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Cat. No.: HY-183205

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SSTR5 antagonist 7

SSTR5 antagonist 7 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.

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

CAS No.: 1628744-37-5
Formula: C₂₉H₃₃ClFN₃O₄
Molecular Weight:542.04

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

SSTR5 antagonist 7 Chemical Structure

CAS No.: 1628744-37-5

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

SSTR5

6.2, 25 nM (IC₅₀)

All Somatostatin Receptor Isoforms :

In Vitro

SSTR5 antagonist 7 (Compound 3p) (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.

Parmacokinetics

Species	Dose	Route	AUC	MRT	V_dss	CL_total	C_max	T_max	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.

Chemical Information

CAS No. 1628744-37-5
Molecular Weight 542.04
Formula C₂₉H₃₃ClFN₃O₄
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
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

Handling Instructions (2659 KB)

References

[1]. Yamasaki T, et al. Discovery of novel somatostatin receptor subtype 5 (SSTR5) antagonists: Pharmacological studies and design to improve pharmacokinetic profiles and human Ether-a-go-go-related gene (hERG) inhibition. Bioorg Med Chem. 2017 Aug 1;25(15):4153-4162. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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