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Necrostatin-1 (Nec-1)

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Necrostatin-1 (Nec-1) 是一種有效的壞死性凋亡 (necroptosis) 抑制劑，在 Jurkat 細(xì)胞中的 EC50 為 490 nM。Necrostatin-1 抑制 RIP1 激酶 (EC50=182 nM) 。Necrostatin-1 (Nec-1) 也是一種 (IDO) 抑制劑。

貨號(hào)：HY-15760
CAS：4311-88-0
參數(shù)品牌：MCE
產(chǎn)品參數(shù)
品牌：MCE
型號(hào)：HY-15760
起訂量：1
規(guī)格:：10mg
價(jià)格:：￥714
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產(chǎn)品詳情

Necrostatin-1 (Synonyms: Nec-1)

Necrostatin-1 (Nec-1) 是一種有效的壞死性凋亡 (necroptosis) 抑制劑，在 Jurkat 細(xì)胞中的 EC50 為 490 nM。Necrostatin-1 抑制 RIP1 激酶 (EC50=182 nM) 。Necrostatin-1 (Nec-1) 也是一種 (IDO) 抑制劑。


生物活性

Necrostatin-1 (Nec-1) is a potent necroptosis inhibitor with an EC50 of 490 nM in Jurkat cells. Necrostatin-1 inhibits RIP1 kinase (EC50=182 nM). Necrostatin-1 is also an IDO inhibitor[1].


IC50 & Target

EC50: 182 nM (RIP1 kinase)[1]


體外研究(In Vitro)

Necrostatin-1 (Nec-1) efficiently inhibits the TNFα-induced necrotic death of L929 cells, which does not require exogenous caspase inhibitors[1].
Necrostatin-1 (Nec-1) prevents radiocontrast media (RCM)-induced dilation of peritubular capillaries, suggesting a novel role unrelated to cell death for the RIP1 kinase domain in the regulation of microvascular hemodynamics and pathophysiology of contrast-induced AKI (CIAKI)[2].
Necrostatin-1 (Nec-1) (30 μM) increases the survival of cardiomyocyte progenitor cell (CMPCs) by inhibiting necrotic cell death[4].


體內(nèi)研究(In Vivo)

Necrostatin-1 (Nec-1) induces tubular bilation and affects the kinetics of the dilation of peritubular capillaries after RCM application. Upon a single intraperitoneal application of a single dose of Necrostatin-1 (1.65 mg/kg body weight, i.p.) 15 minutes before RCM, the return to baseline levels is prevented within the observation period[2].


分子量：259.33


Formula：C13H13N3OS


CAS 號(hào)：4311-88-0


運(yùn)輸條件：Room temperature in continental US; may vary elsewhere.


儲(chǔ)存方式：

Powder-20°C3 years

4°C2 years
In solvent-80°C6 months

-20°C1 month


溶解性數(shù)據(jù)


DMSO : ≥ 46 mg/mL (177.38 mM)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液
濃度溶劑體積質(zhì)量1 mg5 mg10 mg
1 mM3.8561 mL19.2805 mL38.5609 mL
5 mM0.7712 mL3.8561 mL7.7122 mL
10 mM0.3856 mL1.9280 mL3.8561 mL
*

請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。

In Vivo:

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

——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

  • 1.


    請(qǐng)依序添加每種溶劑： 0.5% CMC-Na/saline water

    Solubility: 12.5 mg/mL (48.20 mM); Suspended solution; Need ultrasonic


  • 2.


    請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (9.64 mM); Clear solution


  • 3.


    請(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (9.64 mM); Clear solution


  • 4.


    請(qǐng)依序添加每種溶劑： 10% (50% EtOH    50% Cremophor EL)    90% saline

    Solubility: 1.67 mg/mL (6.44 mM); Suspended solution; Need ultrasonic


參考文獻(xiàn)[1]. Degterev A, et al. Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury. Nat Chem Biol. 2005 Jul;1(2):112-9.

[2]. Linkermann A, et al. The RIP1-kinase inhibitor necrostatin-1 prevents osmotic nephrosis and contrast-induced AKI in mice. J Am Soc Nephrol. 2013 Oct;24(10):1545-57.

[3]. Huang C, et al. Shikonin kills glioma cells through necroptosis mediated by RIP-1. PLoS One. 2013 Jun 28;8(6):e66326.

[4]. Feyen D, et al. Increasing short-term cardiomyocyte progenitor cell (CMPC) survival by necrostatin-1 did not further preserve cardiac function. Cardiovasc Res. 2013 Jul 1;99(1):83-91.

[5]. Zhou K, et al. RIP1-RIP3-DRP1 pathway regulates NLRP3 inflammasome activation following subarachnoid hemorrhage. Exp Neurol. 2017 Sep;295:116-124.







