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  3. RTI-7470-44

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。

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RTI-7470-44 Chemical Structure

RTI-7470-44 Chemical Structure

CAS No. : 825658-63-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3300
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1 mg ¥1363
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5 mg ¥3000
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10 mg ¥4800
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25 mg ¥9500
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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 Ki 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)[1].

IC50 & Target

IC50: 8.4 nM (human TAAR1), 748 nM (rat TAAR1), 1190 nM (mouse TAAR1)[1]

体外研究
(In Vitro)

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 (Ki=1 μM) and a very weak affinity for human sigma 2 (Ki=8.4 μM)[1].

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

体内研究
(In Vivo)

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)[1].
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[1].
Stability of RTI-7470-44 in Human, Rat, and Mouse Liver Microsomes[1].

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

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

分子量

449.84

Formula

C19H11ClF3N5OS

CAS 号
性状

固体

颜色

Off-white to light yellow

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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 20.83 mg/mL (46.31 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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。

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

RTI-7470-44 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2230 mL 11.1151 mL 22.2301 mL 55.5753 mL
5 mM 0.4446 mL 2.2230 mL 4.4460 mL 11.1151 mL
10 mM 0.2223 mL 1.1115 mL 2.2230 mL 5.5575 mL
15 mM 0.1482 mL 0.7410 mL 1.4820 mL 3.7050 mL
20 mM 0.1112 mL 0.5558 mL 1.1115 mL 2.7788 mL
25 mM 0.0889 mL 0.4446 mL 0.8892 mL 2.2230 mL
30 mM 0.0741 mL 0.3705 mL 0.7410 mL 1.8525 mL
40 mM 0.0556 mL 0.2779 mL 0.5558 mL 1.3894 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
RTI-7470-44
目录号:
HY-147319
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