货号:A247277
同义名:
1,7-Dimethylxanthine; NSC 400018
Paraxanthine是咖啡因的主要代谢物,能够通过刺激 Ryanodine 受体通道来抑制多巴胺能细胞的死亡,适用于神经退行性疾病的研究,尤其在帕金森病的机制研究中具有重要意义。
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产品名称 | PARP ↓ ↑ | PARP1 ↓ ↑ | PARP2 ↓ ↑ | PARP3 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
PJ34 HCl |
++
PARP, EC50: 20 nM |
99%+ | |||||||||||||||||
Rucaparib phosphate |
++++
PARP, Ki: 1.4 nM |
99%+ | |||||||||||||||||
3-Aminobenzamide |
++
PARP, IC50: <50 nM |
98% | |||||||||||||||||
AZD-2461 | ✔ | 99%+ | |||||||||||||||||
BGP-15 | ✔ | 99%+ | |||||||||||||||||
NU1025 |
+
PARP, IC50: 400 nM |
98% | |||||||||||||||||
Benzamide |
+
PARP, IC50: 3.3 μM |
98% | |||||||||||||||||
Picolinamide |
+
PARP, IC50: 95 μM |
98% | |||||||||||||||||
AG14361 |
+++
PARP1, Ki: <5 nM |
98+% | |||||||||||||||||
Iniparib | ✔ | 98% | |||||||||||||||||
Talazoparib |
++++
PARP1, IC50: 0.57 nM |
99%+ | |||||||||||||||||
NMS-P118 |
++
PARP1, Kd: 0.009 μM |
97% | |||||||||||||||||
UPF 1069 |
+
PARP1, IC50: 8.0 μM |
++
PARP2, IC50: 0.3 μM |
98% | ||||||||||||||||
A-966492 |
++++
PARP1, EC50: 1 nM PARP1, Ki: 1 nM |
+++
PARP2, Ki: 1.5 nM |
99%+ | ||||||||||||||||
Veliparib |
++
PARP1, Ki: 5.2 nM |
+++
PARP2, Ki: 2.9 nM |
98% | ||||||||||||||||
Niraparib tosylate |
+++
PARP1, IC50: 3.8 nM |
+++
PARP2, IC50: 2.1 nM |
99%+ | ||||||||||||||||
Stenoparib |
++++
PARP1, IC50: 1 nM |
++++
PARP2, IC50: 1.2 nM |
98% | ||||||||||||||||
Olaparib |
+++
PARP1, IC50: 5 nM |
++++
PARP2, IC50: 1 nM |
98% | ||||||||||||||||
Niraparib |
+++
PARP1, IC50: 3.8 nM |
+++
PARP2, IC50: 2.1 nM |
98% | ||||||||||||||||
ME0328 |
+
PARP1, IC50: 6.3 μM |
+
PARP3, IC50: 0.89 μM |
99%+ | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
Administration | Dosage | Frequency | Description | References | ||
Male Swiss Albino mice | Exercise performance evaluation model | Oral | 20.5 mg/kg/day | Once daily for 4 weeks | To evaluate the effects of Paraxanthine on muscle mass, strength, and endurance. Results showed that Paraxanthine significantly increased forelimb grip strength (17%), treadmill exercise performance (39%), gastrocnemius and soleus muscle mass (14% and 41%, respectively), and NO levels (100%), while reducing triglycerides, total cholesterol, and LDL, and increasing HDL. | Nutrients. 2022 Feb 20;14(4):893 |
Mice | Wild-type (WT) and narcoleptic transgenic (TG) mice | Oral | 6.25 mg/kg, 25 mg/kg, 100 mg/kg | Administered at ZT2 and ZT14, monitored for 6 hours post-administration | To evaluate the wake-promoting efficacy of paraxanthine in WT and narcoleptic mice models and compare it with caffeine and modafinil. Paraxanthine significantly promoted wakefulness in both WT and narcoleptic TG mice and proportionally reduced NREM and REM sleep in both genotypes. The wake-promoting potency of paraxanthine is greater and longer lasting than that of the equimolar concentration of caffeine. | Sleep. 2010 Jul;33(7):930-42 |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
5.55mL 1.11mL 0.56mL |
27.75mL 5.55mL 2.78mL |
55.51mL 11.10mL 5.55mL |
CAS号 | 611-59-6 |
分子式 | C7H8N4O2 |
分子量 | 180.16 |
SMILES Code | O=C(N1C)NC2=C(N(C)C=N2)C1=O |
MDL No. | MFCD00005727 |
别名 | 1,7-Dimethylxanthine; NSC 400018 |
运输 | 蓝冰 |
InChI Key | QUNWUDVFRNGTCO-UHFFFAOYSA-N |
Pubchem ID | 4687 |
存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry,2-8°C |
溶解方案 |
DMSO: 25 mg/mL(138.76 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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