RTI-7470-44|cas:825658-63-7|西域试剂

RTI-7470-44,99.79%

产品编号：Bellancom-147319| CAS NO：825658-63-7| 分子式：C₁₉H₁₁ClF₃N₅OS| 分子量：449.84

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货号	价格	库存与货期
Bellancom-147319	￥3000.00	杭州北京（现货）
Bellancom-147319	￥4800.00	杭州北京（现货）
Bellancom-147319	￥9500.00	杭州北京（现货）
Bellancom-147319	￥14500.00	杭州北京（现货）

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RTI-7470-44

产品介绍

RTI-7470-44 是一种有效且具有选择性和血脑屏障透过性的人微量胺相关受体 1 (hTAAR1) 拮抗剂，IC₅₀ 为 8.4 nM。RTI-7470-44 具有中等的代谢稳定性和良好的初步脱靶谱。RTI-7470-44 可增加小鼠中脑腹侧被盖区 (VTA) 多巴胺能神经元的自发放电率。RTI-7470-44 可用于精神分裂症、活性分子成瘾和帕金森病 (PD) 的研究。

生物活性

RTI-7470-44 is a potent, selective and blood-brain barrier (BBB) penetrant human trace amine-associated receptor subtype 1 (hTAAR1) antagonist with an IC₅₀ value of 8.4 nM and a K_i value of 0.3 nM. RTI-7470-44 has moderate metabolic stability, and a favorable preliminary off-target profile. RTI-7470-44 can increase the spontaneous firing rate of mouse ventral tegmental area (VTA) dopaminergic neurons. RTI-7470-44 can be used for researching schizophrenia, agent addiction, and Parkinson’s disease (PD).

体外研究

RTI-7470-44 (10 μM) shows little to no off-target activity with the exception of the benzylpiperazine (BZP) rat brain site and human sigma 2 with inhibition of 75 and 90%, respectively; has a moderate affinity for the BZP rat brain site (K_i=1 μM) and a very weak affinity for human sigma 2 (K_i=8.4 μM).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

RTI-7470-44 (40 μM) significantly increases the firing rate of dopaminergic neurons in VTA slices from DAT-IRES-Cre; td-Tomato mice, and reverses the inhibitory effect of RO5166017 (a TAAR1 agonist).
RTI-7470-44 (10 μM) has decent stability in human liver microsomes, less stable in mouse liver microsomes and very poor stability in rat liver microsomes.
Stability of RTI-7470-44 in Human, Rat, and Mouse Liver Microsomes.

species	half-life (min)	clearance, CLINT (mL/min/mg)
Human	83.9	14.9
Rat	9.11	274
Mouse	65.8	63.5

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

species	half-life (min)	clearance, CLINT (mL/min/mg)
Human	83.9	14.9
Rat	9.11	274
Mouse	65.8	63.5

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : 20.83 mg/mL (46.31 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2230 mL	11.1151 mL	22.2301 mL
5 mM	0.4446 mL	2.2230 mL	4.4460 mL
10 mM	0.2223 mL	1.1115 mL	2.2230 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式