SSTR5 antagonist 1
Based on 1 Customer Validation
SSTR5 antagonist 1 (compound 25a) is a selective and orally available somatostatin receptor subtype 5 (SSTR5) antagonist with IC50s of 9.6 and 57 nM for hSSTR5 and mSSTR5, respectively.
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- Purity: 99.91%
- CAS No.: 1628741-91-2
- 화학식: C28H34FN3O5
- 분자량:511.59
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
IC50: 9.6 nM (hSSTR5), 57 nM (mSSTR5)[1]
SSTR5 antagonist 1 (compound 25a) (30 μM) inhibits hERG activity by 5.6%[1].
SSTR5 antagonist 1 (10 μM) shows highly selective inhibitory effect on SSTR5 over SSTR1-4, with inhibition rates of 11%, 8%, 14%, 10%[1].
SSTR5 antagonist 1 (1 μM; 15 min and 30 min) exhibits good metabolic stability toward both human and mouse microsomes with in vitro CLint value of <10 μL/min/kg (HLM) and 19 μL/min/kg (MLM), respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SSTR5 antagonist 1 (100 mg/kg; p.o.; single dose; measured at 0-120 min) augments insulin secretion in a glucose-dependent manner and lowers blood glucose concentration in high-fat diet fed C57BL/6J mice[1].
SSTR5 antagonist 1 (1, 3, 10, and 30 mg/kg; p.o.; single dose) shows dose-dependent effect on glucose excursion measured during the oral glucose tolerance test in HFD fed C57BL/6J mice[1].
Pharmacokinetic profiles in male ICR mouse (8-week-old)[1]
| Route | Dose (mg/kg) | CLtotal (mL/h/kg) | Vss (mL/kg) | MRT (h) | |
| iv | 0.1 | 1761 | 3052 | 1.7 | / |
| Route | Dose (mg/kg) | Cmax (ng/mL) | Tmax |
AUC0-8 h |
F (%) |
| po | 1 | 74.8 | 2.0 | 332 | 58 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:High-fat diet fed C57BL/6J mice[1]
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Dosage:100 mg/kg
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Administration:Oral gavage; single dose; monitored over 2 h
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Result:Showed the maximum efficacy superior to that of 10 mg/kg Glibenclamide (HY-15206) and comparable to that of 30 mg/kg Alogliptin (HY-A0023A).
Augmented insulin secretion in a glucose-dependent manner and displayed a blood glucose-lowering effect, indicating its anti-diabetic efficacy in vivo.
Chemical Information
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CAS No. 1628741-91-2
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Appearance Solid
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분자량 511.59
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화학식 C28H34FN3O5
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Color White to off-white
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SMILES
OC(C1CCN(C2=NOC3(CN(CC4=CC(OCC)=C(C5=CC=C(F)C=C5)C(OCC)=C4)C3)C2)CC1)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
용액&용해도
DMSO : 90 mg/mL (175.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.25 mg/mL (4.40 mM); Clear solution
This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.25 mg/mL (4.40 mM); Clear solution
This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9547 mL | 9.7735 mL | 19.5469 mL | 48.8673 mL |
| 5 mM | 0.3909 mL | 1.9547 mL | 3.9094 mL | 9.7735 mL | |
| 10 mM | 0.1955 mL | 0.9773 mL | 1.9547 mL | 4.8867 mL | |
| 15 mM | 0.1303 mL | 0.6516 mL | 1.3031 mL | 3.2578 mL | |
| 20 mM | 0.0977 mL | 0.4887 mL | 0.9773 mL | 2.4434 mL | |
| 25 mM | 0.0782 mL | 0.3909 mL | 0.7819 mL | 1.9547 mL | |
| 30 mM | 0.0652 mL | 0.3258 mL | 0.6516 mL | 1.6289 mL | |
| 40 mM | 0.0489 mL | 0.2443 mL | 0.4887 mL | 1.2217 mL | |
| 50 mM | 0.0391 mL | 0.1955 mL | 0.3909 mL | 0.9773 mL | |
| 60 mM | 0.0326 mL | 0.1629 mL | 0.3258 mL | 0.8145 mL | |
| 80 mM | 0.0244 mL | 0.1222 mL | 0.2443 mL | 0.6108 mL | |
| 100 mM | 0.0195 mL | 0.0977 mL | 0.1955 mL | 0.4887 mL |
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