Dapansutrile OLT1177|cas:54863-37-5|西域试剂

Dapansutrile OLT1177,98.0%

产品编号：Bellancom-17629| CAS NO：54863-37-5| 分子式：C₄H₇NO₂S| 分子量：133.17

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货号	价格	库存与货期
Bellancom-17629	￥500.00	杭州北京（现货）
Bellancom-17629	￥850.00	杭州北京（现货）
Bellancom-17629	￥2800.00	杭州北京（现货）
Bellancom-17629	￥4500.00	杭州北京（现货）

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Dapansutrile OLT1177

产品介绍

Dapansutrile (OLT1177) 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 (OLT1177) is a potent, orally active and selective NLRP3 inflammasome inhibitor. Dapansutrile has anti-inflammatory activity and decreases immune factor levels. Dapansutrile can be used for research of inflammatory diseases.

体外研究

体内研究

Dapansutrile (3.75 g/kg; p.o.; daily, for 22 d) ameliorates neurological decline and nervous tissue damage in experimental autoimmune encephalomyelitis (EAE) mice.
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.
Dapansutrile (6-600 mg/kg; i.p.; once; male ICR (CD1) mice) reduces infarct size and reduces caspase-1 activity in the heart.
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.

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

Animal Model:	EAE-induced female adult C57BL/6 (8–10 weeks old)
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 (CD45^high, CD11b⁺, F4/80⁺), microglia (CD45^low, CD11b⁺), and other cells (CD45⁺, CD11b^-, CD3^-, CD24⁺).

Animal Model:	Male ICR (CD1) mice (8-12 weeks old)
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)
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.

体内研究

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

Animal Model:	EAE-induced female adult C57BL/6 (8–10 weeks old)
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 (CD45^high, CD11b⁺, F4/80⁺), microglia (CD45^low, CD11b⁺), and other cells (CD45⁺, CD11b^-, CD3^-, CD24⁺).

Animal Model:	Male ICR (CD1) mice (8-12 weeks old)
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)
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (750.92 mM)

H₂O : 36.67 mg/mL (275.36 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°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。

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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
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。