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  2. Metabolic Enzyme/Protease
  3. PCSK9
  4. R-IMPP

R-IMPP (PF-00932239) 是一種 PCSK9 的抗分泌活性分子 (IC50=4.8 μM)，其靶向 80S 核糖體抑制 PCSK9 蛋白翻譯。

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R-IMPP Chemical Structure

R-IMPP Chemical Structure

CAS No. : 2133832-83-2

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規(guī)格 價(jià)格 是否有貨 數(shù)量
1 mg ￥419
In-stock
5 mg ￥1400
In-stock
10 mg ￥2240
In-stock
25 mg ￥4060
In-stock
50 mg ￥5950
In-stock
100 mg 現(xiàn)貨 詢價(jià)
200 mg   詢價(jià)  
500 mg   詢價(jià)  

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Customer Review

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

R-IMPP (PF-00932239) is an anti-secretagogue of PCSK9 (IC50=4.8 μM), which targets the 80S ribosome to inhibit PCSK9 protein translation[1].

IC50 & Target

IC50: 4.8 μM (PCSK9)[1]
細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
Bone marrow cell IC50
> 20 μM
Compound: 1; PF-00932239
Cytotoxicity against rat bone marrow cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay
Cytotoxicity against rat bone marrow cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo assay
[PMID: 29878763]
CHO-K1 IC50
< 10 μM
Compound: 1; R-IMPP, PF-00932239
Inhibition of human recombinant full length ProLabel-tagged PCSK9 expressed in CHO-K1 cells incubated overnight and measured after 3 days by chemiluminescence assay
Inhibition of human recombinant full length ProLabel-tagged PCSK9 expressed in CHO-K1 cells incubated overnight and measured after 3 days by chemiluminescence assay
[PMID: 30448414]
CHO-K1 IC50
> 10 μM
Compound: 1; R-IMPP, PF-00932239
Inhibition of human recombinant PCSK9 expressed in CHO-K1 cells assessed as alkaline phosphatase secretion incubated overnight and measured after 3 days by HTS assay
Inhibition of human recombinant PCSK9 expressed in CHO-K1 cells assessed as alkaline phosphatase secretion incubated overnight and measured after 3 days by HTS assay
[PMID: 30448414]
CHO-K1 IC50
> 10 μM
Compound: 1; R-IMPP, PF-00932239
Cytotoxicity against CHOK1 cells expressing human recombinant full length ProLabel-tagged PCSK9 after overnight incubation by CellTiter blue assay
Cytotoxicity against CHOK1 cells expressing human recombinant full length ProLabel-tagged PCSK9 after overnight incubation by CellTiter blue assay
[PMID: 30448414]
CHO-K1 IC50
4.8 μM
Compound: 1; R-IMPP, PF-00932239
Inhibition of human recombinant full length ProLabel-tagged PCSK9 expressed in CHO-K1 cells incubated overnight and measured after 3 days by HTS assay
Inhibition of human recombinant full length ProLabel-tagged PCSK9 expressed in CHO-K1 cells incubated overnight and measured after 3 days by HTS assay
[PMID: 30448414]
CHO-K1 IC50
4.8 μM
Compound: Fig 8, Cpd 80S
Inhibition of 80s ribosome in CHOK1 cells assessed as reduction in PL-tagged PCSK9 expression incubated for over night by EFC kit method
Inhibition of 80s ribosome in CHOK1 cells assessed as reduction in PL-tagged PCSK9 expression incubated for over night by EFC kit method
[PMID: 31673315]
HeLa IC50
8.04 μM
Compound: 1; PF-00932239
Binding affinity to 80S ribosome in human HeLa cells lysates using human full length PCSK9 encoding mRNAs assessed as inhibition of PCSK9 mRNA translation after 45 mins by Steady-Glo luciferase reporter gene assay
Binding affinity to 80S ribosome in human HeLa cells lysates using human full length PCSK9 encoding mRNAs assessed as inhibition of PCSK9 mRNA translation after 45 mins by Steady-Glo luciferase reporter gene assay
[PMID: 30482620]
Huh-7 IC50
2.2 μM
Compound: 13; R-IMPP
Inhibition of PCSK9 expression in human HuH7 cells after overnight incubation by ELISA
Inhibition of PCSK9 expression in human HuH7 cells after overnight incubation by ELISA
[PMID: 29519739]
Huh-7 IC50
2.63 μM
Compound: 1; PF-00932239
Binding affinity to 80S ribosome in human HuH7 cells harboring human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay
Binding affinity to 80S ribosome in human HuH7 cells harboring human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay
[PMID: 30482620]
Huh-7 IC50
2.63 μM
Compound: 1; PF-00932239
Binding affinity to 80S ribosome in human HuH7 cells harboring pCMV-truncated human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay
Binding affinity to 80S ribosome in human HuH7 cells harboring pCMV-truncated human PCSK9 (1 to 152 residues)-proLuc assessed as inhibition of PCSK9 mRNA translation after overnight incubation by luciferase reporter gene assay
[PMID: 29878763]
Huh-7 IC50
8.37 μM
Compound: 1; PF-00932239
Binding affinity to 80S ribosome in human HuH7 cells assessed as inhibition of PCSK9 mRNA translation after overnight incubation by ELISA
Binding affinity to 80S ribosome in human HuH7 cells assessed as inhibition of PCSK9 mRNA translation after overnight incubation by ELISA
[PMID: 29878763]
體外研究
(In Vitro)

