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  2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. ROR
  4. GNE-6468

GNE-6468 是一個有效且有選擇性的 RORγ (RORc) 反向激動劑，EC50 值為 2 nM。GNE-6468 抑制 PBMC 中 IL-17 的 EC50 值為 30 nM。

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GNE-6468 Chemical Structure

GNE-6468 Chemical Structure

CAS No. : 1677668-27-7

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥4180
In-stock
1 mg ￥1600
In-stock
5 mg ￥3800
In-stock
10 mg 現(xiàn)貨 詢價
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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

GNE-6468 is a highly potent and selective RORγ (RORc) inverse agonist with an EC50 value of 13 nM for HEK-293 cell. GNE-6468 exhibits an EC50 of 30 nM for IL-17 PBMC[1].

IC50 & Target[1]

ROR-γ

2 nM (EC50)

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK-293T EC50
> 10 μM
Compound: 28, GNE-6468
Inverse agonist activity at GAL4-fused human RORb expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
Inverse agonist activity at GAL4-fused human RORb expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
[PMID: 26048793]
HEK-293T EC50
> 10 μM
Compound: 28, GNE-6468
Inverse agonist activity at GAL4-fused human RORa expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
Inverse agonist activity at GAL4-fused human RORa expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
[PMID: 26048793]
HEK-293T EC50
> 10 μM
Compound: 28, GNE-6468
Agonist activity at GAL4-fused human FXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
Agonist activity at GAL4-fused human FXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
[PMID: 26048793]
HEK-293T EC50
> 10 μM
Compound: 28, GNE-6468
Agonist activity at GAL4-fused human LXRbeta expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
Agonist activity at GAL4-fused human LXRbeta expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
[PMID: 26048793]
HEK-293T EC50
> 10 μM
Compound: 28, GNE-6468
Agonist activity at GAL4-fused human LXRalpha expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
Agonist activity at GAL4-fused human LXRalpha expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
[PMID: 26048793]
HEK-293T EC50
> 10 μM
Compound: 28, GNE-6468
Agonist activity at GAL4-fused human PXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
Agonist activity at GAL4-fused human PXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
[PMID: 26048793]
HEK-293T EC50
0.013 μM
Compound: 28, GNE-6468
Inverse agonist activity at GAL4-fused human RORc expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
Inverse agonist activity at GAL4-fused human RORc expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
[PMID: 26048793]
PBMC EC50
> 10 μM
Compound: 28, GNE-6468
Cytotoxicity against human PBMC assessed as effect on cell physiology after 48 hrs by CellTiter-Glo assay
Cytotoxicity against human PBMC assessed as effect on cell physiology after 48 hrs by CellTiter-Glo assay
[PMID: 26048793]
PBMC EC50
> 10 μM
Compound: 28, GNE-6468
Inhibition of IFNgamma production in human PBMC after 48 hrs by Sandwich ELISA
Inhibition of IFNgamma production in human PBMC after 48 hrs by Sandwich ELISA
[PMID: 26048793]
PBMC EC50
0.03 μM
Compound: 28, GNE-6468
Antiinflammatory activity in human PBMC assessed as inhibition of IL-17 production after 48 hrs by Sandwich ELISA
Antiinflammatory activity in human PBMC assessed as inhibition of IL-17 production after 48 hrs by Sandwich ELISA
[PMID: 26048793]
體內(nèi)研究
(In Vivo)

GNE-6468 (compound 28) displays high predicted clearance values in human and rodent hepatocytes (CLhep = 17 and 42 mL/min/kg, respectively) [1].

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

433.84

Formula

C23H16ClN3O4
CAS 號
性狀

固體

顏色

Light yellow to yellow

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
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)
細胞實驗： 

DMSO 中的溶解度 : 5 mg/mL (11.52 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 2.3050 mL 11.5250 mL 23.0500 mL
5 mM 0.4610 mL 2.3050 mL 4.6100 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, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(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
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
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, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1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 2.3050 mL 11.5250 mL 23.0500 mL 57.6249 mL
5 mM 0.4610 mL 2.3050 mL 4.6100 mL 11.5250 mL
10 mM 0.2305 mL 1.1525 mL 2.3050 mL 5.7625 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：
GNE-6468
目錄號：
HY-19775
需求量：