Necrostatin-1 (Nec-1)
Necrostatin-1 (Nec-1)

Necrostatin-1 (Nec-1)

分享到微信

×
Necrostatin-1 (Nec-1) 是一種有效的壞死性凋亡 (necroptosis) 抑制劑，在 Jurkat 細(xì)胞中的 EC50 為 490 nM。Necrostatin-1 抑制 RIP1 激酶 (EC50=182 nM) 。Necrostatin-1 (Nec-1) 也是一種 (IDO) 抑制劑。

貨號(hào)：HY-15760
CAS：4311-88-0
品牌：MCE
型號(hào)：HY-15760
起訂量：1
規(guī)格:：10mg
價(jià)格:：￥714
15906629305
在線客服
產(chǎn)品詳情

Necrostatin-1 (Synonyms: Nec-1)

Necrostatin-1 (Nec-1) 是一種有效的壞死性凋亡 (necroptosis) 抑制劑，在 Jurkat 細(xì)胞中的 EC50 為 490 nM。Necrostatin-1 抑制 RIP1 激酶 (EC50=182 nM) 。Necrostatin-1 (Nec-1) 也是一種 (IDO) 抑制劑。


生物活性

Necrostatin-1 (Nec-1) is a potent necroptosis inhibitor with an EC50 of 490 nM in Jurkat cells. Necrostatin-1 inhibits RIP1 kinase (EC50=182 nM). Necrostatin-1 is also an IDO inhibitor[1].


IC50 & Target

EC50: 182 nM (RIP1 kinase)[1]


體外研究(In Vitro)

Necrostatin-1 (Nec-1) efficiently inhibits the TNFα-induced necrotic death of L929 cells, which does not require exogenous caspase inhibitors[1].
Necrostatin-1 (Nec-1) prevents radiocontrast media (RCM)-induced dilation of peritubular capillaries, suggesting a novel role unrelated to cell death for the RIP1 kinase domain in the regulation of microvascular hemodynamics and pathophysiology of contrast-induced AKI (CIAKI)[2].
Necrostatin-1 (Nec-1) (30 μM) increases the survival of cardiomyocyte progenitor cell (CMPCs) by inhibiting necrotic cell death[4].


體內(nèi)研究(In Vivo)

Necrostatin-1 (Nec-1) induces tubular bilation and affects the kinetics of the dilation of peritubular capillaries after RCM application. Upon a single intraperitoneal application of a single dose of Necrostatin-1 (1.65 mg/kg body weight, i.p.) 15 minutes before RCM, the return to baseline levels is prevented within the observation period[2].


分子量：259.33


Formula：C13H13N3OS


CAS 號(hào)：4311-88-0


運(yùn)輸條件：Room temperature in continental US; may vary elsewhere.


儲(chǔ)存方式：

Powder-20°C3 years

4°C2 years
In solvent-80°C6 months

-20°C1 month


溶解性數(shù)據(jù)


DMSO : ≥ 46 mg/mL (177.38 mM)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液
濃度溶劑體積質(zhì)量1 mg5 mg10 mg
1 mM3.8561 mL19.2805 mL38.5609 mL
5 mM0.7712 mL3.8561 mL7.7122 mL
10 mM0.3856 mL1.9280 mL3.8561 mL
*

請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。

In Vivo:

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

——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

  • 1.


    請(qǐng)依序添加每種溶劑： 0.5% CMC-Na/saline water

    Solubility: 12.5 mg/mL (48.20 mM); Suspended solution; Need ultrasonic


  • 2.


    請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (9.64 mM); Clear solution


  • 3.


    請(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (9.64 mM); Clear solution


  • 4.


    請(qǐng)依序添加每種溶劑： 10% (50% EtOH    50% Cremophor EL)    90% saline

    Solubility: 1.67 mg/mL (6.44 mM); Suspended solution; Need ultrasonic


參考文獻(xiàn)[1]. Degterev A, et al. Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury. Nat Chem Biol. 2005 Jul;1(2):112-9.

[2]. Linkermann A, et al. The RIP1-kinase inhibitor necrostatin-1 prevents osmotic nephrosis and contrast-induced AKI in mice. J Am Soc Nephrol. 2013 Oct;24(10):1545-57.

[3]. Huang C, et al. Shikonin kills glioma cells through necroptosis mediated by RIP-1. PLoS One. 2013 Jun 28;8(6):e66326.

[4]. Feyen D, et al. Increasing short-term cardiomyocyte progenitor cell (CMPC) survival by necrostatin-1 did not further preserve cardiac function. Cardiovasc Res. 2013 Jul 1;99(1):83-91.

[5]. Zhou K, et al. RIP1-RIP3-DRP1 pathway regulates NLRP3 inflammasome activation following subarachnoid hemorrhage. Exp Neurol. 2017 Sep;295:116-124.







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