2. GPCR/G Protein Neuronal Signaling
  3. Somatostatin Receptor G protein-coupled Bile Acid Receptor 1
  4. SSTR5/TGR5-modulator-1

SSTR5/TGR5-modulator-1 is an orally active and dual-target small molecule, balanced in vitro activity at human TGR5 and human SSTR5. SSTR5/TGR5-modulator-1 activates human TGR5 to promote cAMP accumulation. SSTR5/TGR5-modulator-1 blocks human SSTR5 to inhibit agonist-induced calcium mobilization. SSTR5/TGR5-modulator-1 improves glucose tolerance in mice. SSTR5/TGR5-modulator-1 alleviates gallbladder filling in mice at pharmacologically relevant doses. SSTR5/TGR5-modulator-1 has suboptimal physicochemical and metabolic properties.SSTR5/TGR5-modulator-1 can be used for the research of type 2 diabetes mellitus.

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SSTR5/TGR5-modulator-1

SSTR5/TGR5-modulator-1 Chemical Structure

CAS No. : 3069267-46-2

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SSTR5/TGR5-modulator-1 Related Antibodies

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Description

SSTR5/TGR5-modulator-1 is an orally active and dual-target small molecule, balanced in vitro activity at human TGR5 and human SSTR5. SSTR5/TGR5-modulator-1 activates human TGR5 to promote cAMP accumulation. SSTR5/TGR5-modulator-1 blocks human SSTR5 to inhibit agonist-induced calcium mobilization. SSTR5/TGR5-modulator-1 improves glucose tolerance in mice. SSTR5/TGR5-modulator-1 alleviates gallbladder filling in mice at pharmacologically relevant doses. SSTR5/TGR5-modulator-1 has suboptimal physicochemical and metabolic properties.SSTR5/TGR5-modulator-1 can be used for the research of type 2 diabetes mellitus[1].

IC50 & Target

SSTR5

4.37 nM (IC50)

In Vitro

SSTR5/TGR5-modulator-1 (Compound 19) (30 min (cAMP assay); 10 min (calcium assay pre-incubation)) potently activates human TGR5 (EC50=5.91 nM) and antagonizes human SSTR5 (IC50=4.37 nM) in vitro[1].
SSTR5/TGR5-modulator-1 (30 min (cAMP assay); 10 min (calcium assay pre-incubation)) exhibits comparable cross-species potency, activating mouse TGR5 (EC50=3.40-5.30 nM) and antagonizing mouse SSTR5 (IC50=2.97-19.6 nM) in vitro[1].
SSTR5/TGR5-modulator-1 (1 μM; up to 60 min) shows rapid metabolic turnover in in vitro, with a T1/2 of 2.2 min in human liver microsomes and 2.8 min in mouse liver microsomes[1].
SSTR5/TGR5-modulator-1 (30-100 μM; 24 h) is non-toxic to primary hepatocytes at 30 μM but induces significant cytotoxicity at 100 μM after 24 h incubation[1].

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

SSTR5/TGR5-modulator-1 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: primary hepatocytes
Concentration: 30 μM; 100 μM
Incubation Time: 24 h
Result: Induced significant cytotoxicity at 100 μM.
Showed no significant toxicity observed at 30 μM.
Parmacokinetics
Species Dose Route T1/2 AUClast Clearance (CL) Vss_obs Tmax Cmax Bioavailability
Mice[1] 50 mg/kg p.o. 0.99 h 1646 ng·h/mL / / 0.25 h 1387 ng/mL 16 %
Mice[1] 2 mg/kg i.v. 1.16 h 417 ng·h/mL 81.8 mL/min/kg 3.61 L/kg / / /
In Vivo

SSTR5/TGR5-modulator-1 (Compound 19) (10-100 mg/kg; p.o.; single dose) produces a dose-dependent improvement in oral glucose tolerance in male C57BL/6 mice, with the 100 mg/kg dose showing greater efficacy than the 50 mg/kg positive control[1].
SSTR5/TGR5-modulator-1 (100 mg/kg; p.o.; single dose) attenuates TGR5-mediated gallbladder filling in male C57BL/6 mice compared to the TGR5 agonist monotherapy control[1].
SSTR5/TGR5-modulator-1 (100 mg/kg; p.o.; single dose) enhances the GLP-1-insulin axis in male C57BL/6 mice, supporting its glucose-lowering mechanism of action[1].

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

Animal Model: C57BL/6 (8-week-old male, ~25 g)[1]
Dosage: 10 mg/kg; 30 mg/kg; 100 mg/kg
Administration: p.o.; single dose
Result: Demonstrated dose-dependent suppression of blood glucose levels.
Elicited a greater glucose-lowering effect at 100 mg/kg than positive control compound 2 at 50 mg/kg.
Significantly reduced the area under the plasma glucose curve (AUC0-90 min) at all tested doses compared to vehicle control.
Animal Model: C57BL/6 (8-week-old male)[1]
Dosage: 100 mg/kg
Administration: p.o.; single dose
Result: Reduced gallbladder size compared to both vehicle control subgroup without egg yolk stimulation and compound 2 (50 mg/kg)-treated group, indicating a weaker effect on gallbladder filling.
Molecular Weight

727.87

Formula

C39H45N5O7S
CAS No.
SMILES

O=C([C@H]1N(CSC1)CC2=C(C=C(C(OC)=C2)CN3CCC4(CC3)OC(N(C4)C5=CC=C(C=C5)C(O)=O)=O)OC)N6CCN(C7=C6C=CC=C7)C8CC8
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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SSTR5/TGR5-modulator-1 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:

SSTR5/TGR5-modulator-13069267-46-2Somatostatin ReceptorG protein-coupled Bile Acid Receptor 1SSTRsSSTRG-protein coupled receptor 19GPCR19TGR5GPBAR1primary hepatocytesmouse TGR5calcium mobilizationhuman liver microsomeshuman SSTR5type 2 diabetes mellituscAMPmicemouse SSTR5human TGR5Inhibitorinhibitorinhibit

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