MCC950

カタログ番号 T3701 CAS 210826-40-7

別名: CP-456773

CP-456773 (MCC950 (CP-456773) and CRID3) is an effective and specific cytokine release inhibitor and NLRP3 inflammasome inhibitor. CP-456773 inhibits IL-1β secretion and caspase 1 processing. MCC950 blocked canonical and noncanonical NLRP3 activation at nanomolar concentrations. MCC950 specifically inhibited activation of NLRP3 but not the AIM2, NLRC4 or NLRP1 inflammasomes. MCC950 reduced IL-1β production in vivo and attenuated the severity of experimental autoimmune encephalomyelitis (EAE), a disease model of multiple sclerosis.

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MCC950, CAS 210826-40-7

パッケージサイズ	在庫状況	単価(税別)
サンプルについてお問い合わせ
2 mg	在庫あり	￥ 10,000
5 mg	在庫あり	￥ 12,500
10 mg	在庫あり	￥ 20,500
25 mg	在庫あり	￥ 44,000
50 mg	在庫あり	￥ 79,000
100 mg	在庫あり	￥ 140,500
1 mL * 10 mM (in DMSO)	在庫あり	￥ 13,000

バルクのお問い合わせ

バッチを選択

DATASHEET SDS

バッチの詳細情報はお問い合わせください

化学的特性

保存条件 & 溶解度情報

ターゲット＆IC50	HMDM:8.1 nM, BMDM:7.5nM
In vitro	MCC950 effectively inhibits both canonical and non-canonical NLRP3 activators at nanomolar concentrations, distinguishing its specificity towards NLRP3 inhibition while not affecting AIM2, NLRC4, or NLRP1 activations. Its impact on NLRP3 inflammasome activity was evaluated in both mouse bone marrow-derived macrophages (BMDM) and human monocyte-derived macrophages (HMDM), demonstrating similar IC50 values of approximately 7.5 nM and 8.1 nM, respectively. MCC950 selectively reduces IL-1β secretion without influencing TNF-α levels, and it uniquely prevents caspase-11-mediated NLRP3 and IL-1β activation in the non-canonical pathway. However, MCC950 does not suppress NLRC4-induced IL-1β and TNF-α secretion, even at concentrations up to 10 μM, and fails to block caspase-1 activation or IL-1β processing following Salmonella typhimurium exposure. Furthermore, MCC950 does not markedly alter the expression levels of pro-caspase-1 and pro-IL-1β in treated cell lysates[1].
In vivo	MCC950 effectively lowers production of Interleukin-1β (IL-1β) and lessens the severity of experimental autoimmune encephalomyelitis (EAE), serving as a model for multiple sclerosis. It not only reduces serum levels of IL-1β and IL-6 without significantly affecting TNF-α concentrations but also delays the onset and diminishes the severity of EAE in treated mice. Furthermore, analysis through intracellular cytokine staining and FACS of brain mononuclear cells from mice euthanized on day 22 reveals that MCC950 treatment slightly decreases the prevalence of IL-17 and IFN-γ producing CD3+ T cells, in comparison to PBS-treated controls. Notably, the numbers of cells producing IFN-γ and especially IL-17 are lower in both CD4+ and γδ+ subsets of CD3+ T cells.

