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  2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. ROR
  4. SR2211

SR2211 是 RORγ 有效的，選擇性合成調(diào)節(jié)劑，可作為逆向激動劑發(fā)揮功能，其 Ki 值為 105 nM，IC50 值為 ~320 nM。

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SR2211 Chemical Structure

SR2211 Chemical Structure

CAS No. : 1359164-11-6

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥2437
In-stock
1 mg ￥899
In-stock
5 mg ￥2100
In-stock
10 mg ￥3525
In-stock
25 mg ￥5000
In-stock
50 mg 現(xiàn)貨 詢價
100 mg 現(xiàn)貨 詢價
200 mg   詢價  
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Customer Review

查看 ROR 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

SR2211 is a potent, selective synthetic RORγ modulator and functions as an inverse agonist, with a Ki of 105 nM and an IC50 of ~320 nM.

IC50 & Target

IC50: ~320 nM (RORγ), Ki: 105 nM (RORγ)[1][2].
細胞效力
(Cellular Effect)
Cell Line Type Value Description References
CWR22R IC50
10.13 μM
Compound: 1; SR2211
Antiproliferative activity against human 22Rv1 cells assessed as cell viability incubated for 96 hrs by Cell-Titer Glo assay
Antiproliferative activity against human 22Rv1 cells assessed as cell viability incubated for 96 hrs by Cell-Titer Glo assay
[PMID: 34121397]
CWR22R IC50
6.42 μM
Compound: 2; SR2211
Antiproliferative activity against human 22Rv1 cells measured after 96 hrs by celltiter-glo assay
Antiproliferative activity against human 22Rv1 cells measured after 96 hrs by celltiter-glo assay
[PMID: 30964293]
DU-145 IC50
45.69 μM
Compound: 2; SR2211
Antiproliferative activity against human DU145 cells measured after 72 hrs by celltiter-glo assay
Antiproliferative activity against human DU145 cells measured after 72 hrs by celltiter-glo assay
[PMID: 30964293]
HEK293 EC50
320 nM
Compound: 13, SR2211
Agonist activity at RoRc-LBD (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 reporter assay
Agonist activity at RoRc-LBD (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 reporter assay
[PMID: 24502334]
HEK-293T IC50
0.11 μM
Compound: 2; SR2211
Inhibition of Gal4-RORgamma-LBD (180 to 507 residues) (unknown origin) expressed in HEK293T cells after 24 hrs by dual-luciferase reporter assay
Inhibition of Gal4-RORgamma-LBD (180 to 507 residues) (unknown origin) expressed in HEK293T cells after 24 hrs by dual-luciferase reporter assay
[PMID: 27043267]
HEK-293T IC50
320 nM
Compound: SR2211
Inhibition of GAL4-fused ROR gamma (unknown origin) expressed in HEK293T cells assessed as suppression of transcriptional activity after 20 hrs
Inhibition of GAL4-fused ROR gamma (unknown origin) expressed in HEK293T cells assessed as suppression of transcriptional activity after 20 hrs
10.1039/C3MD00005B
HepG2 IC50
150 nM
Compound: 13, SR2211
Displacement of [3H]T0901317 from human RoRc expressed in HepG2 cells by scintillation proximity binding assay
Displacement of [3H]T0901317 from human RoRc expressed in HepG2 cells by scintillation proximity binding assay
[PMID: 24502334]
LNCaP IC50
5.38 μM
Compound: 1; SR2211
Antiproliferative activity against human LNCaP cells assessed as cell viability incubated for 96 hrs by Cell-Titer Glo assay
Antiproliferative activity against human LNCaP cells assessed as cell viability incubated for 96 hrs by Cell-Titer Glo assay
[PMID: 34121397]
LNCaP IC50
6.79 μM
Compound: 2; SR2211
Antiproliferative activity against human LNCAP cells measured after 96 hrs by celltiter-glo assay
Antiproliferative activity against human LNCAP cells measured after 96 hrs by celltiter-glo assay
[PMID: 30964293]
LNCaP C4-2B IC50
10.06 μM
Compound: 2; SR2211
Antiproliferative activity against human C4-2B cells measured after 96 hrs by celltiter-glo assay
Antiproliferative activity against human C4-2B cells measured after 96 hrs by celltiter-glo assay
[PMID: 30964293]
LNCaP C4-2B IC50
5.38 μM
Compound: 1; SR2211
Antiproliferative activity against human LNCaP C4-2B cells assessed as cell viability incubated for 96 hrs by Cell-Titer Glo assay
Antiproliferative activity against human LNCaP C4-2B cells assessed as cell viability incubated for 96 hrs by Cell-Titer Glo assay
[PMID: 34121397]
PC-3 IC50
24.82 μM
Compound: 2; SR2211
Antiproliferative activity against human PC3 cells measured after 72 hrs by celltiter-glo assay
Antiproliferative activity against human PC3 cells measured after 72 hrs by celltiter-glo assay
[PMID: 30964293]
體外研究
(In Vitro)

用 SR2211 處理 EL4 會抑制 IL-17 基因表達。同樣，IL-23 受體 (Il23r) 的表達被 SR2211 顯著抑制。與載體處理的細胞相比，用 SR2211 處理 EL-4 細胞會顯著抑制 IL-17 細胞內(nèi)染色[1]。

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

527.48

Formula

C26H24F7N3O
CAS 號
性狀

固體

顏色

Off-white to light brown

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : 100 mg/mL (189.58 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)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 1.8958 mL 9.4790 mL 18.9581 mL
5 mM 0.3792 mL 1.8958 mL 3.7916 mL
查看完整儲備液配制表

* 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備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-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。

  • 摩爾計算器

  • 稀釋計算器

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

動物實驗：

請根據(jù)您的 實驗動物和給藥方式 選擇適當?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

  • 方案 一

    請依序添加每種溶劑： 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.74 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，此方案實驗周期在半個月以上的動物實驗酌情使用。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中，混合均勻。

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動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。
計算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，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。
動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，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，請謹慎選擇該方案。
請確保第一步儲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

純度: 99.67%

參考文獻

完整儲備液配制表

* 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備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-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。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8958 mL 9.4790 mL 18.9581 mL 47.3952 mL
5 mM 0.3792 mL 1.8958 mL 3.7916 mL 9.4790 mL
10 mM 0.1896 mL 0.9479 mL 1.8958 mL 4.7395 mL
15 mM 0.1264 mL 0.6319 mL 1.2639 mL 3.1597 mL
20 mM 0.0948 mL 0.4740 mL 0.9479 mL 2.3698 mL
25 mM 0.0758 mL 0.3792 mL 0.7583 mL 1.8958 mL
30 mM 0.0632 mL 0.3160 mL 0.6319 mL 1.5798 mL
40 mM 0.0474 mL 0.2370 mL 0.4740 mL 1.1849 mL
50 mM 0.0379 mL 0.1896 mL 0.3792 mL 0.9479 mL
60 mM 0.0316 mL 0.1580 mL 0.3160 mL 0.7899 mL
80 mM 0.0237 mL 0.1185 mL 0.2370 mL 0.5924 mL
100 mM 0.0190 mL 0.0948 mL 0.1896 mL 0.4740 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：
SR2211
目錄號：
HY-16998
需求量：