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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- CAS No.: 3069267-46-2
- 화학식: C39H45N5O7S
- 분자량:727.87
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
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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.
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Cell Line:primary hepatocytes
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Concentration:30 μM; 100 μM
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Incubation Time:24 h
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Result:Induced significant cytotoxicity at 100 μM.
Showed no significant toxicity observed at 30 μM.
Parmacokinetics
In Vivo
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.
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Animal Model:C57BL/6 (8-week-old male, ~25 g)[1]
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Dosage:10 mg/kg; 30 mg/kg; 100 mg/kg
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Administration:p.o.; single dose
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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.
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Animal Model:C57BL/6 (8-week-old male)[1]
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Dosage:100 mg/kg
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Administration:p.o.; single dose
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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.
Chemical Information
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CAS No. 3069267-46-2
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분자량 727.87
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화학식 C39H45N5O7S
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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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SSTR5/TGR5-modulator-1 Related Classifications
HY-182905 Related Classifications
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