別名	CP-456773
分子量	404.48
分子式	C20H24N2O5S
CAS No.	210826-40-7

保存条件

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度情報

DMSO: 28 mg/mL

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. 2. Li L H, Chen T L, Chiu H W, et al. Critical Role for the NLRP3 Inflammasome in Mediating IL-1β Production in Shigella sonnei-Infected Macrophages[J]. Frontiers in Immunology. 2020, 11: 1115. 3. Li L H, Lin J S, Chiu H W, et al. Mechanistic insight into the activation of the NLRP3 inflammasome by Neisseria gonorrhoeae in macrophages[J]. Frontiers in Immunology. 2019, 10: 1815. 4. Li S, Hui Y, Yuan J, et al. Syk-Targeted, a New 3-Arylbenzofuran Derivative EAPP-2 Blocks Airway Inflammation of Asthma–COPD Overlap in vivo and in vitro[J]. Journal of Inflammation Research. 2021, 14: 2173-2185. 5. Wu C H, Gan C H, Li L H, et al. A Synthetic Small Molecule F240B Decreases NLRP3 Inflammasome Activation by Autophagy Induction[J]. Frontiers in Immunology. 2020, 11. 6. Xie D, Ge X, Ma Y, et al. Clemastine improves hypomyelination in rats with hypoxic–ischemic brain injury by reducing microglia-derived IL-1β via P38 signaling pathway[J]. Journal of Neuroinflammation. 2020, 17(1): 1-17. 7. Chen Y Q, Wang S N, Shi Y J, et al. CRID3, a blocker of apoptosis associated speck like protein containing a card, ameliorates murine spinal cord injury by improving local immune microenvironment[J]. Journal of Neuroinflammation. 2020, 17(1): 1-18. 8. Wei Shi, Guang Xu, Xiaoyan Zhan, Yuan Gao, Zhilei Wang, Shubin Fu, Nan Qin, Xiaorong Hou, Yongqiang Ai, Chunyu Wang, Tingting He, Hongbin Liu, Yuanyuan Chen, Yan Liu, Jiabo Wang, Ming Niu, Yuming Guo, Xiaohe Xiao & Zhaofang Bai. Carnosol inhibits inflammasome activation by directly targeting HSP90 to treat inflammasome-mediated diseases. Cell death & disease. 2020 9. Zhilei Wang, Guang Xu, Yuan Gao, Xiaoyan Zhan, Nan Qin, Shubin Fu, Ruisheng Li et al. Cardamonin from a medicinal herb protects against LPS-induced septic shock by suppressing NLRP3 inflammasome [J]. Acta Pharmaceutica Sinica B. 2019 Feb 14.

引用文献

1. Shi W, Xu G, Gao Y, et al.Novel role for epalrestat: protecting against NLRP3 inflammasome-driven NASH by targeting aldose reductase.Journal of Translational Medicine.2023, 21(1): 1-17. 2. Li N, Jiang X, Zhang R, et al.Discovery of Triazinone Derivatives as Novel, Specific, and Direct NLRP3 Inflammasome Inhibitors for the Treatment of DSS-Induced Ulcerative Colitis.Journal of Medicinal Chemistry.2023 3. Cao X, Di G, Bai Y, et al.Aquaporin5 Deficiency Aggravates ROS/NLRP3 Inflammasome-Mediated Pyroptosis in the Lacrimal Glands.Investigative Ophthalmology & Visual Science.2023, 64(1): 4-4. 4. Li Q, Zhao P, Wen Y, et al.POLYDATIN AMELIORATES TRAUMATIC BRAIN INJURY–INDUCED SECONDARY BRAIN INJURY BY INHIBITING NLRP3-INDUCED NEUROINFLAMMATION ASSOCIATED WITH SOD2 ACETYLATION.Shock.2023, 59(3): 460-468. 5. Chen Y Q, Wang S N, Shi Y J, et al. CRID3, a blocker of apoptosis associated speck like protein containing a card, ameliorates murine spinal cord injury by improving local immune microenvironment. Journal of Neuroinflammation. 2020, 17(1): 1-18. 6. Li S, Hui Y, Yuan J, et al. Syk-Targeted, a New 3-Arylbenzofuran Derivative EAPP-2 Blocks Airway Inflammation of Asthma–COPD Overlap in vivo and in vitro. Journal of Inflammation Research. 2021, 14: 2173-2185. 7. Zhang H, Gao J, Fang W, et al. Role of NINJ1 in Gout Flare and Potential as a Drug Target. Journal of Inflammation Research. 2022, 15: 5611-5620. 8. Gao Y, Xu G, Ma L, et al. Icariside I specifically facilitates ATP or nigericin-induced NLRP3 inflammasome activation and causes idiosyncratic hepatotoxicity. Cell Communication and Signaling. 2021 Feb 11;19(1):13. doi: 10.1186/s12964-020-00647-1. 9. Yang S R, Hua K F, Yang C Y, et al. Cf‐02, a novel benzamide‐linked small molecule, blunts NF‐κB activation and NLRP3 inflammasome assembly and improves acute onset of accelerated and severe lupus nephritis in mice. The FASEB Journal. 2021, 35(8): e21785. 10. Qin N, Xu G, Wang Y, et al. Bavachin enhances NLRP3 inflammasome activation induced by ATP or nigericin and causes idiosyncratic hepatotoxicity. Frontiers of Medicine. 2021 Aug;15(4):594-607.

