2. GPCR/G Protein Neuronal Signaling
  3. Somatostatin Receptor
  4. SSTR5 antagonist 7

SSTR5 antagonist 7 (Compound 3p) is an orally active SSTR5 antagonist, with an IC50 of 6.2 nM against hSSTR5 and an IC50 of 25 nM against mouse-derived SSTR5. SSTR5 antagonist 7 exerts a sustained hypoglycemic effect. SSTR5 antagonist 7 can be used for the research of diabetes.

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SSTR5 antagonist 7

SSTR5 antagonist 7 Chemical Structure

CAS No. : 1628744-37-5

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SSTR5 antagonist 7 Related Antibodies

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Description

SSTR5 antagonist 7 (Compound 3p) is an orally active SSTR5 antagonist, with an IC50 of 6.2 nM against hSSTR5 and an IC50 of 25 nM against mouse-derived SSTR5. SSTR5 antagonist 7 exerts a sustained hypoglycemic effect. SSTR5 antagonist 7 can be used for the research of diabetes[1].

IC50 & Target[1]

SSTR5

6.2, 25 nM (IC50)

In Vitro

SSTR5 antagonist 7 (preincubated for 15 min, stimulated for 30 min) potently inhibits hSSTR5 (IC50 = 6.2 nM) and mouse-derived SSTR5 (IC50 = 25 nM) in CHO cells stably expressing the corresponding receptors[1].

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

SSTR5 antagonist 7 Related Antibodies
Parmacokinetics
Species Dose Route AUC MRT Vdss CLtotal Cmax Tmax Bioavailability
Mice[1] 0.1 mg/kg i.v. 173.8 ng·h/mL 3.40 h 2013 mL/kg 591 mL/h/kg / / /
Mice[1] 1.0 mg/kg p.o. 1479 ng·h/mL 3.90 h / / 260 ng/mL 2.70 h 85 %
In Vivo

Compound 3p (3 mg/kg; p.o.; single administration) exerts potent and sustained hypoglycemic effects in high-fat diet-fed C57BL/6J Jcl mice[1].

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

Animal Model: C57BL/6J Jcl (male, 9 weeks of age, high-fat diet-fed)[1]
Dosage: 3 mg/kg
Administration: p.o.; single dose
Result: Exhibited a persistent glucose-lowering effect comparable to positive control compound 3a at 100 mg/kg.
Reached a plasma concentration of 0.484 μg/mL at 8 hours after dosing.
Reduced blood glucose levels significantly relative to vehicle control at multiple time points after glucose loading.
Achieved a 21% reduction in blood glucose area under the curve (BG-AUC) relative to vehicle.
Molecular Weight

542.04

Formula

C29H33ClFN3O4
CAS No.
SMILES

O=C(C1(CCN(CC1)C2=NOC3(CN(C3)CC4=C(OC)C(Cl)=C(C5=CC=C(F)C=C5)C(C6CC6)=C4)C2)C)O
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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
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SSTR5 antagonist 7 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 antagonist 71628744-37-5Somatostatin ReceptorSSTRsSSTRsomatostatin receptor subtype 5CHO cellssomatostatindiabeteshuman SSTR5mouse SSTR5pancreatic hormone secretionhigh-fat diet-fed C57BL/6J Jcl micegastrointestinal hormone secretionInhibitorinhibitorinhibit

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