitro)	VU0810464 (0, 0.1, 0.3, 1, 3, 10, 30 μM) produces a concentration‐dependent response curves of currents in SAN and HPC cells, in addition, VU0810464 is 9‐fold higher potency for Kir3 channel activation in neurons as compared to SAN cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	VU0810464 (intraperitoneal injection; 30 mg/kg, 10 mg/kg; 30mg/kg; pre-treated 30 mins) produces a dose-dependent reduction of SIH response in Male C57BL/6J mice. To test if VU0810464 plays it role through Kir3 channel activation, VU0810464 (10 mg/kg) suppresses the SIH response in wild‐ type mice, but has no impact on Kcnj3 mice. VU0810464 (intraperitoneal injection ; 30 mg/kg; 15, 30, 45, or 60 min post‐injection) displays a favourable distribution to the brain (K p,uu = 0.83), has a improvement over ML297 (K p,uu = 0.32). Clearance of VU0810464 is rapid,brain and plasma half-lives is 20 min in a PK study. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Vo BN, et al. VU0810464, a non-urea G protein-gated inwardly rectifying K+ (Kir 3/GIRK) channel activator, exhibits enhanced selectivity for neuronal Kir 3 channels and reduces stress-induced hyperthermia in mice.Br J Pharmacol. 2019 Jul;176(13):2238-2249 [2]. Wieting JM,et al. Discovery and Characterization of 1H-Pyrazol-5-yl-2-phenylacetamides as Novel, Non-Urea-Containing GIRK1/2 Potassium Channel Activators.ACS Chem Neurosci. 2017 Sep 20;8(9):1873-1879.

溶解度数据	In Vitro: DMSO : ≥ 250 mg/mL (714.63 mM)配制储备液

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[1]. Vo BN, et al. VU0810464, a non-urea G protein-gated inwardly rectifying K+ (Kir 3/GIRK) channel activator, exhibits enhanced selectivity for neuronal Kir 3 channels and reduces stress-induced hyperthermia in mice.Br J Pharmacol. 2019 Jul;176(13):2238-2249
[2]. Wieting JM,et al. Discovery and Characterization of 1H-Pyrazol-5-yl-2-phenylacetamides as Novel, Non-Urea-Containing GIRK1/2 Potassium Channel Activators.ACS Chem Neurosci. 2017 Sep 20;8(9):1873-1879.

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。

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