2. Vitamin D Related/Nuclear Receptor
  3. Thyroid Hormone Receptor
  4. KAT681

KAT681 is a liver-selective thyromimetic.

For research use only. We do not sell to patients.

KAT681 Chemical Structure

KAT681 Chemical Structure

CAS No. : 373641-87-3

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KAT681 Related Antibodies

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Description

KAT681 is a liver-selective thyromimetic.

IC50 & Target

Thyroid Hormone Receptor[1]
In Vitro

The impact of the liver-selective thyromimetic KAT681 (T-0681) is investigated on lipoprotein metabolism. Prolonged treatment with KAT681 increases the hepatic expression of both low-density lipoprotein (LDL) receptor and scavenger receptor class B, type I without affecting cholesteryl ester transfer protein activity. Western blot showing human SR-BI (CLA-1) expression in normal HepG2 cells and in HepG2 cells loaded with AcLDL and subsequently incubated with vehicle or KAT681. SR-BI protein expression is markedly downregulated by incubation with 50 μg/mL AcLDL. This effect can not be reversed by addition of KAT681[1]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

KAT681 Related Antibodies
In Vivo

In preliminary dose-titration studies, a marked decrease of plasma cholesterol is observed at 36 nmoles/kg/day KAT681 (T-0681), whereas doses higher than 36 nmoles/kg/day show no further lipid-lowering effect. In the subsequent study, New Zealand White (NZW) rabbits are fed a 0.2% cholesterol diet and dosed with 36 nmoles/kg/day KAT681 or a respective placebo control for 4 weeks. KAT681 treatment results in a 60% decrease of plasma cholesterol and a 70% decrease of plasma triglycerides[1]. In preliminary dose-titration studies in wild-type (WT) mice, a marked increase of hepatic SR-BI expression at 36 nmol/kg/d KAT681 (T-0681), and a concomitant 50% decrease of plasma cholesterol are observed. Higher doses than 36 nmol/kg/d show no further lipid-lowering effect. KAT681 significantly increases hepatic LDLrs in SR-BI KO mice (2-fold of controls, P<0.01), along with a marked decrease in plasma cholesterol[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

461.41

Formula

C24H21FNNaO6
CAS No.
SMILES

O=C(CC(NC1=CC(C)=C(C(C)=C1)OC2=CC=C(C(C(O)C3=CC=C(C=C3)F)=C2)O)=O)O[Na]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Cell Assay
[2]

HepG2 cells are used. At a confluency of 70%, HepG2 cells are incubated with 50 μg/mL of acetylated LDL (AcLDL) for 24 h and subsequently treated with indicated amounts of KAT681 (0.5 μM) in serum-free medium for another 24 h. Cellular protein extraction and Western blot analysis are performed.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1][2]

Rabbits[1]
Male NZW rabbits are subcutaneously implanted with Alzet osmotic pumps carrying KAT681 (36 nmoles/kg/day) in 1% DMSO/PBS or 1% DMSO/PBS alone as control for the entire duration of the studies. Rabbits are fed a 0.2% cholesterol and 3.5% fat diet or a 2% cholesterol and 5% fat diet. Food consumption is restricted to 100 g/day/animal. At the end of the studies, animals are fasted 5 h before the collection of blood samples, killed by a threefold overdose of pentobarbital, and organ biopsies snap-frozen.
Mice[2]
Male C57/B6 (WT) mice are fed a standard chow diet. After 2 weeks of acclimatization, mice are divided into two groups and subcutaneously implanted with Alzet micro-osmotic pumps carrying KAT681 in PBS (36 nmol/kg/d) or PBS alone as control for 14 days. After 14 days of treatment, animals are fasted for 5 h and anesthetized. Blood samples are taken, mice sacrificed by cervical dislocation, and organ biopsies are snap-frozen. Male SR-BI KO and LDLr KO mice are fed a standard chow diet, and subcutaneously implanted with Alzet micro-osmotic pumps carrying KAT681 in PBS (36 nmol/kg/d) or PBS alone as control. Mice are then fasted for 5 h, blood samples are taken, mice are sacrificed by cervical dislocation, and liver biopsies are snap-frozen.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
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KAT681 Related Classifications

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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.

Keywords:

KAT681373641-87-3T0681KAT 681KAT-681T 0681T-0681Thyroid Hormone ReceptorTHRInhibitorinhibitorinhibit

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