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1mg |
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5mg |
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10mg |
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Other Sizes |
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ln Vitro |
SSTR5 antagonist 1 (compound 25a) reduced hERG activity by 5.6% at 30 μM[1]. The inhibitory effect of SSTR5 antagonist 1 (10 μM) on SSTR5 is higher than that of SSTR1-4, with respective inhibition rates of 11%, 8%, 14%, and 10% [1]. On both human and mouse microsomes, SSTR5 antagonist 1 (1 μM; 15 min and 30 min) shows good metabolic stability, with in vitro CLint values of <10 μL/min/kg (HLM) and 19 μL/min/kg (MLM), respectively [1].
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ln Vivo |
In pharmacokinetic screens, SSTR5 antagonist 1 (compound 25a) (1 mg/kg; oral; single dose) was given orally with good solubility (260 μg/mL, pH= 6.8) and acceptable mouse plasma exposure[1]. In C57BL/6J mice fed a high-fat diet, SSTR5 antagonist 1 (100 mg/kg; oral; single dose; measured 0-120 minutes) lowers blood glucose concentrations and increases insulin secretion in a glucose-dependent manner [1]. In C57BL/6J mice given a high-fat diet, SSTR5 antagonist 1 (1, 3, 10, and 30 mg/kg; oral; single dose) exhibits a dose-dependent effect on glucose excursions as assessed by an oral glucose tolerance test [1]. Male ICR mice (8 weeks old) with respect to pharmacokinetic characteristics [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 (h) AUC0-8 h (ng·h/mL) F (%) po 1 74.8 2.0 332 58
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Animal Protocol |
Animal/Disease Models: C57BL/6J mice fed with high-fat diet [1]
Doses: 100 mg/kg Doses: po (oral gavage); single dose; monitoring over 2 hrs (hrs (hours)) Experimental Results: demonstrated maximum efficacy better than 10 mg/kg glibenclamide and equivalent to 30 mg/kg alogliptin . Increases insulin secretion in a glucose-dependent manner and exhibits hypoglycemic effects, indicating its antidiabetic efficacy in vivo. |
References |
Molecular Formula |
C28H34FN3O5
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Molecular Weight |
511.585071086884
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Exact Mass |
511.248
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CAS # |
1628741-91-2
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PubChem CID |
90423921
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Appearance |
White to off-white solid powder
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LogP |
1.1
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Hydrogen Bond Donor Count |
1
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Hydrogen Bond Acceptor Count |
8
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Rotatable Bond Count |
9
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Heavy Atom Count |
37
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Complexity |
790
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Defined Atom Stereocenter Count |
0
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SMILES |
FC1C=CC(=CC=1)C1=C(C=C(C=C1OCC)CN1CC2(CC(=NO2)N2CCC(C(=O)O)CC2)C1)OCC
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InChi Key |
UQRAIIGEZLINAT-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C28H34FN3O5/c1-3-35-23-13-19(14-24(36-4-2)26(23)20-5-7-22(29)8-6-20)16-31-17-28(18-31)15-25(30-37-28)32-11-9-21(10-12-32)27(33)34/h5-8,13-14,21H,3-4,9-12,15-18H2,1-2H3,(H,33,34)
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Chemical Name |
1-[2-[[3,5-diethoxy-4-(4-fluorophenyl)phenyl]methyl]-5-oxa-2,6-diazaspiro[3.4]oct-6-en-7-yl]piperidine-4-carboxylic acid
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~90 mg/mL (~175.92 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.25 mg/mL (4.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.25 mg/mL (4.40 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.25 mg/mL (4.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.9547 mL | 9.7735 mL | 19.5469 mL | |
5 mM | 0.3909 mL | 1.9547 mL | 3.9094 mL | |
10 mM | 0.1955 mL | 0.9773 mL | 1.9547 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.