MCC950 sodium

MCC950 sodium (CP-456773 sodium; CRID3 sodium salt) 是一種有效，選擇性的 NLRP3 抑制劑，在BMDMs 和 HMDMs中的 IC50 分別為 7.5 nM 和 8.1 nM。

貨號：HY-12815A
CAS： 256373-96-3

參數(shù)品牌：MCE

產(chǎn)品參數(shù)

品牌：MCE

型號：HY-12815A

起訂量：1

規(guī)格:：10mg

價格:：￥950

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產(chǎn)品詳情

MCC950 sodium

MCC950 sodium (CP-456773 sodium; CRID3 sodium salt) 是一種有效，選擇性的 NLRP3 抑制劑，在BMDMs 和 HMDMs中的 IC₅₀ 分別為 7.5 nM 和 8.1 nM。

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.

IC₅₀ & Target

IC50: 7.5 nM (NLRP3, in BMDMs), 8.1 nM (NLRP3, in HMDMs)^[1]

體外研究(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^[1].

體內(nèi)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^[1].

分子量：426.46

Formula：C₂₀H₂₃N₂NaO₅S

CAS 號：256373-96-3

運輸條件：Room temperature in continental US; may vary elsewhere.

儲存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性數(shù)據(jù)

DMSO : 50 mg/mL (117.24 mM; Need ultrasonic)

H₂O : ≥ 30 mg/mL (70.35 mM)

* "≥" means soluble, but saturation unknown.

配制儲備液

濃度溶劑體積質(zhì)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

*

請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。

In Vivo:

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：

——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

1.

請依序添加每種溶劑： PBS
Solubility: 6.25 mg/mL (14.66 mM); Clear solution; Need ultrasonic
2.

請依序添加每種溶劑： 5%DMSO 95%PBS
Solubility: ≥ 5 mg/mL (11.72 mM); Clear solution
3.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution
4.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution
5.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution
6.

請依序添加每種溶劑： 2％DMSO 98％PBS
Solubility: ≥ 2 mg/mL (4.69 mM); Clear solution

參考文獻

[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]. 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.

MCC950 sodium

MCC950 sodium (CP-456773 sodium; CRID3 sodium salt) 是一種有效，選擇性的 NLRP3 抑制劑，在BMDMs 和 HMDMs中的 IC50 分別為 7.5 nM 和 8.1 nM。

貨號：HY-12815A
CAS： 256373-96-3

品牌：MCE

型號：HY-12815A

起訂量：1

規(guī)格:：10mg

價格:：￥950

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產(chǎn)品詳情

MCC950 sodium

MCC950 sodium (CP-456773 sodium; CRID3 sodium salt) 是一種有效，選擇性的 NLRP3 抑制劑，在BMDMs 和 HMDMs中的 IC₅₀ 分別為 7.5 nM 和 8.1 nM。

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.

IC₅₀ & Target

IC50: 7.5 nM (NLRP3, in BMDMs), 8.1 nM (NLRP3, in HMDMs)^[1]

體外研究(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^[1].

體內(nèi)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^[1].

分子量：426.46

Formula：C₂₀H₂₃N₂NaO₅S

CAS 號：256373-96-3

運輸條件：Room temperature in continental US; may vary elsewhere.

儲存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性數(shù)據(jù)

DMSO : 50 mg/mL (117.24 mM; Need ultrasonic)

H₂O : ≥ 30 mg/mL (70.35 mM)

* "≥" means soluble, but saturation unknown.

配制儲備液

濃度溶劑體積質(zhì)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

*

請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。

In Vivo:

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：

——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

1.

請依序添加每種溶劑： PBS
Solubility: 6.25 mg/mL (14.66 mM); Clear solution; Need ultrasonic
2.

請依序添加每種溶劑： 5%DMSO 95%PBS
Solubility: ≥ 5 mg/mL (11.72 mM); Clear solution
3.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution
4.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution
5.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution
6.

請依序添加每種溶劑： 2％DMSO 98％PBS
Solubility: ≥ 2 mg/mL (4.69 mM); Clear solution

參考文獻

[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]. 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.

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MCC950 sodium

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MCC950 sodium