11. Niu L, Luo S S, Xu Y, et al. The critical role of the hippocampal NLRP3 inflammasome in social isolation-induced cognitive impairment in male mice. Neurobiology of Learning and Memory. 2020: 107301 12. Gao Y, Xu G, Ma L, et al. Icarisid I specifically facilitates ATP or nigericin-induced NLRP3 inflammasome activation and causes idiosyncratic hepatotoxicity. Cell Communication and Signaling. 2020 13. Wu C H, Gan C H, Li L H, et al. A Synthetic Small Molecule F240B Decreases NLRP3 Inflammasome Activation by Autophagy Induction. Frontiers in Immunology. 2020 Dec 18;11:607564. doi: 10.3389/fimmu.2020.607564. eCollection 2020. 14. Meng Z, Liu H, Zhang J, et al. Sesamin promotes apoptosis and pyroptosis via autophagy to enhance antitumour effects on murine T-cell lymphoma. Journal of Pharmacological Sciences. 2021 15. Wei Shi, Guang Xu, Xiaoyan Zhan, Yuan Gao, Zhilei Wang, Shubin Fu, Nan Qin, Xiaorong Hou, Yongqiang Ai, Chunyu Wang, Tingting He, Hongbin Liu, Yuanyuan Chen, Yan Liu, Jiabo Wang, Ming Niu, Yuming Guo, Xiaohe Xiao & Zhaofang Bai Carnosol inhibits inflammasome activation by directly targeting HSP90 to treat inflammasome-mediated diseases. Cell Death & Disease. 2020 16. Tian C, Han X, He L, et al. Transient receptor potential ankyrin 1 contributes to the ATP-elicited oxidative stress and inflammation in THP-1-derived macrophage. Molecular and Cellular Biochemistry. 2020: 1-14 17. Li L H, Chen T L, Chiu H W, et al. Critical Role for the NLRP3 Inflammasome in Mediating IL-1β Production in Shigella sonnei-Infected Macrophages. Frontiers in Immunology. 2020, 11: 1115 18. Li L H, Lin J S, Chiu H W, et al. Mechanistic insight into the activation of the NLRP3 inflammasome by Neisseria gonorrhoeae in macrophages. Frontiers in Immunology. 2019, 10: 1815 19. Wang Z, Xu G, Gao Y, et al. Cardamonin from a medicinal herb protects against LPS-induced septic shock by suppressing NLRP3 inflammasome. Acta Pharmaceutica Sinica B. 2019, 9(4): 734-744 20. Tian C, Huang R, Tang F, et al. Transient Receptor Potential Ankyrin 1 Contributes to Lysophosphatidylcholine-Induced Intracellular Calcium Regulation and THP-1-Derived Macrophage Activation. The Journal of Membrane Biology. 2019: 1-13 21. Xie D, Ge X, Ma Y, et al. Clemastine improves hypomyelination in rats with hypoxic–ischemic brain injury by reducing microglia-derived IL-1β via P38 signaling pathway. Journal of neuroinflammation. 2020, 17(1): 1-17. 22. Ni B, Pei W, Qu Y, et al. MCC950, the NLRP3 Inhibitor, Protects against Cartilage Degradation in a Mouse Model of Osteoarthritis. Oxidative Medicine and Cellular Longevity. 2021, 2021. 23. Yuan X, Chen P, Luan X, et al.NLRP3 deficiency protects against acetaminophen‑induced liver injury by inhibiting hepatocyte pyroptosis.Molecular Medicine Reports.2024, 29(4): 1-15. 24. Chiu H W, Wu C H, Lin W Y, et al.The Angiotensin II Receptor Neprilysin Inhibitor LCZ696 Inhibits the NLRP3 Inflammasome By Reducing Mitochondrial Dysfunction in Macrophages and Alleviates Dextran Sulfate Sodium-induced Colitis in a Mouse Model.Inflammation.2024: 1-22.

