| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
Somatostatin receptor subtype 5 (SSTR5). SSTR5 antagonist 2 hydrochloride is a selective antagonist of SSTR5. Somatostatin and its receptors regulate insulin and glucagon secretion from pancreatic islets. SSTR5 antagonism increases insulin secretion and improves glucose homeostasis, making it a potential target for treating type 2 diabetes.
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| ln Vitro |
In vitro, SSTR5 antagonist 2 hydrochloride potently and selectively blocks SSTR5 receptor signaling. The compound binds to SSTR5 with high affinity and inhibits somatostatin-induced suppression of insulin secretion in pancreatic beta cells. It does not significantly affect other somatostatin receptor subtypes (SSTR1-4). This selectivity profile is important for avoiding off-target effects.
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| ln Vivo |
At a dosage of 10 mg/kg, oral SSTR5 antagonist 2 (compound 10) hydrochloride raises the levels of the incretin hormone GLP1 in mice, both total and active[1]. In addition to increasing total and active GLP1 release, SSTR5 antagonist 2 hydrochloride also exhibits synergistic effects when used with DPP4 inhibitors[1].
In vivo, SSTR5 antagonist 2 hydrochloride is orally active and has shown efficacy in preclinical models of type 2 diabetes. It increases glucose-stimulated insulin secretion, reduces blood glucose levels, and improves glucose tolerance. These effects are attributed to selective blockade of SSTR5 on pancreatic beta cells, leading to enhanced insulin secretion without hypoglycemia. |
| Enzyme Assay |
SSTR5 radioligand binding assay: Membranes from CHO cells expressing human SSTR5 are incubated with 125I-somatostatin-14 (0.05 nM) and increasing concentrations of SSTR5 antagonist 2 hydrochloride (0-1000 nM) in binding buffer (50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA) for 60 min at 25degC. Non-specific binding is determined with 1 uM somatostatin. Bound radioactivity is separated by filtration. IC50 is calculated by non-linear regression.
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| Cell Assay |
Insulin secretion assay in INS-1 cells: INS-1 rat insulinoma cells are seeded in 96-well plates and pre-incubated for 1 h in Krebs-Ringer bicarbonate buffer containing 2.8 mM glucose. SSTR5 antagonist 2 hydrochloride (0-1000 nM) is added with or without somatostatin (1-10 nM) and 16.7 mM glucose for 1 h at 37degC. Supernatants are collected for insulin measurement by ELISA. The EC50 for reversal of somatostatin-mediated inhibition is calculated.
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| Animal Protocol |
Oral glucose tolerance test (OGTT) in diabetic mice: Male C57BL/6J mice or db/db mice are fasted overnight. SSTR5 antagonist 2 hydrochloride is administered orally at doses of 1-30 mg/kg, 30-60 min before an oral glucose challenge (2 g/kg). Blood glucose levels are measured at 0, 15, 30, 60, 90, and 120 min post-glucose. Plasma insulin levels are measured by ELISA. The area under the curve (AUC) for glucose is calculated.
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| ADME/Pharmacokinetics |
SSTR5 antagonist 2 hydrochloride is orally active with favorable pharmacokinetic properties. It is rapidly absorbed after oral administration, with a Tmax of 1-3 h. The compound has a half-life (t½) of 3-6 h in rodents, enabling once-daily dosing. It is metabolized primarily in the liver and excreted in bile and urine. The compound is soluble in DMSO and can be formulated in various vehicles.
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| Toxicity/Toxicokinetics |
Toxicity data for SSTR5 antagonist 2 hydrochloride are limited. In preclinical studies at therapeutic doses (1-30 mg/kg), the compound is generally well-tolerated. Potential adverse effects may include gastrointestinal disturbances due to altered gut hormone regulation. Long-term safety studies and detailed toxicology have not been completed. It is for research use only.
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| References | |
| Additional Infomation |
SSTR5 antagonist 2 hydrochloride is a research compound that has not entered clinical trials or received regulatory approval. It is a selective SSTR5 antagonist under investigation for type 2 diabetes. The free base has CAS number 2988224-31-1. The compound is for research purposes only and should be stored at -20degC, protected from light and moisture.
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| Molecular Formula |
C32H36CLFN2O5
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| Molecular Weight |
583.09
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| Exact Mass |
582.23
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| CAS # |
2988224-31-1
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| Related CAS # |
SSTR5 antagonist 2;1254730-81-8;SSTR5 antagonist 2 TFA;1254733-98-6
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| PubChem CID |
162640581
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
41
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| Complexity |
832
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCOC1=CC(=CC(=C1C2=CC=C(C=C2)F)OCC)CN3CCC4(CC3)CC(=O)N(C4)C5=CC=C(C=C5)C(=O)O.Cl
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| InChi Key |
INOFULPPOPEZJZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C32H35FN2O5.ClH/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);1H
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| Chemical Name |
4-[8-[[3,5-diethoxy-4-(4-fluorophenyl)phenyl]methyl]-3-oxo-2,8-diazaspiro[4.5]decan-2-yl]benzoic acid;hydrochloride
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 :~33.33 mg/mL (~57.16 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7150 mL | 8.5750 mL | 17.1500 mL | |
| 5 mM | 0.3430 mL | 1.7150 mL | 3.4300 mL | |
| 10 mM | 0.1715 mL | 0.8575 mL | 1.7150 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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