1. Metabolic Enzyme/Protease
    Autophagy
  2. FXR
    Autophagy
  3. Cilofexor

Cilofexor (Synonyms: GS-9674)

製品番号: HY-109083 純度: 99.82%
取扱説明書

Cilofexor (GS-9674) is a potent, selective and orally active nonsteroidal FXR agonist with an EC50 of 43 nM. Cilofexor has anti-inflammatory and antifibrotic effects. Cilofexor has the potential for primary sclerosing cholangitis (PSC) and nonalcoholic steatohepatitis (NASH) research.

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Cilofexor 構造式

Cilofexor 構造式

CAS 番号 : 1418274-28-8

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1  mL in DMSO USD 194 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 150 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 240 在庫あり
Estimated Time of Arrival: December 31
25 mg USD 490 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 840 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 1400 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 1 publication(s) in Google Scholar

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製品説明

Cilofexor (GS-9674) is a potent, selective and orally active nonsteroidal FXR agonist with an EC50 of 43 nM. Cilofexor has anti-inflammatory and antifibrotic effects. Cilofexor has the potential for primary sclerosing cholangitis (PSC) and nonalcoholic steatohepatitis (NASH) research[1][2].

IC50 & Target

EC50: 43 nM (FXR)[1]

体内実験

Cilofexor (GS-9674; 30 mg/kg; oral gavage; once daily; for 10 weeks; male Wistar rats) treatment significantly increases Fgf15 expression in the ileum and decreased Cyp7a1 in the liver in nonalcoholic steatohepatitis (NASH) rats. Liver fibrosis and hepatic collagen expression are significantly reduced. Cilofexor also significantly reduces hepatic stellate cell (HSC) activation and significantly decreases portal pressure, without affecting systemic hemodynamics[3].

Animal Model: Male Wistar rats received a choline-deficient high fat diet (CDHFD)[3]
Dosage: 30 mg/kg
Administration: Oral gavage; once daily; for 10 weeks
Result: Significantly increased Fgf15 expression in the ileum and decreased Cyp7a1 in the liver. Liver fibrosis and hepatic collagen expression were significantly reduced.
臨床実験
分子量

586.85

分子式

C₂₈H₂₂Cl₃N₃O₅

CAS 番号

1418274-28-8

SMILES

ClC1=C(C2(CN(C3=CC(C(O)=O)=CC=N3)C2)O)C=CC(OCC4=C(C5CC5)ON=C4C(C(Cl)=CC=C6)=C6Cl)=C1

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 50 mg/mL (85.20 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7040 mL 8.5201 mL 17.0401 mL
5 mM 0.3408 mL 1.7040 mL 3.4080 mL
10 mM 0.1704 mL 0.8520 mL 1.7040 mL
*Please refer to the solubility information to select the appropriate solvent.
体内:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.54 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.54 mM); Clear solution

*All of the co-solvents are provided by MCE.
参考文献

純度: 99.82%

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The molarity calculator equation

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

CilofexorGS-9674GS9674GS 9674FXRAutophagyNR1H4PSCnonsteroidalsafetyanti-inflammatoryantifibroticNASHoralInhibitorinhibitorinhibit

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製品名:
Cilofexor
製品番号:
HY-109083
数量:
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