もっと見る隠し

投与量変換

You can also refer to dose conversion for different animals. 詳細

In vivo投与量計算 (透明溶液)

ステップ1: 以下の情報を入力してください

投与量

mg/kg

動物の平均体重

動物あたりの投与量

動物数

溶媒の組成を入力してください

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

計算するリセット

計算結果:

作業濃度: mg/ml;

DMSO溶液の作成方法: mg あらかじめ溶解した薬剤 μL DMSO (マスター溶液の濃度 mg/mL)，濃度がそのバッチの薬剤のDMSO溶解度を超える場合は、まずご連絡ください。

生体内薬剤の調合法：取る μL DMSO マスター溶液、次に追加 μL PEG300，確実に混ぜてから加える μL Tween 80，確実に混ぜてから加える μL ddH₂O, 確実に混ぜる

お問合せ内容:

必ず順番通りに溶媒を加えてください。ボルテックスミキサーや超音波、湯煎することで溶解しやすくなります

計算器

モル濃度計算機

希釈計算機

再構成計算

分子量計算機

質量

濃度

体積

分子量

モル度計算機では以下の計算が可能です

既知の体積と濃度の溶液を調製するために必要な化合物の質量
質量が既知の化合物を目的の濃度まで溶解させるのに必要な溶液の量
特定の体積の中に既知の質量の化合物を入れて得られる溶液の濃度

参考例

モル濃度計算機を使用したモル濃度計算の例
化合物の分子量が197.13g/molである場合、10mlの水に10mMのストック溶液を作るのに必要な化合物の質量はどれくらいですか？
［分子量（MW）］の欄に［197.13］と入力してください
[濃度]ボックスに10と入力し、正しい単位（millimolar）を選択します
[容量]ボックスに10と入力し、正しい単位（milliliter）を選択します
計算を押します
答えの19.713mgが質量欄に表示されます

濃度 (開始)

体積 (開始)

濃度 (終了)

体積 (終了)

溶液を作るのに必要な希釈率の計算

溶液の調製に必要な希釈率の算出
希釈計算機は、既知の濃度の原液をどのように希釈するかを計算することができる便利なツールです。V1を計算するためにC1、C2＆V2を入力します。

参考例

Tocrisの希釈計算器を用いた希釈計算の一例
50μMの溶液を20ml作るためには、10mMの原液を何ml必要ですか？
C1V1=C2V2という式を用いて、C1=10mM、C2=50μM、V2=20ml、V1を未知数とします。
濃度（開始）ボックスに10を入力し正しい単位(millimolar)を選択してください
濃度（終了）ボックスに50を入力し正しい単位(millimolar)を選択してください
体積（終了）ボックスに20を入力し正しい単位(millimolar)を選択してください
計算を押します
100 microliter (0.1 ml) という答えが体積（開始）ボックスに表示されます。

分子式

分子量 g/mol

化合物の化学式を入力して、そのモル質量や元素組成を計算します

Tヒント：化学式は大文字と小文字を区別します。: C10H16N2O2 c10h16n2o2

化合物のモル質量（分子量）を計算する手順:
化学物質のモル質量を計算するには、その化学式を入力し、「計算」をクリックしてください。.
分子質量、分子量、モル質量、モル重量の定義:
分子質量（分子量）とは、物質の1分子の質量であり、統一された原子質量単位（u）で表されます。(1uは炭素12の1原子の質量の1/12に等しい）
モル質量（molar weight）とは、ある物質の1モルの質量のことで、単位はg/molです。

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技術サポート

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

MCC950 210826-40-7 Immunology/Inflammation NF-Κb NOD CP 456773 MCC 950 Inhibitor CRID-3 NOD-like Receptor (NLR) inhibit CP-456773 MCC-950 CRID3 CP456773 CRID 3 inhibitor

本ウェブサイトに掲載されている製品は全て研究用試薬です。研究目的以外の用途にはご使用できません。

MCC950

保存条件

溶解度情報

参考文献

引用文献

関連化合物ライブラリー

関連製品

投与量変換

In vivo投与量計算 (透明溶液)

計算器

モル度計算機では以下の計算が可能です

溶液を作るのに必要な希釈率の計算

バイアルを再構成するのに必要な溶媒の量を計算する.

化合物の化学式を入力して、そのモル質量や元素組成を計算します

技術サポート

Keywords