Dapansutrile 是一种口服有效的选择性 NLRP3 炎症小体抑制剂。Dapansutrile 具有抗炎活性，能够降低免疫因子水平。Dapansutrile 可用于炎性疾病的研究。
| 生物活性 | Dapansutrile is a potent, orally active and selectiveNLRP3inflammasomeinhibitor. Dapansutrile has anti-inflammatory activity and decreases immune factor levels. Dapansutrile can be used for research of inflammatory diseases[1][2]. |
体内研究
(In Vivo) | Dapansutrile (3.75 g/kg; p.o.; daily, for 22 d) ameliorates neurological decline and nervous tissue damage in experimental autoimmune encephalomyelitis (EAE) mice[1].
Dapansutrile (3.75 g/kg; p.o.; daily, for 22 d) attenuates the protein levels of pro-inflammatory cytokines in the spinal cord of experimental autoimmune encephalomyelitis (EAE) mice[1].
Dapansutrile (6-600 mg/kg; i.p.; once; male ICR (CD1) mice) reduces infarct size and reduces caspase-1 activity in the heart[2].
Dapansutrile (6-600 mg/kg; i.p.; once, for 24 hours and 7 days; mice subjected to acute myocardial infarction) preserves cardiac function following myocardial ischemia-reperfusion injury[2].
| Animal Model: | EAE-induced female adult C57BL/6 (8–10 weeks old)[1] | | Dosage: | 3.75 g/kg | | Administration: | Oral administration; daily, for 22 days | | Result: | Ameliorated the neurological deficits of EAE disease.
Reduced the levels of IL-1β, L-18 , TNFα, CXCL-1 and IL-6. Showed ~2-fold reduction in the infiltration of T cells (CD45+, CD3+). Reduced the accumulation macrophages (CD45high, CD11b+, F4/80+), microglia (CD45low, CD11b+), and other cells (CD45+, CD11b-, CD3-, CD24+). |
| Animal Model: | Male ICR (CD1) mice (8-12 weeks old)[2] | | Dosage: | 6, 60, and 600 mg/kg | | Administration: | Intraperitoneal injection; once | | Result: | Reduced infarct size in a dose-dependent manner. |
| Animal Model: | Mice subjected to acute myocardial infarction (AMI)[2] | | Dosage: | 6, 60, and 600 mg/kg | | Administration: | Intraperitoneal injection; once, for 24 hours and 7 days | | Result: | Preserved left ventricular (LV) systolic function at 24 hours.
Increased in cardiac function at 7 days of reperfusion when compared with the control mice. |
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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 : ≥ 125 mg/mL(938.65 mM) H2O : 36.67 mg/mL(275.36 mM;Need ultrasonic) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 7.5092 mL | 37.5460 mL | 75.0920 mL | | 5 mM | 1.5018 mL | 7.5092 mL | 15.0184 mL | | 10 mM | 0.7509 mL | 3.7546 mL | 7.5092 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： PBS Solubility: 120 mg/mL (901.10 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (15.62 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (15.62 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 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。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (15.62 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (15.62 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。 4. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (15.62 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (15.62 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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