SBI-797812 是一种口服有效的烟酰胺磷酸核糖基转移酶 (NAMPT) 激活剂。SBI-797812 激活NAMPT向 NMN 转变,增加NAMPT对 ATP 的亲和力,稳定磷酸化NAMPT,促进焦磷酸盐副产物的消耗,并减弱 NAD+的反馈抑制。SBI-797812 增加细胞内 NMN,并提高小鼠肝脏内 NAD+水平。
生物活性 | SBI-797812 is an orally activenicotinamide phosphoribosyltransferase (NAMPT)activator. SBI-797812 shiftsNAMPTto NMN formation, increasesNAMPTaffinity for ATP, stabilizes phosphorylatedNAMPT, promotes consumption of the pyrophosphate by-product, and blunts feedback inhibition by NAD+. SBI-797812 increases intracellular nicotinamide mononucleotide (NMN) and elevates liver NAD+in mice[1][2]. |
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体外研究 (In Vitro) | SBI-797812 (0-4 μM; 4 h) activates NAMPT in a dose-dependent manner with an EC50value of 0.37 μM, and (1 μM, 2 μM; 1 h) increases NAMPT-mediated NMN in cells[1]. SBI-797812 (2 μM; 1 or 4 h) exerts NAMPT (30 nM) activation requiring ATP (2 mM)[1]. SBI-797812 (5 μM; 2 h) impacts PP (20 μM) consumption and pHisNAMPT reactivity[1]. SBI-797812 (0.4, 2, 10 μM; 4 h) increases the level of nicotinamide mononucleotide (NMN) and NAD+in A549 human lung carcinoma cells as well as in human or mouse primary myotubes at 10 μM[1]. SBI-797812, as an NRAMPT activator plays a role in successive aging promotion, while NAMPT is a rate limiting enzyme in NAD+salvage pathway of Aging/Senescence process[2].
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体内研究 (In Vivo) | SBI-797812 (10 mg/kg; i.p. or o.p.; single dose) shows high plasma exposure by intraperitoneal injection, with Cmaxvalue of 3297 ng/mL, 8.2 μM[1]. SBI-797812 (20 mg/kg; i.p.; single dose; measured 2 h post-dose) significant increases NAD+in mouse liver[1].
Animal Model: | Male C57BL/6 J mice (8-week-old)[1] | Dosage: | 20 mg/kg | Administration: | Intraperitoneal injection; administrated 1 h after fasting; added Buthanasia-D (165 mg/kg; i.p.) 4 h after fasting | Result: | Showed 0.311, 0.144, 0.078, and 0.078 μg/mg dry powder about NAD+in liver, heart, gastrocnemius and quadriceps, respectively by LC-MS/MS measurement.
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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 |
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溶解性数据 | In Vitro: DMSO : 250 mg/mL(621.16 mM;Need ultrasonic) 配制储备液 1 mM | 2.4847 mL | 12.4233 mL | 24.8466 mL | 5 mM | 0.4969 mL | 2.4847 mL | 4.9693 mL | 10 mM | 0.2485 mL | 1.2423 mL | 2.4847 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制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 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 2.08 mg/mL (5.17 mM); Clear solution; Need ultrasonic
此方案可获得 2.08 mg/mL (5.17 mM) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (5.17 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.17 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (5.17 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.17 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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