| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vivo |
Oral administration of SSTR5 antagonist 2 (10 mg/kg) in mice results in an increase in both the total and active levels of circulating incretin hormone GLP1 [1]. When coupled with DPP4 inhibitors, SSTR5 antagonist 2 has a synergistic effect that increases pancreatic insulin secretion as well as total and active GLP1 release [1].
|
|---|---|
| Animal Protocol |
Animal/Disease Models: Rodent diabetes model without risk of hypoglycemia [1].
Doses: 10 mg/kg. Mode of Route of Administration: Orally. Experimental Results: Both total and active levels of the circulating incretin hormone GLP1 were increased. |
| References |
| Molecular Formula |
C32H35FN2O5
|
|---|---|
| Molecular Weight |
546.629112482071
|
| Exact Mass |
546.253
|
| CAS # |
1254730-81-8
|
| Related CAS # |
SSTR5 antagonist 2 hydrochloride;SSTR5 antagonist 2 TFA;1254733-98-6
|
| PubChem CID |
49800498
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
6.01
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
40
|
| Complexity |
832
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C(O)(=O)C1=CC=C(N2C(=O)CC3(CCN(CC4=CC(OCC)=C(C5=CC=C(F)C=C5)C(OCC)=C4)CC3)C2)C=C1
|
| InChi Key |
BLQCUVNVAODGCA-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C32H35FN2O5/c1-3-39-27-17-22(18-28(40-4-2)30(27)23-5-9-25(33)10-6-23)20-34-15-13-32(14-16-34)19-29(36)35(21-32)26-11-7-24(8-12-26)31(37)38/h5-12,17-18H,3-4,13-16,19-21H2,1-2H3,(H,37,38)
|
| Chemical Name |
4-[8-[[3,5-diethoxy-4-(4-fluorophenyl)phenyl]methyl]-3-oxo-2,8-diazaspiro[4.5]decan-2-yl]benzoic acid
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~45.73 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.57 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 25.0 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: ≥ 2.5 mg/mL (4.57 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 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8294 mL | 9.1470 mL | 18.2939 mL | |
| 5 mM | 0.3659 mL | 1.8294 mL | 3.6588 mL | |
| 10 mM | 0.1829 mL | 0.9147 mL | 1.8294 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.
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