2. Metabolic Enzyme/Protease GPCR/G Protein
  3. FXR G protein-coupled Bile Acid Receptor 1 GLP Receptor
  4. Colesevelam hydrochloride

Colesevelam hydrochloride is an orally active bile acid sequestrant, lipid-lowering agent, and glycemic control agent. Colesevelam hydrochloride binds bile acids in the gastrointestinal tract to form nonabsorbable complexes, interrupts enterohepatic recirculation and increases fecal bile acid elimination. Colesevelam hydrochloride modulates FXR, TGR5, and Cyp7a1 activity and triggers cAMP signaling and GLP-1 release. Colesevelam hydrochloride alters hepatic lipid and glucose metabolism, suppresses hepatic glycogenolysis, reduces hepatic triglyceride and cholesterol levels, and increases LDL-C (low-density lipoprotein cholesterol) clearance. Colesevelam hydrochloride can be used for the research of type 2 diabetes mellitus, hypercholesterolemia, and alcohol-related liver disease.

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Colesevelam hydrochloride

Colesevelam hydrochloride Chemical Structure

CAS No. : 182815-44-7

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Colesevelam hydrochloride Related Antibodies

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Description

Colesevelam hydrochloride is an orally active bile acid sequestrant, lipid-lowering agent, and glycemic control agent. Colesevelam hydrochloride binds bile acids in the gastrointestinal tract to form nonabsorbable complexes, interrupts enterohepatic recirculation and increases fecal bile acid elimination. Colesevelam hydrochloride modulates FXR, TGR5, and Cyp7a1 activity and triggers cAMP signaling and GLP-1 release. Colesevelam hydrochloride alters hepatic lipid and glucose metabolism, suppresses hepatic glycogenolysis, reduces hepatic triglyceride and cholesterol levels, and increases LDL-C (low-density lipoprotein cholesterol) clearance. Colesevelam hydrochloride can be used for the research of type 2 diabetes mellitus, hypercholesterolemia, and alcohol-related liver disease[1][2][3][4].

IC50 & Target[1]

PKA

 

In Vitro

Colesevelam hydrochloride (5 mg/mL; 45 min incubation with taurocholic acid and oleic acid, followed by real-time cell treatment) forms a complex with taurocholic acid that activates human TGR5-mediated cAMP signaling in HEK293 TGR5-BRET cells, demonstrating that bile acids bound to Colesevelam hydrochloride retain TGR5 agonist activity[1].
Colesevelam hydrochloride (1 h) maintains stable bile acid binding affinity and capacity after suspension in common beverages, exhibits greater total bile acid binding (including higher affinity for GC) than traditional bile acid sequestrants under physiological conditions, and is four to six times as potent as these traditional agents[4].

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

Colesevelam hydrochloride Related Antibodies
In Vivo

Colesevelam hydrochloride (2%; oral; ad libitum; 7 days) suppresses hepatic glycogenolysis and reduces hyperglycemia in diet-induced obese mice via a TGR5/GLP-1-dependent mechanism, while improving cholesterol metabolism via an FXR-dependent, TGR5/GLP-1-independent mechanism[1].
Colesevelam hydrochloride (rectal) complexed with taurocholic acid is sufficient to induce GLP-1 release in normal mice[1].
Colesevelam hydrochloride (2%; oral; daily; from day 6 until study end) treatment mitigates ethanol-induced liver steatosis in humanized gnotobiotic mice by reducing hepatic lipid accumulation and related gene expression, but significantly increases serum liver injury markers and does not improve intestinal barrier function[2].

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

Animal Model: C57Bl/6J wild-type (male);[1]
Dosage: 2%
Administration: oral; ad libitum; 7 days
Result: Normalized hepatic cholesterol levels.
Reduced fed plasma glucose concentrations and glucose excursion during glucose tolerance tests.
Alleviated hyperinsulinemia in diet-induced obese mice.
Decreased basal endogenous glucose production by suppressing hepatic glycogenolysis without altering gluconeogenic flux.
Elevated hepatic glycogen content in fed wild-type mice.
Animal Model: TGR5 knockout (male); FXR knockout (male)[1]
Dosage: 2%
Administration: oral; ad libitum; 7 days
Result: Increased portal GLP-1 levels in wild-type lean and obese mice but not in TGR5-knockout mice.
Blocked the suppression of hepatic glycogenolysis and attenuated glucose lowering when coadministered with the GLP-1 receptor antagonist exendin-(9–39).
Retained the ability to reduce hyperinsulinemia despite GLP-1 receptor inhibition.
Reduced hepatic cholesterol levels in both wild-type and TGR5-knockout mice.
Induced hepatic expression of the cholesterol biosynthetic genes Cyp7a1 and Hmgcs.
Increased de novo cholesterol synthesis by sevenfold.Moderately reduced plasma insulin and decreased plasma glucose similarly in FXR-knockout mice.
Animal Model: C57BL/6 (female, 5-6 weeks old, germ-free, colonized with feces from alcoholic hepatitis patients, chronic-binge ethanol feeding model)[2]
Dosage: 2% (by dry powder weight)
Administration: oral; daily; from day 6 until study end
Result: Reduced hepatic triglyceride and cholesterol levels.
Reduced hepatic mRNA expression of lipogenic and cholesterol synthesis genes (Acc1, Fasn, Hmgcr, Srebp1c) and ethanol-metabolizing genes (Adh1, Cyp2e1).
Reduced hepatic Cyp7a1 protein and Cyp27a1 mRNA expression.
Reduced hepatic Mpo (neutrophil marker) mRNA expression.
Significantly increased serum ALT and ALP levels.
Did not reduce serum bile acid levels, nor improve intestinal barrier function (serum LPS levels unchanged).
Clinical Trial
Molecular Weight

3694.64

Formula

(C3H8NCl)2.(C9H20N2OCl2).(C13H28NCl)7.(C12H28N2Cl2)6
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

[Colesevelam (hydrochloride)]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Purity & Documentation

Purity: 98.00%

SDS (252 KB)

COA (243 KB)

Handling Instructions (2659 KB)
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Colesevelam hydrochloride 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:

Colesevelam182815-44-7FXRG protein-coupled Bile Acid Receptor 1GLP ReceptorNR1H4G-protein coupled receptor 19GPCR19TGR5GPBAR1GLP-1HEK293 TGR5-BRET cellsCyp7a1type 2 diabetes mellitusalcohol-related liver diseasehypercholesterolemiacAMP signalingbile acidsInhibitorinhibitorinhibit

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