2. Metabolic Enzyme/Protease
  3. Acyltransferase
  4. Pradigastat

Pradigastat (Synonyms: LCQ-908)

製品番号: HY-16278 純度: 98.39%
取扱説明書

Pradigastat (LCQ-908) is a potent, selective and orally active diacylglycerol acyltransferase 1 (DGAT1) inhibitor. Pradigastat has anti-obesity and anti-diabetic effects.

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Pradigastat 構造式

Pradigastat 構造式

CAS 番号 : 956136-95-1

容量 価格（税別） 在庫状況 数量
10 mM * 1 mL in DMSO USD 377 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 343 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 443 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 1195 在庫あり
Estimated Time of Arrival: December 31
100 mg   お問い合わせ  
200 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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Acyltransferase アイソフォーム固有の製品をすべて表示:

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ACAT1 ACAT2 ACAT

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製品説明

Pradigastat (LCQ-908) is a potent, selective and orally active diacylglycerol acyltransferase 1 (DGAT1) inhibitor. Pradigastat has anti-obesity and anti-diabetic effects[1][2].

IC50 & Target

Diacylglycerol acyltransferase 1 (DGAT1)[1]
体外実験

Pradigastat inhibits breast cancer resistance protein (BCRP)-mediated efflux activity in a dose-dependent fashion in a BCRP over-expressing human ovarian cancer cell line with an IC50 value of 5 μM. Pradigastat inhibits OATP1B1, OATP1B3, and OAT3 activity in a concentration-dependent manner with estimated IC50 values of 1.66 μM, 3.34 μM, and 0.973 μM, respectively[2].
体内実験

Pradigastat (LCQ-908) inhibits the postprandial triglyceride levels in rats, dogs and monkeys. In rats whose lipoprotein lipase (LPL) activity has been abolished, Pradigastat reduces the postprandial accumulation of plasma triglyceride. Pradigastat decreases the postprandial rate of chylomicron triglyceride (CM-TG) secretion into the lymphatic duct and reduces the size of chylomicrons[3].
臨床実験
分子量

455.47

分子式

C₂₅H₂₄F₃N₃O₂
CAS 番号

956136-95-1
SMILES

O=C(O)C[[email protected]]1CC[[email protected]](C2=CC=C(C3=NC=C(NC4=CC=C(C(F)(F)F)N=C4)C=C3)C=C2)CC1
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 : 16.67 mg/mL (36.60 mM; ultrasonic and warming and heat to 60°C)

H2O : < 0.1 mg/mL (insoluble)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1955 mL 10.9777 mL 21.9553 mL
5 mM 0.4391 mL 2.1955 mL 4.3911 mL
10 mM 0.2196 mL 1.0978 mL 2.1955 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: ≥ 1.67 mg/mL (3.67 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.67 mg/mL (3.67 mM); Clear solution

  • 3.

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

    Solubility: ≥ 1.67 mg/mL (3.67 mM); Clear solution

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

純度: 98.39%

COA (93 KB) LCMS (123 KB)

取扱説明書 (2659 KB)
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The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

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)
× = ×
C1   V1   C2   V2

Keywords:

PradigastatLCQ-908LCQ908LCQ 908AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseDGAT1anti-obesityanti-diabeticBCRPOATPOAT3chylomicronstriglycerideInhibitorinhibitorinhibit

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製品名:
Pradigastat
製品番号:
HY-16278
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