MCC950 sodium|256373-96-3|(CP-456773 sodium; CRID3 sodium salt)-陌孚医药/Medlife

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MCC950 sodium (Synonyms: CP-456773 sodium; CRID3 sodium salt)

目录号: PC16942 纯度: ≥98%

CAS No. :256373-96-3

商品编号	规格	价格	会员价
PC16942-10mg	10mg	¥735.00	请登录
PC16942-50mg	50mg	¥3067.40	请登录
PC16942-200mg	200mg	¥6840.40	请登录

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中文名称	MCC950 sodium
中文别名	N-[[(1,2,3,5,6,7-六氢-S-引达省-4-基)氨基]羰基]-4-(1-羟基-1-甲基乙基)-2-呋喃磺酰胺单钠盐
英文名称	CRID3 sodium salt
英文别名	CRID3 sodium salt;MCC950(CP-456773) sodium;CP456773 sodium;CP-456773 sodium;CRID-3 sodium salt;MCC-950 sodium;CRID3;Cytokine release inhibitory drug 3;MCC950;N-[[(1,2,3,5,6,7-Hexahydro-s-indacen-4-yl)amino]carbonyl]-4-(1-hydroxy-1-methylethyl)-2-furansulfonamide sodium salt;MCC950 (sodium);MCC950 sodium;MCC950 sodium salt;AOB6854;MCC 950;BCP16648;s7809;AK547693;sodium;1,2,3,5,6,7-hexahydro-s-indacen-4-ylcarbamoyl-[4-(2-hydroxypropan-2-yl)
Cas No.	256373-96-3
分子式	C₂₀H₂₃N₂NaO₅S
分子量	426.46
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性	MCC950 sodium (CP-456773 sodium; CRID3 sodium salt) is a potent, selective NLRP3 inhibitor with IC₅₀s of 7.5 and 8.1 nM in BMDMs and HMDMs, respectively.
性状	Solid
IC50 & Target[1][2]	IC50: 7.5 nM (NLRP3, in BMDMs), 8.1 nM (NLRP3, in HMDMs)
体外研究(In Vitro)	MCC950 blocks canonical and non-canonical NLRP3 activation at nanomolar concentrations. MCC950 specifically inhibits NLRP3 but not AIM2, NLRC4 or NLRP1 activation. The effect of MCC950 on NLRP3 inflammasome activation is tested in mouse bone marrow derived macrophages (BMDM) and human monocyte derived macrophages (HMDM). The IC₅₀ of MCC950 in BMDM is approximately 7.5 nM, while in HMDM it has a similar inhibitory capacity (IC₅₀=8.1 nM). MCC950 also dose dependently inhibit IL-1β but not TNF-α secretion.MCC950 specifically blocks caspase-11-directed NLRP3 activation and IL-1β secretion upon stimulation of the non-canonical pathway. NLRC4-stimulated IL-1β and TNF-α secretion (as activated by Salmonella typhimurium) are not inhibited by MCC950 even at a concentration of 10 μM. MCC950 does not inhibit caspase-1 activation or IL-1β processing in response to S. typhimurium. The expression of pro-caspase-1 and pro-IL-1β in cell lysates is not substantially affected by MCC950 treatment. Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	MCC950 reduces Interleukin-1p (IL-1β) production and attenuates the severity of experimental autoimmune encephalomyelitis (EAE), a disease model of multiple sclerosis. Pre-treatment with MCC950 reduces serum concentrations of IL-1β and IL-6 while it does not considerably decrease the amount of TNF-α. Treatment of mice with MCC950 delays the onset and reduced the severity of EAE. Intracellular cytokine staining and FACS analysis of brain mononuclear cells from mice sacrificed on day 22 shows modestly reduced frequencies of IL-17 and IFN-γ producing CD3 T cells in MCC950 treated mice in comparison with PBS-treated mice. IFN-γ and particularly IL-17 producing cell numbers are also reduced in both the CD4 and γδ sub-populations of CD3 T cells. Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature or refrigerated transportation.
储存方式	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[1]. Coll RC, et al. A small-molecule inhibitor of the NLRP3 inflammasome for the treatment of inflammatory diseases. Nat Med. 2015 Mar;21(3):248-55. [Information] [2]. Zhai Y, et al. Inhibiting the NLRP3 Inflammasome Activation with MCC950 Ameliorates Diabetic Encephalopathy in db/db Mice. Molecules. 2018 Feb 27;23(3). pii: E522. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (234.49 mM; Need ultrasonic)

H₂O : ≥ 30 mg/mL (70.35 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3449 mL	11.7244 mL	23.4489 mL
5 mM	0.4690 mL	2.3449 mL	4.6898 mL
10 mM	0.2345 mL	1.1724 mL	2.3449 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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 (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： PBS
Solubility: 6.25 mg/mL (14.66 mM); Clear solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： 5%DMSO 95%PBS
Solubility: ≥ 5 mg/mL (11.72 mM); Clear solution
3.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.86 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.86 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.86 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.86 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
5.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.88 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 ddH?O 中，得到澄清透明的生理盐水溶液
6.

建议依照次序添加每种溶剂： 2％DMSO 98％PBS
Solubility: ≥ 2 mg/mL (4.69 mM); Clear solution

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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