R-IMPP 通過增加 LDL-R 水平刺激肝癌細(xì)胞攝取 LDL-C，而不改變分泌的轉(zhuǎn)鐵蛋白水平。R-IMPP 不會(huì)降低 PCSK9 轉(zhuǎn)錄或增加 PCSK9 降解，但會(huì)導(dǎo)致轉(zhuǎn)錄依賴性 PCSK9 翻譯抑制。R-IMPP 能夠選擇性地與人類核糖體結(jié)合，但不能與大腸桿菌核糖體結(jié)合[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

389.49

Formula

C24H27N3O2
CAS 號
性狀

固體

顏色

Light yellow to yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 100 mg/mL (256.75 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.5675 mL 12.8373 mL 25.6746 mL
5 mM 0.5135 mL 2.5675 mL 5.1349 mL
查看完整儲(chǔ)備液配制表

* 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(chǔ)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(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn)：

請根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 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

  • 方案 一

    請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.42 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

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

    Solubility: 2.5 mg/mL (6.42 mM); 懸濁液; 超聲助溶

    此方案可獲得 2.5 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
動(dòng)物溶解方案計(jì)算器
請輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
請輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
請確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料
參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 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(chǔ)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(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5675 mL 12.8373 mL 25.6746 mL 64.1865 mL
5 mM 0.5135 mL 2.5675 mL 5.1349 mL 12.8373 mL
10 mM 0.2567 mL 1.2837 mL 2.5675 mL 6.4187 mL
15 mM 0.1712 mL 0.8558 mL 1.7116 mL 4.2791 mL
20 mM 0.1284 mL 0.6419 mL 1.2837 mL 3.2093 mL
25 mM 0.1027 mL 0.5135 mL 1.0270 mL 2.5675 mL
30 mM 0.0856 mL 0.4279 mL 0.8558 mL 2.1396 mL
40 mM 0.0642 mL 0.3209 mL 0.6419 mL 1.6047 mL
50 mM 0.0513 mL 0.2567 mL 0.5135 mL 1.2837 mL
60 mM 0.0428 mL 0.2140 mL 0.4279 mL 1.0698 mL
80 mM 0.0321 mL 0.1605 mL 0.3209 mL 0.8023 mL
100 mM 0.0257 mL 0.1284 mL 0.2567 mL 0.6419 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產(chǎn)品名稱：
R-IMPP
目錄號：
HY-101354
需求量：